Composition and Methods for Stimulating Gastrointestinal Motility

- Ipsen Pharma S.A.S.

The present invention relates to a method of treating a transient impairment of the motility of the gastrointestinal system resulting from postoperative ileus in a patient wherein said method includes the step of administering a therapeutically effective amount of a peptidyl analog of ghrelin to said patient.

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Description

This application is a divisional application of pending U.S. Ser. No. 15/333,240, filed Oct. 25, 2016, which is a continuation application of pending U.S. Ser. No. 14/628,379, filed Feb. 23, 2015, which issued as U.S. Pat. No. 9,499,599 on Nov. 22, 2016, which is a continuation application of U.S. Ser. No. 13/046,324, filed Mar. 11, 2011, which issued as U.S. Pat. No. 8,981,054 on Mar. 17, 2015, which is a continuation application of pending U.S. Ser. No. 11/992,780, filed Mar. 29, 2008, which issued as U.S. Pat. No. 7,932,231 on Apr. 26, 2011, which is a United States national filing under 35 U.S.C. § 371 of international (PCT) application No. PCT/US2006/038027, filed Sep. 28, 2006 and designating the US, which claims priority to U.S. provisional application No. 60/721,916, filed Sep. 29, 2005, each of which is herein incorporated by reference in its entirety.

SEQUENCE LISTING

The instant application contains a Sequence Listing which has been submitted in ASCII format via EFS-Web, and is hereby incorporated by reference in its entirety. The ASCII copy, is named “149P_PCT2_USA_SEQ_LISTING_ST25.txt”, created on Feb. 23, 2015, and has the file size of 228,000 bytes.

BACKGROUND OF THE INVENTION Field of the Invention

The present invention is directed to methods for stimulating the motility of the gastrointestinal system in a patient which comprises administering peptidyl analogs that possess agonistic ghrelin activity, a prodrug thereof, or a pharmaceutically acceptable salt of said analogs or said prodrug.

Description of the Related Art

Gastrointestinal (GI) motility is a coordinated neuromuscular process that transports nutrients through the digestive system (Scarpignato, C., Dig. Dis., (1997), 15:112), the impairment of which may result in a variety of ailments including gastroesophageal reflux disease (GERD), gastroparesis (e.g., diabetic and post-surgical), irritable bowel syndrome (IBS), constipation (e.g. that associated with the hypomotility phase of IBS), emesis (e.g., that caused by cancer chemotherapy agents), ileus and colonic pseudo-obstruction (U.S. Pat. No. 6,548,501; U.S. Patent Application No. 20040266989). These various complications of interrupted GI motility contribute significantly to the health care burdens of industrialized nations (U.S. Pat. No. 6,548,501; Feighner, S. D. et al., Science, (1999), 284:2184-8).

“Ileus” refers to the obstruction of the bowel or gut, especially the colon (see, e.g., Dorland's Illustrated Medical Dictionary, p. 816, 27th ed. (W.B. Saunders Company, Philadelphia 1988)). Generally, any trauma to the bowel resulting in the release of inflammatory mediators leading to activation of inhibitory neural reflexes will result in the onset of ileus. Ileus may be diagnosed by the disruption of the normal coordinated movements of the gut, resulting in failure of the propulsion of intestinal contents (Resnick, J., Am. J. of Gastroentero., (1997), 92:751; Resnick, J., Am. J. of Gastroentero., (1997), 92:934). Ileus should be distinguished from constipation, which refers to infrequent or difficulty in evacuating the feces (see, e.g., Dorland's Illustrated Medical Dictionary, p. 375, 27th ed. (W.B. Saunders Company, Philadelphia 1988)).

Ileus may be brought about by a variety of causes such as parturition; intestinal ischaemia; retroperitoneal haematoma; intraabdominal sepsis; intraperitoneal inflammation, e.g., acute appendicitis, choecystitis, pancreatitis; fractures of the spine; ureteric colic; thoracic lesions; basal pneumonia; rib fractures; myocardial infarction; and metabolic disturbances. Post-partum ileus is a common problem for women in the period following childbirth and is thought to be caused by fluctuations in natural opioid levels as a result of birthing stress. Patients having undergone procedures such as major abdominal surgery including laparotomy for abdominal abscess or small intestinal transplantation (SITx), chest, pelvic or orthopedic surgery, often suffer from a period of transient impairment of bowel function called post-surgical or post-operative ileus (referred to hereinafter as POI).

POI commonly occurs for 24 to 72 hours following surgery. In some instances, the bowel dysfunction may become quite severe, lasting for more than a week and affecting more than one portion of the GI tract (Livingston, E. H. et al., Digest. Dis. and Sci., (1990), 35:121). Gastrointestinal dysmotility associated with POI is generally most severe in the colon. POI is characterized by abdominal nausea, distension, vomiting, obstipation, inability to eat and cramps. POI not only delays the normal resumption of food intake after surgery and prolongs hospitalization, but also fosters postoperative complications, especially aspiration pneumonia.

The administration of opioid analgesics to a patient after surgery may often contribute to and/or exacerbate existing bowel dysfunction, thereby delaying recovery of normal bowel function. Since virtually all patients receive opioid analgesics, such as morphine or other narcotics for pain relief after surgery, particularly major surgery, current post-surgical pain treatment may actually slow recovery of normal bowel function, resulting in a delay in hospital discharge and increasing the cost of medical care.

Agents which act to affect gastrointestinal motility may also confer beneficial effects upon patients suffering from emesis. Emesis, or vomiting, is often preceded by retching and may be accompanied by dry heaves. Emesis may be caused by imbalances in the digestive tract, such as ileus, dyspepsia, or inflammation of the gastric wall, or by imbalances in the sensory system or brain, such as motion sickness, migraine or tumors. Emesis may be self-induced such as in anorexia or bulimia, and it may also occur in response to severe pain, emotional responses (e.g., to disagreeable sights or odors), or pregnancy. Emesis is a common complication following the administration of many medications, particularly anti-cancer treatments such as chemotherapy. Prolonged episodes or repetitive emesis may result in a variety of injuries to the organism, including dehydration and electrolyte imbalances (Quigley, E. M. et al., Gastroentero., (2001), 120:263-86).

Agents which act to affect gastrointestinal motility may also confer beneficial effects upon patients suffering from gastroparesis. Gastroparesis, also called delayed gastric emptying, is a disorder in which the nerves to the stomach are damaged or stop working and the stomach takes too long to empty its contents. For example, following damage to the vagus nerve, the nerve which controls the movement of food through the digestive tract, the muscles of the stomach and intestines do not work normally and the movement of food is slowed or stopped. High blood glucose causes chemical changes in nerves and damages the blood vessels that carry oxygen and nutrients to the nerves. If blood glucose levels remain high over a long period of time, as is often the case in diabetes, the vagus nerve can be damaged; gastroparesis often occurs in people with type 1 diabetes or type 2 diabetes (Murray, C. D. et al., Gut, (2005), 54:1693-8).

The traditional therapies for impaired GI motility, such as that of ileus, gastroparesis and emesis, are considered ineffective. Current therapies for treating ileus include functional stimulation of the intestinal tract, stool softeners, laxatives such as Dulcolax®, lubricants, intravenous hydration, nasogastric suction, prokinetic agents, early enteral feeding, and nasogastric decompression. Nasogastric intubation to decompress the stomach has also traditionally been used to treat ileus.

Traditional pharmaceuticals used to treat impaired GI motility, such as that of ileus, include drugs that act to increase colonic motility, such as Leu13-motilin and prostaglandin F2 alpha, and prokinetic agents, such as Cisapride®. PROPULSID®, which contains Cisapride® monohydrate, is an oral gastrointestinal agent (U.S. Pat. No. 4,962,115) indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. Other prokinetic agents include, for example, metoclopramide, domperidone, ondansetron, tropisetron, mosapride and itopride. Other treatments include administering adenosine-antagonizing pyrazolopyridine compounds (U.S. Pat. No. 6,214,843); pituitary adenylate cyclase activating peptide (PACAP) receptor antagonist in combination with a vasoactive intestinal peptide (VIP) receptor antagonist (U.S. Pat. No. 6,911,430); fedotozine (U.S. Pat. No. 5,362,756); neuropeptides (U.S. Pat. No. 5,929,035); and proteinase-activated receptor-2 antagonists (U.S. Pat. No. 5,929,035). In extreme cases, ileus has been treated with surgical intervention to unblock the colon.

These therapeutic regimens, however, suffer from numerous problems. For instance, PROPULSID® was recently removed from the market due to its potential to induce cardiac arrhythmias (U.S. Pat. No. 6,548,501). Adolor Corporation is presently in phase III clinical trials for a therapy to treat postoperative ileus using Alvimopan (Entereg®). Adolor's therapy, however, utilizes opioid receptor antagonists which merely block the side effects of opiate analgesics, rather than actually relieving the ileus condition. The phase III trials demonstrate marginal efficacy and minimal applicability for the treatment of ileus, particularly postoperative ileus.

Furthermore, these prior art methods for treatment of impaired GI motility lack specificity for different types of impairments, e.g., postoperative ileus or post-partum ileus. Also, these prior art methods offer no means for the prevention of impaired GI motility, such as that of ileus, gastroparesis and emesis. If impaired GI motility, such as that of ileus, gastroparesis and emesis, could be prevented or more effectively treated, hospital stays, recovery times, and medical costs would be significantly decreased with the additional benefit of minimizing patient discomfort.

Drugs which selectively target gut motility to correct gastrointestinal dysfunction caused by postoperative ileus would be ideal candidates for preventing and/or treating post-surgical and post-partum ileus. Such drugs would also be excellent candidates for the treatment of gastroparesis and/or emesis, particularly emesis associated with chemotherapies or other drug induced gastrointestinal dysfunction. Of those, drugs that do not interfere with the effects of opioid analgesics would be of special benefit in that they may be administered simultaneously with drugs for pain management with limited side effects.

Peptides affecting the release of growth hormone (GH) are now thought to exhibit gastrokinetic or “prokinetic” effects (U.S. Pat. No. 6,548,501; Peeters, T. L., J Physiol. Pharmacol., (2003), 54 (supp 4):95-103 and references therein; Trudel, L. et al, J. Physiol. Gastrointest. Liver Physiol., (2002), 282:G948-52). Such growth hormone-releasing peptides, or GHRPs, are also referred to as growth hormone secretagogues (GHS). Exemplary growth hormone-releasing peptides (GHRPs) believed to exhibit prokinetic effects include GHRP-1, GHRP-2 and ghrelin.

Ghrelin, a recently discovered orexigenic hormone, is produced as a preprohormone that is proteolytically processed to yield a peptide of the following sequence: H-Gly-Ser-Ser-Phe-Leu-Ser-Pro-Glu-His-Gln-Arg-Val-Gln-Gln-Arg-Lys-Glu-Ser-Lys-Lys-Pro-Pro-Ala-Lys-Leu-Gln-Pro-Arg-NH2 (Kojima, M. et al., Nature, (1999), 402(6762):656-60; (SEQ ID NO:338)). Ghrelin is produced by epithelial cells lining the fundus of the stomach and functions to stimulate appetite; its levels increase prior to a meal and decrease thereafter.

Ghrelin powerfully stimulates GH secretion from the anterior pituitary gland, mainly at the hypothalamic level, through its interaction with growth hormone secretagoue receptor (GHS-R) both in animals and in humans (Ukkola, O. et al., 2002 Ann. Med., (2002), 34:102-8; (Kojima, M. et al., Nature, (1999), 402(6762):656-60).

The native structures of ghrelin from several mammalian and non-mammalian species are known (Kaiya, H. et al., J. of Biol. Chem., (2001), 276:40441-8 and International Patent Application PCT/JP00/04907 [WO 01/07475]). A core region present in ghrelin is responsible for observed activity at the GHS receptor. The core region comprises the four N-terminal amino acids wherein the serine in the third position is normally modified with n-octanoic acid. In addition to acylation by n-octanoic acid, native ghrelin may also be acylated with n-decanoic acid (Kaiya, H. et al., J. of Biol. Chem., (2001), 276:40441-8).

Prior to the discovery that ghrelin is a native ligand for the GHS receptor, it was known that GHRPs controlled the release of growth hormone from the pituitary somatotrops. The hexapeptide His-D-Trp-Ala-Trp-D-Phe-Lys-amide (GHRP-6; (SEQ ID NO:342)), was found to release growth hormone from the somatotrops in a dose-dependent manner in several species including man (Bowers, C. Y. et al., Endocrinology, (1984), 114(5):1537-45). Subsequent chemical studies on GHRP-6 led to the identification of other potent, synthetic GHSs such as GHRP-I, GHRP-2 and hexarelin (Cheng, K. et al., Endocrinology, (1989), 124(6):2791-8; Bowers, C. Y., Novel GH-Releasing Peptides, Molecular and Clinical Advances in Pituitary Disorders, Ed: Melmed, S., Endocrine Research and Education, Inc., Los Angeles, Calif., USA, (1993), 153-7; and Deghenghi, R. et al., Life Sci., (1994), 54(18):1321-8). The structures of these compounds are as shown:

GHRP-I (SEQ ID NO: 339) Ala-His-D-(2′)-Nal-Ala-Trp-D-Phe-Lys-NH2; GHRP-2 (SEQ ID NO: 340) D-Ala-D-(2′)-Nal-Ala-Trp-D-Nal-Lys-NH2; and Hexarelin (SEQ ID NO: 341) His-D-2-MeTrp-Ala-Trp-D-Phe-Lys-NH2.

GHRP-I, GHRP-2, GHRP-6, and hexarelin are classified as synthetic GHSs.

A number of recent studies have demonstrated the potential use of GHSs such as ghrelin, GHRP-6 and others to stimulate motor activity in the intestinal tract and to treat conditions such as ileus and emesis. For example, ghrelin and GHRP-6 have been shown to accelerate gastric emptying in rats and mice (Peeters, T. L., J Physiol. Pharmacol., (2003), 54 (supp 4):95-103). In rats, ghrelin has been shown to reverse the delay of gastric emptying in a post-operative ileus model (Peeters, T. L., J Physiol. Pharmacol., (2003), 54 (supp 4):95-103; Trudel, L. et al., J. Physiol. Gastrointest. Liver Physiol., (2002), 282(6):G948-52) and in laparectomized dogs, ghrelin was shown to improve POI in the treated animals (Trudel, L. et al, Peptides, (2003), 24:531-4). In septic mice, ghrelin and GHRP-6 accelerated gastric emptying although had little effect upon increasing transit in the small intestine (De Winter, B. Y. et al., Neurogastroenterol. Motil., (2004), 16:439-46).

In experiments designed to mimic hospitalization conditions for a human patient experiencing POI, laparectomized rats were exposed to opiates as well as ghrelin analog RC-1139 (Poitras, P. et al., Peptides, (2005), 26:1598-601). In an assay measuring gastric empyting, RC-1139 was shown to reverse POI in the control and laparectomized rats in the presence of morphine. It is thus believed that ghrelin exhibits gastrokinetic effects without interfering with opiate activity.

Ferrets exposed to the cytotoxic anti-cancer agent cisplatin exhibited significantly reduced occurrences of retching and vomiting following intracerebroventricular administration of ghrelin (Rudd, J. A. et al., Neurosci. Lett., (2006), 392:79-83) thus confirming the ability of ghrelin to reduce emesis in a manner consistent with its role in modulating gastro-intestinal functions. It is thought that ghrelin's role in modulating gastric motility is independent of the GH-secretory activation and may be mediated by the vagal-cholinergic muscarinic pathway (U.S. Patent Application No. 20060025566).

Ghrelin has also been shown to increase gastric emptying in patients with diabetic gastroparesis (Murray, C. D. et al., Gut, (2005), 54:1693-8).

It is interesting to note that in the studies referenced above, the ghrelin or ghrelin analog was administered using intraperitoneal (ip), intravenous (iv) or intracerebroventricular (icy) injection. Other disclosures (U.S. Pat. No. 6,548,501; U.S. Patent Application No. 20020042419; U.S. Patent Application No. 20050187237; U.S. Patent Application No. 20060025566) report on the oral administration of GHSs as a means to treat impaired gastrointestinal motility.

Very few compounds are known in the art to be useful for treating impaired GI motility and more compounds affecting gastrointestinal motility, e.g. stimulation of motility, would be highly desirable. Compounds affecting gastrointestinal kinetics are useful in the treatment of interruptions in normal GI functions such as ileus and emesis.

SUMMARY OF THE INVENTION

The present invention relates to a method of stimulating gastrointestinal motility in a patient (e.g., a mammal such as a human). The method includes the step of administering a therapeutically effective amount of a peptidyl analog of ghrelin to said patient experiencing or at risk of experiencing gastrointestinal dysmotility.

In one aspect, the present invention provides a method of treating gastrointestinal dysmotility conditions by administering a therapeutically effective amount of a peptidyl analog of ghrelin or prodrug thereof suitable for attenuating such gastrointestinal conditions where the analog or prodrug comprises a compound according to Formula (I), Formula (II) or Formula (III), or a pharmaceutically acceptable salt thereof. The method of the invention is useful for promoting gastric and gastrointestinal motility in a patient (e.g., a mammal such as a human) and as such, is useful for treating conditions benefiting from improved gastric and gastrointestinal motility such as gastroesophageal reflux disease (GERD), IBS, constipation, ileus, emesis, gastroparesis, colonic pseudo-obstruction, and the like.

In another aspect, the invention provides a method of treating ileus, gastroparesis or emesis by administering a therapeutically effective amount of a peptidyl analog of ghrelin suitable for attenuating ileus, emesis, or gastroparesis. In yet another aspect, the condition treated by the method of the invention is ileus, such as post-operative ileus and the operation may be a gastrointestinal surgery. In yet another aspect of the invention, the condition treated by the method of the invention is emesis, such as emesis associated with or provoked by the administration of an anti-cancer chemotherapeutic agent. In yet another aspect, the condition treated by the method of the invention is gastroparesis, such as diabetic gastroparesis. The diabetes may be Type I or Type II diabetes.

In one aspect, the invention provides amethod of treating gastrointestinal conditions such as GERD, IBS, constipation, ileus, emesis, gastroparesis, and colonic pseudo-obstruction and the like, by administering a therapeutically effective amount of a peptidyl ghrelin analog according to the following formula (I):


(R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1

wherein:

A1 is Gly, Aib, Ala, ß-Ala, or Acc;

A2 is Ser, Aib, Act, Ala, Acc, Abu, Ava, Thr, or Val;

A3 is Ser, Ser(C(O)—R4), Asp(O—R8), Asp(NH—R9), Cys(S—R14), Dap(S(O)2—R10), Dab(S(O)2—R11), Glu(O—R6), Glu(NH—R7), Thr, Thr(C(O)—R5), or HN—CH((CH2)n—N(R12R13))—C(O);

A4 is Phe, Acc, Aic, Cha, 2-Fua, 1-Nal, 2-Nal, 2-Pal, 3-Pal, 4-Pal, hPhe, (X1,X2,X3,X4,X5)Phe, Taz, 2-Thi, 3-Thi, Trp, or Tyr;

A5 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, or Val;

A6 is Ser, Abu, Acc, Act, Aib, Ala, Gly, Thr, or Val;

A7 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A8 is Glu, Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A9 is His, Apc, Aib, Acc, 2-Fua, 2-Pal, 3-Pal, 4-Pal, Taz, 2-Thi, 3-Thi, (X1,X2,X3,X4,X5-)Phe or deleted;

A10 is Gln, Acc, Aib, Asn, Asp, Glu, or deleted;

A11 is Arg, Apc, hArg, Dab, Dap, Lys, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A12 is Val, Abu, Acc, Aib, Ala, Cha, Nva, Gly, Ile, Leu, Nle, Tle, or deleted;

A13 is Gln, Acc, Aib, Asn, Asp, Glu, or deleted;

A14 is Gln, Acc, Aib, Asn, Asp, Glu, or deleted;

A15 is Arg, hArg, Acc, Aib, Apc, Dab, Dap, Lys, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A16 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A17 is Glu, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A18 is Ser, Abu, Acc, Act, Aib, Ala, Thr, Val, or deleted;

A19 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A20 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A21 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A22 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A23 is Abu, Acc, Act, Aib, Ala, Apc, Gly, Nva, Val, or deleted;

A24 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

A25 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, Val, or deleted;

A26 is Gln, Aib, Asn, Asp, Glu, or deleted;

A27 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic, or deleted;

A28 is Acc, Aib, Apc, Arg, hArg, Dab, Dap, Lys, Orn, HN—CH((CH2)n—N(R12R13))—C(O), or deleted;

R1 is —OH, —NH2, —(C1-C30)alkoxy, or NH—X6—CH2—Z0, wherein X6 is a (C1-C12)alkyl, (C2-C12)alkenyl, and Z0 is —H, —OH, —CO2H or —C(O)—NH2;

R2 and R3 each is, independently for each occurrence, H, (C1-C20)alkyl or (C1-C20)acyl;

R4, R5, R6, R7, R8, R9, R10, R11 and R14 each is, independently for each occurrence, (C1-C40)alkyl, (C2-C40)alkenyl, substituted (C1-C40) alkyl, substituted (C2-C40) alkenyl, alkylaryl, substituted alklyaryl, aryl or substituted aryl;

R12 and R13 each is, independently for each occurrence, H, (C1-C40)alkyl, (C1-C40)acyl, (C1-C30)alkylsulfonyl, or —C(NH)—NH2, wherein when R12 is (C1-C40)acyl, (C1-C30)alkylsulfonyl, or —C(NH)—NH2, then R13 is H or (C1-C40)alkyl;

n is, independently for each occurrence, 1, 2, 3, 4 or 5;

X1, X2, X3, X4, and X1 each is, independently for each occurrence, H, F, Cl, Br, I, (C1-10)alkyl, substituted (C1-10)alkyl, aryl, substituted aryl, OH, NH2, NO2, or CN;

provided that the peptide contains at least one amino acid selected from the groups consisting of:

A2 is Aib, Acc, or Act;

A3 is Dap(S(O)2—R10), Dab(S(O)2—R11), Glu(NH-Hexyl), or Cys(S-Decyl);

A5 is Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, or Val;

A6 is Abu, Acc, Act, Aib, Ala, Gly, Thr or Val;

A7 is Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz or Tic;

A8 is Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, or HN—CH((CH2)n—N(R12R13))—C(O);

A9 is Aib, Acc, Apc, 2-Fua, 2-Pal, 3-Pal, 4-Pal, Taz, 2-Thi, 3-Thi, or (X1,X2,X3,X4,X5)Phe; and

A10 is Acc, Aib, Asn, Asp, or Glu;

    • and further provided that the peptide is not (Lys8)hGhrelin(1-8)-NH2 or (Arg8)hGhrelin(1-8)-NH2; or a pharmaceutically acceptable salt thereof.

In another aspect, the invention provides a preferred group of compounds according to formula (I), wherein:

A1 is Gly or Aib;

A2 is Ser, Aib, A5c, Act, or Ava;

A3 is Ser(C(O)—R4), Glu(O—R6), Glu(NH—R7), Dap(S(O)2—R10), or Dab(S(O)2—R11);

A4 is Phe;

A5 is Leu, Acc, Aib, Cha, or hLeu;

A6 is Ser, Abu, Act, Aib, or Thr;

A7 is Pro, Dhp, Dmt, 4-Hyp, Ktp, Pip, Tic, or Thz;

A8 is Glu or Aib;

A9 is His, Aib, Apc, 2-Fua, 2-Pal, 3-Pal, 4-Pal, Taz, or 2-Thi;

A10 is Gln or Aib;

A11 is Arg;

A12 is Aib, Val or Acc;

A13 is Gln;

A14 is Gln;

A15 is Arg or Orn;

A16 is Lys or Apc;

A17 is Glu;

A18 is Ser;

A19 is Lys;

A20 is Lys;

A21 is Pro;

A22 is Pro;

A23 is Ala;

A24 is Lys;

A25 is Leu;

A26 is Gln;

A27 is Pro; and

A28 is Arg, or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention provides a preferred group of compounds according to formula (I), wherein:

R2 and R3 each is, independently, H, Acyl, n-butyryl, isobutyryl, or n-octanoyl;

R4 is octyl;

R6 is hexyl;

R7 is hexyl;

R10 is octyl; and

R11 is octyl, or a pharmaceutically acceptable salt thereof, wherein Acc is, independently for each occurrence, A5c or A6c.

In yet another aspect, the invention provides a preferred group of compounds according to formula (I), where the compound is:

Example #75 (SEQ ID NO: 1) (Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; Example #96 (SEQ ID NO: 2) (Aib2,A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (A6c5)hGhrelin(1-28)-NH2; Example #108 (SEQ ID NO: 4) (Aib2,6)hGhrelin(1-28)-NH2; (SEQ ID NO: 5) (Aib2,A5c12)hGhrelin(1-28)-NH2; (SEQ ID NO: 6) (Aib2,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 7) (Aib2,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 7) (Aib2,Act6)hGhrelin(1-28)-NH2; Example #29 (SEQ ID NO: 8) (Aib2,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Thz7)hGhrelin(1-28)-NH2; Example #52 (SEQ ID NO: 10) (A5c2)hGhrelin(1-28)-NH2; Example #94 (SEQ ID NO: 10) (Act2)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,6)hGhrelin(1-28)-NH2; Example #114 (SEQ ID NO: 4) (Aib2,Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Thr6)hGhrelin(1-28)-NH2; Example #88 (SEQ ID NO: 4) (Aib2,Abu6)hGhrelin(1-28)-NH2; Example #36 (SEQ ID NO: 9) (Aib2,4-Hyp7)hGhrelin(1-28)-NH2; Example #54 (SEQ ID NO: 9) (Aib2,Thz7)hGhrelin(1-28)-NH2; Example #65 (SEQ ID NO: 9) (Aib2,Pip7)hGhrelin(1-28)-NH2; Example #44 (SEQ ID NO: 9) (Aib2,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ktp7)hGhrelin(1-28)-NH2; Example #49 (SEQ ID NO: 11) (Aib2,8)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,3-Pal9)hGhrelin(1-28)-NH2; Example #55 (SEQ ID NO: 8) (Aib2,4-Pal9)hGhrelin(1-28)-NH2; Example #27 (SEQ ID NO: 8) (Aib2,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,9)hGhrelin(1-28)-NH2; Example #48 (SEQ ID NO: 12) (Aib2,10)hGhrelin(1-28)-NH2; Example #53 (SEQ ID NO: 9) (Aib2,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Aib6)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (A5c5)hGhrelin(1-28)-NH2; Example #102 (SEQ ID NO: 3) (A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Act6)hGhrelin(1-28)-NH2; Example #32 (SEQ ID NO: 14) (3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (Aib5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Ktp7)hGhrelin(1-28)-NH2; Example #10 (SEQ ID NO: 16) (Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Taz9)hGhrelin(1-28)-NH2; Example #26 (SEQ ID NO: 14) (2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Aib9)hGhrelin(1-28)-NH2; (SEQ ID NO: 17) (Aib10)hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(octanesulfonyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(octanesulfonyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 20) (Aib2,6,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 21) (Aib2,Dap3(octanesulfonyl),A5c12)hGhrelin(1-28)- NH2; (SEQ ID NO: 22) (Aib2,Dap3(octanesulfonyl),A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 23) (Aib2,Dap3(octanesulfonyl),A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 20) (Aib2,Dap3(octanesulfonyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),3-Pal9)hGhrelin(1-28)- NH2; (SEQ ID NO: 25) (Aib2,Dap3(octanesulfonyl),Dmt7)hGhrelin(1-28)- NH2; (SEQ ID NO: 25) (Aib2,Dap3(octanesulfonyl),Thz7)hGhrelin(1-28)- NH2; (SEQ ID NO: 26) (A5c2,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 26) (Act2,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(octanesulfonyl),A5c5)hGhrelin(1-28)- NH2; (SEQ ID NO: 18) (Aib2,5,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(octanesulfonyl),hLeu5)hGhrelin(1-28)- NH2; (SEQ ID NO: 18) (Aib2,Dap3(octanesulfonyl),Cha5)hGhrelin(1-28)- NH2; (SEQ ID NO: 20) (Aib2,6,Dap3(octanesulfonyl))hGhrelin(1-28)- NH2; (SEQ ID NO: 20) (Aib2,Dap3(octanesulfonyl),Thr6)hGhrelin(1-28)- NH2; (SEQ ID NO: 20) (Aib2,Dap3(octanesulfonyl),Abu6)hGhrelin(1-28)- NH2; (SEQ ID NO: 25) (Aib2,Dap3(octanesulfonyl),4-Hyp7)hGhrelin(1-28)- NH2; (SEQ ID NO: 25) (Aib2,Dap3(octanesulfonyl),Pip7)hGhrelin(1-28)- NH2; (SEQ ID NO: 25) (Aib2,Dap3(octanesulfonyl),Dhp7)hGhrelin(1-28)- NH2; (SEQ ID NO: 25) (Aib2,Dap3(octanesulfonyl),Ktp7)hGhrelin(1-28)- NH2; (SEQ ID NO: 27) (Aib2,8,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),2-Pal9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),3-Pal9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),4-Pal9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),Taz9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),2-Thi9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),2-Fua9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,Dap3(octanesulfonyl),Apc9)hGhrelin(1-28)- NH2; (SEQ ID NO: 24) (Aib2,9,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 28) (Aib2,10,Dap3(octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(octanesulfonyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(octanesulfonyl),Aib6)hGhrelin(1-28)-NH2; (SEQ ID NO: 30) (Dap3(octanesulfonyl),A5c12)hGhrelin(1-28)-NH2; (SEQ ID NO: 31) (Dap3(octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 32) (Dap3(octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 29) (Dap3(octanesulfonyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(octanesulfonyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(octanesulfonyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(octanesulfonyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(octanesulfonyl),Aib5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(octanesulfonyl),hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(octanesulfonyl),Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(octanesulfonyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(octanesulfonyl),Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(octanesulfonyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(octanesulfonyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(octanesulfonyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(octanesulfonyl),Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 35) (Dap3(octanesulfonyl),Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(octanesulfonyl),Aib9)hGhrelin(1-28)-NH2; (SEQ ID NO: 36) (Dap3(octanesulfonyl),Aib10)hGhrelin(1-28)-NH2; (SEQ ID NO: 31) (Dap3(octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 31) (Dab3(octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 37) (Aib2,A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,Act6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Dmt7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Thz7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,A5c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,hLeu5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,Cha5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,Thr6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,Abu6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,4-Hyp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Pip7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Dhp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Ktp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 42) (Aib2,8,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,2-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,4-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,Taz9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,2-Thi9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,2-Fua9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,Apc9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 43) (Aib2,10,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 32) (Dap3(octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 32) (Dab3(octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 44) (Aib2,A6c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (A6c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,Act6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Dmt7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Thz7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,A5c5,12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,hLeu5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,Cha5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,Thr6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,Abu6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,4-Hyp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Pip7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Dhp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Ktp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 49) (Aib2,8,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,2-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,4-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,Taz9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,2-Thi9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,2-Fua9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,Apc9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 50) (Aib2,10,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Aib6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Act6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Dmt7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Thz7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (A5c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (Aib5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (hLeu5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (Cha5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Aib6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Thr6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Abu6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (4-Hyp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Pip7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Dhp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Ktp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 54) (Aib8,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (2-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (4-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (Taz9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (2-Thi9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (2-Fua9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (Apc9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (Aib9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 55) (Aib10,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Aib6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (A5c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Act6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Dmt7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Thz7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (Aib5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (hLeu5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (Cha5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Thr6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Abu6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (4-Hyp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Pip7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Dhp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Ktp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 59) (Aib8,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (2-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (4-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (Taz9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (2-Thi9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (2-Fua9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (Apc9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (Aib9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 60) (Aib10,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,Glu3(NH-hexyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-hexyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,6,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,Glu3(NH-hexyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,Glu3(NH-hexyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,5,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,Glu3(NH-hexyl),hLeu5)hGhrelin(1-28)-NH2; Example #81 (SEQ ID NO: 2) (Aib2,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,6,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,Glu3(NH-hexyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,Glu3(NH-hexyl),Abu6)hGhrelin(1-28)-NH2; Example #79 (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),Ktp7)hGhrelin(1-28)-NH2; Example #56 (SEQ ID NO: 27) (Aib2,8,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),2-Pal9)hGhrelin(1-28)-NH2; Example #80 (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),3-Pal9)hGhrelin(1-28)-NH2; Example #85 (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),4-Pal9)hGhrelin(1-28)-NH2; Example #43 (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),Taz9)hGhrelin(1-28)-NH2; Example #51 (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-hexyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,9,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; Example #59 (SEQ ID NO: 28) (Aib2,10,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-hexyl),Aib6)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-hexyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-hexyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-hexyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-hexyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-hexyl),Aib5)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-hexyl),hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-hexyl),Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-hexyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-hexyl),Abu6)hGhrelin(1-28)-NH2; Example #82 (SEQ ID NO: 68) (Glu3(NH-hexyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-hexyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-hexyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-hexyl),Ktp7)hGhrelin(1-28)-NH2; Example #35 (SEQ ID NO: 35) (Glu3(NH-hexyl),Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-hexyl),Aib9)hGhrelin(1-28)-NH2; (SEQ ID NO: 36) (Glu3(NH-hexyl),Aib10)hGhrelin(1-28)-NH2; (SEQ ID NO: 69) (Aib2,Glu3(NH-hexyl),A6c5,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 70) (A6c5,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 71) (Aib2,6,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 71) (Aib2,Glu3(NH-hexyl),Act6,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),3-Pal9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-hexyl),Dmt7,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-hexyl),Thz7,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 69) (Aib2,Glu3(NH-hexyl),A5c5,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 69) (Aib2,5,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 37) (Aib2,hLeu5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 69) (Aib2,Glu3(NH-hexyl),Cha5,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 71) (Aib2,6,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 71) (Aib2,Glu3(NH-hexyl),Thr6,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 71) (Aib2,Glu3(NH-hexyl),Abu6,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-hexyl),4-Hyp7,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-hexyl),Pip7,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-hexyl),Dhp7,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-hexyl),Ktp7,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 74) (Aib2,8,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin(1-28)- NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),2-Pal9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),3-Pal9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),4-Pal9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),Taz9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),2-Thi9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),2-Fua9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-hexyl),Apc9,A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 72) (Aib2,9,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin(1-28)- NH2; Example #89 (SEQ ID NO: 75) (Aib2,12,Glu3(NH-hexyl),4-Pal9,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 76) (Aib2,10,Glu3(NH-hexyl),A5c12,Orn15)hGhrelin (1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-hexyl),A6c5,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 78) (Glu3(NH-hexyl),A6c5,A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 79) (Aib2,6,Glu3(NH-hexyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 79) (Aib2,Glu3(NH-hexyl),Act6,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),3-Pal9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-hexyl),Dmt7,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-hexyl),Thz7,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-hexyl),A5c5,12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 77) (Aib2,5,Glu3(NH-hexyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-hexyl),hLeu5,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-hexyl),Cha5,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 79) (Aib2,6,Glu3(NH-hexyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 79) (Aib2,Glu3(NH-hexyl),Thr6,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 79) (Aib2,Glu3(NH-hexyl),Abu6,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-hexyl),4-Hyp7,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-hexyl),Pip7,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-hexyl),Dhp7,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-hexyl),Ktp7,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 82) (Aib2,8,Glu3(NH-hexyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),2-Pal9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),3-Pal9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),4-Pal9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),Taz9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),2-Thi9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),2-Fua9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-hexyl),Apc9,A5c12,Apc16)hGhrelin (1-28)-NH2; (SEQ ID NO: 80) (Aib2,9,Glu3(NH-hexyl),A5c12,Apc16)hGhrelin(1-28)- NH2; (SEQ ID NO: 83) (Aib2,10,Glu3(NH-hexyl),A5c12,Apc16)hGhrelin (1-28)-NH2; Example #21 (SEQ ID NO: 1) (Glu3(O-hexyl))hGhrelin(1-28)-NH2; Example #25 (SEQ ID NO: 10) (Aib2)hGhrelin(1-28)-NH2; Example #76 (SEQ ID NO: 1) (Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 84) (Aib2,Glu3(O-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 85) (Aib1,Glu3(O-hexyl))hGhrelin(1-28)-NH2; Example #8 (SEQ ID NO: 84) (Aib2,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 1) (Dap3(1-octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 84) (Aib2,Dap3(1-octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 85) (Aib1,Dap3(1-octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 86) (Ava2,Dap3(1-octanesulfonyl))hGhrelin(2-28)-NH2; (SEQ ID NO: 87) (Ac-Gly1)hGhrelin(1-5)-NH2; (SEQ ID NO: 88) (Ac-Gly1)hGhrelin(1-6)-NH2; (SEQ ID NO: 89) (Ac-Gly1)hGhrelin(1-7)-NH2; Example #63 (SEQ ID NO: 90) (Ac-Gly1,Aib2)hGhrelin(1-28)-NH2; (SEQ ID NO: 91) (Ac-Gly1,Aib2,Glu3(NH-hexyl))hGhrelin(1-5)-NH2; (SEQ ID NO: 92) (Ac-Gly1,Aib2,Glu3(NH-hexyl))hGhrelin(1-6)-NH2; (SEQ ID NO: 93) (Ac-Gly1,Aib2,Glu3(NH-hexyl))hGhrelin(1-7)-NH2; (SEQ ID NO: 94) (Ac-Gly1,Aib2,Glu3(NH-hexyl),Arg8)hGhrelin(1-8)- NH2; (SEQ ID NO: 94) (Ac-Gly1,Aib2,Glu3(NH-hexyl),Lys8)hGhrelin(1-8)- NH2; Example #95 (SEQ ID NO: 95) (n-butyryl-Gly1)hGhrelin(1-28)-NH2; Example #99 (SEQ ID NO: 95) (isobutyryl-Gly1)hGhrelin(1-28)-NH2; Example #92 (SEQ ID NO: 95) (n-octanoyl-Gly1)hGhrelin(1-28)-NH2; Example #61 (SEQ ID NO: 1) Cys3(S(CH2)9CH3)hGhrelin(1-28)-NH2; Example #42 (SEQ ID NO: 3) (Lys5)hGhrelin(1-28)-NH2 (SEQ ID NO: 10) (Aib2,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,6,Ser3)hGhrelin(1-28)-NH2 (SEQ ID NO: 8) (Aib2,Ser3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,Ser3,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Ser3,Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Ser3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 11) (Aib2,8,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 96) (Ac-Gly1,Aib2,10,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 12) (Aib2,10,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 97) (n-butyryl-Gly1,Aib2,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 97) (Ac-Gly1,Aib2,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 98) (Ac-Gly1,Aib2,Ser3,Arg8)hGhrelin(1-28)-NH2; (SEQ ID NO: 16) (Ser3,Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Ser3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Ser3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 99) (Aib2,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 99) (Aib2,6,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 100) (A5c5,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 101) (Aib2,Thr3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 103) (Aib2,Thr3,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 99) (Aib2,Thr3,Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 101) (Aib2,Thr3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 11) (Aib2,8,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 104) (Ac-Gly1,Aib2,10,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 106) (Aib2,10,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 105) (n-butyryl-Gly1,Aib2,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 105) (Ac-Gly1,Aib2,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 90) (Ac-Gly1,Aib2,Thr3,Arg8)hGhrelin(1-28)-NH2; (SEQ ID NO: 107) (Thr3,Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 101) (Aib2,Thr3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 109) (Thr3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 110) (Ac-Gly1,Glu3(NH-hexyl))hGhrelin(1-28)-NH2; or

or pharmaceutically acceptable salts thereof.

In one aspect, the invention provides a method of treating gastrointestinal conditions such as gastroesophageal reflux disease, IBS, constipation, ileus, emesis, gastroparesis, and colonic pseudo-obstruction and the like, by administering a therapeutically effective amount of a peptidyl ghrelin analog according to the following formula (II):


R1-A1-A2-A3-A4-A5-R2

wherein:

A1 is Aib, Apc or Inp;

A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1-Nal, D-2-Nal, D-Ser(Bzl), or D-Trp;

A3 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1-Nal, D-2-Nal, D-Ser(Bzl), or D-Trp;

A4 is 2-Fua, Orn, 2-Pal, 3-Pal, 4-Pal, Pff, Phe, Pim, Taz, 2-Thi, 3-Thi, Thr(Bzl);

A5 is Apc, Dab, Dap, Lys, Orn, or deleted;

R1 is hydrogen, (C1-6)alkyl, (C5-14)aryl, (C1-6)alkyl(C5-14)aryl, (C3-8)cycloakyl, or (C2-10)acyl; and

R2 is OH or NH2;

provided that when A5 is Dab, Dap, Lys, or Orn, then:

    • A2 is D-Bip, D-Bpa, D-Dip or D-Bal; or
    • A3 is D-Bip, D-Bpa, D-Dip or D-Bal; or
    • A4 is 2-Thi, 3-Thi, Taz, 2-Fua, 2-Pal, 3-Pal, 4-Pal, Orn, Thr(Bzl), or Pff;
      when A5 is deleted, then:
    • A3 is D-Bip, D-Bpa, or D-Dip; or
    • A4 is 2-Fua, Pff, Taz, or Thr(Bzl); or
    • A1 is Apc when
      • A2 is D-Bip, D-Bpa, D-Dip or D-Bal; or
      • A3 is D-Bip, D-Bpa, D-Dip or D-Bal; or
      • A4 is 2-Thi, 3-Thi, Orn, 2-Pal, 3-Pal or 4-Pal;
        or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention provides a preferred compound of formula (II), wherein:

A1 is Aib, Apc or H-Inp;

A2 is D-Bal, D-Bip, D-Bpa, D-Dip, D-1-Nal, D-2-Nal, D-Ser(Bzl), or D-Trp;

A3 is D-Bal, D-Bpa, D-Dip, D-1-Nal, D-2-Nal, or D-Trp;

A4 is Orn, 3-Pal, 4-Pal, Pff, Phe, Pim, Taz, 2-Thi, or Thr(Bzl); and

A5 is Apc, Lys, or deleted;

or a pharmaceutically acceptable salt thereof.

In yet another aspect of the immediately foregoing group of compounds, the invention provides a preferred compound of formula (II), wherein:

A1 is Apc or H-Inp;

A2 is D-Bal, D-Bip, D-1-Nal, or D-2-Nal;

A3 is D-Bal, D-1-Nal, D-2-Nal, or D-Trp;

A4 is 3-Pal, 4-Pal, Pff, Phe, Pim, Taz, 2-Thi, or Thr(Bzl); and

or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention provides a preferred group of compounds according to formula (I), where the compound is:

Example 2 (SEQ ID NO: 111) Inp-D-2-Nal-D-Trp-Phe-Lys-NH2 Example #50 (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Pal-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-4-Pal-Lys-NH2; Example #116 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Orn-Lys-NH2; Example #66 (SEQ ID NO: 111) H-Inp-D-Bip-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-Lys-NH2; Example #100 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Pff-Lys-NH2; Example #15 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-2-Thi-Lys-NH2; Example #37 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Taz-Lys-NH2; Example #105 (SEQ ID NO: 111) H-Inp-D-Dip-D-Trp-Phe-Lys-NH2; Example #109 (SEQ ID NO: 111) H-Inp-D-Bpa-D-Trp-Phe-Lys-NH2; Example #118 (SEQ ID NO: 114) H-Inp-D-2-Nal-D-Bpa-Phe-Lys-NH2; Example #93 (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-3-Pal-NH2; Example #112 (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-4-Pal-NH2; Example #97 (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-3-Pal-NH2; Example #98 (SEQ ID NO: 117) H-Inp-D-Bip-D-Trp-Phe-NH2; Example #87 (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-NH2; Example #103 (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; Example #84 (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-2-Thi-NH2; Example #90 (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; Example #111 (SEQ ID NO: 117) H-Inp-D-Dip-D-Trp-Phe-NH2; Example #110 (SEQ ID NO: 118) H-Inp-D-2-Nal-D-Dip-Phe-NH2; Example #78 (SEQ ID NO: 119) H-Inp-D-Bal-D-Trp-Phe-NH2; Example #101 (SEQ ID NO: 118) H-Inp-D-2-Nal-D-Bal-Phe-NH2; Example #71 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Pal-Lys-NH2; Example #115 (SEQ ID NO: 120) H-Inp-D-Trp-D-2-Nal(Ψ)-Pim; Example #12 (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Thi-Lys-NH2; Example #5 (SEQ ID NO: 111) H-Inp-D-Bal-D-Trp-Phe-Lys-NH2; Example #3 (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Thi-Lys-NH2; Example #28 (SEQ ID NO: 122) H-Inp-D-2-Nal-D-Trp-Phe-Apc-NH2; Example #6 (SEQ ID NO: 122) H-Inp-D-1-Nal-D-Trp-Phe-Apc-NH2; Example #19 (SEQ ID NO: 122) H-Inp-D-Bal-D-Trp-Phe-Apc-NH2; Example #11 (SEQ ID NO: 123) H-Apc-D-2-Nal-D-Trp-Phe-Lys-NH2; Example #1 (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Thi-Lys-NH2; Example #39 (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-2-Thi-NH2; Example #31 (SEQ ID NO: 125) H-Apc-D-1-Nal-D-Trp-Phe-NH2; Example #113 (SEQ ID NO: 126) H-Inp-D-2-Nal-D-Trp(Ψ)-Pim; Example #107 (SEQ ID NO: 126) H-Inp-D-1-Nal-D-Trp(Ψ)-Pim; Example #106 (SEQ ID NO: 126) H-Inp-D-Bal-D-Trp(Ψ)-Pim; Example #119 (SEQ ID NO: 127) H-Aib-D-Ser(Bzl)-D-Trp(Ψ)-Pim; Example #57 (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Taz-Lys-NH2; Example #23 (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Taz-Lys-NH2; Example #14 (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Taz-Lys-NH2; Example #20 (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Taz-Lys-NH2; Example #7 (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Thi-Lys-NH2; Example #4 (SEQ ID NO: 123) H-Apc-D-Bal-D-Trp-Phe-Lys-NH2; Example #18 (SEQ ID NO: 129) H-Apc-D-1-Nal-D-Trp-Phe-Apc-NH2; Example #33 (SEQ ID NO: 130) H-Apc-D-Bal-D-Trp-Phe-Apc-NH2; Example #74 (SEQ ID NO: 129) H-Apc-D-1-Nal-D-1-Nal-Phe-Apc-NH2; Example #73 (SEQ ID NO: 129) H-Apc-D-1-Nal-D-2-Nal-Phe-Apc-NH2; Example #64 (SEQ ID NO: 131) H-Apc-D-1-Nal-D-1-Nal-Phe-Lys-NH2; Example #83 (SEQ ID NO: 130) H-Apc-D-Bal-D-1-Nal-Phe-Apc-NH2; Example #69 (SEQ ID NO: 130) H-Apc-D-Bal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-1-Nal-Phe-Lys-NH2; Example #30 (SEQ ID NO: 132) H-Apc-D-Bal-D-2-Nal-Phe-Lys-NH2; Example #34 (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Thi-NH2; Example #41 (SEQ ID NO: 125) H-Apc-D-Bal-D-Trp-Phe-NH2; Example #67 (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Taz-NH2; Example #47 (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-2-Thi-NH2; Example #72 (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-Taz-NH2; Example #45 (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Thi-NH2; Example #77 (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Taz-NH2; Example #60 (SEQ ID NO: 135) H-Inp-D-1-Nal-D-Trp-Taz-Apc-NH2; Example #38 (SEQ ID NO: 135) H-Inp-D-Bal-D-Trp-Taz-Apc-NH2; Example #46 (SEQ ID NO: 136) H-Apc-D-1-Nal-D-Trp-Taz-Apc-NH2; Example #58 (SEQ ID NO: 136) H-Apc-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Pal-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Pal-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 136) H-Apc-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-2-Fua-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Fua-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Pal-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-2-Thi-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Thi-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-3-Pal-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-3-Thi-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-3-Thi-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-4-Pal-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-Pff-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Pff-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-Bal-Phe-Apc-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Phe-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-Taz-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Taz-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-2-Fua-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-2-Pal-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-3-Pal-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-3-Thi-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-4-Pal-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-Pff-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 146) H-Inp-D-1-Nal-D-Bal-2-Fua-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 146) H-Inp-D-1-Nal-D-Bal-Pff-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 146) H-Inp-D-1-Nal-D-Bal-Taz-NH2; (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 135) H-Inp-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-2-Fua-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-Pff-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-Taz-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-2-Fua-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-Pff-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-Taz-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-2-Fua-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-Pff-NH2; or (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-Taz-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-2-Fua-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-Pff-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-Taz-Lys-NH2; or (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-Taz-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Pal-Lys-NH2; Example #91 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-4-Pal-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Orn-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bip-D-Trp-Phe-Lys-NH2; Example #70 (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Dip-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bpa-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 114) H-Inp-D-2-Nal-D-Bpa-Phe-Lys-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 118) H-Inp-D-2-Nal-D-Dip-Phe-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Pal-Lys-NH2; (SEQ ID NO: 120) H-Inp-D-Trp-D-2-Nal(Ψ)-Pim; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 122) H-Inp-D-2-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 122) H-Inp-D-1-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 122) H-Inp-D-Bal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 123) H-Apc-D-2-Nal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 126) H-Inp-D-2-Nal-D-Trp(Ψ)-Pim; (SEQ ID NO: 126) H-Inp-D-1-Nal-D-Trp(Ψ)-Pim; (SEQ ID NO: 126) H-Inp-D-Bal-D-Trp(Ψ)-Pim; (SEQ ID NO: 127) H-Aib-D-Ser(Bzl)-D-Trp(Ψ)-Pim; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 123) H-Apc-D-Bal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-1-Nal-Phe-Apc-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 131) H-Apc-D-1-Nal-D-1-Nal-Phe-Lys-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-1-Nal-Phe-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-1-Nal-Phe-Lys-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-2-Nal-Phe-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-Phe-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-2-Thi-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-Taz-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 135) H-Inp-D-1-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 135) H-Inp-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-1-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 135) H-Inp-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 160) H-Inp-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 160) H-Inp-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 160) H-Inp-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-Bal-Phe-Apc-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-2-Thi-Apc-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-3-Thi-Apc-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-Taz-Apc-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-2-Fua-Apc-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-Pff-Apc-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-Taz-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-2-Fua-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-Pff-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-3-Thi-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-2-Fua-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-Pff-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-4-Pal-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-3-Pal-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-2-Pal-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-Taz-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-2-Fua-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-Pff-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Phe-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Thi-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-3-Thi-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Taz-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Fua-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Pff-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-4-Pal-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-3-Pal-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Pal-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 161) H-Inp-D-1-Nal-D-Bal-Taz-NH2; (SEQ ID NO: 161) H-Inp-D-1-Nal-D-Bal-2-Fua-NH2; (SEQ ID NO: 161) H-Inp-D-1-Nal-D-Bal-Pff-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Pal-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Pal-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-Taz-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-2-Fua-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-Pff-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-Taz-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-2-Fua-NH2; or (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-Pff-NH2; Example #24 (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-2-Thi-Apc-NH2; Example #9 (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-2-Thi-Apc-NH2; Example #17 (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-2-Thi-Apc-NH2; Example #22 (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-2-Thi-Apc-NH2; or Example #13 (SEQ ID NO: 131) H-Apc-D-1-Nal-D-Trp-Phe-Lys-NH2

or a pharmaceutically acceptable salts thereof.

In yet another aspect, the invention provides amethod of treating gastrointestinal conditions such as gastroesophageal reflux disease, IBS, constipation, ileus, emesis, gastroparesis, and colonic pseudo-obstruction and the like, by administering a therapeutically effective amount of a peptidyl ghrelin analog according to the following formula (III):


(R2R3)-A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-A17-A18-A19-A20-A21-A22-A23-A24-A25-A26-A27-A28-R1

wherein:

A1 is Gly, Aib, Ala, ß-Ala, Acc or Gly(myristyl);

A2 is Ser, Aib, Ala, Acc, Abu, Act, Ava, Thr or Val;

A3 is Ser, Ser(C(O)—R4), Asp(O—R8), Asp(NH—R9), Cys(S—R14), Dap(S(O)2—R10), Dab(S(O)2—R11), Glu(O—R6), Glu(NH—R7), Thr(C(O)—R5) or HN—CH((CH2)n—N(R12R13)—C(O);

A4 is Phe, Acc, Aic, Cha, 2-Fua, 1-Nal, 2-Nal, 2-Pal, 3-Pal, 4-Pal, hPhe, (X1,X2,X3,X4,X5)Phe, Taz, 2-Thi, 3-Thi, Trp or Tyr;

A5 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle or Val;

A6 is Ser, Abu, Acc, Act, Aib, Ala, Gly, Thr or Val;

A7 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz or Tic;

A8 is Glu, Acc, Aib, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn or HN—CH((CH2)n—N(R12R13)—C(O);

A9 is His, Apc, Aib, Acc, 2-Fua, 2-Pal, 3-Pal, 4-Pal, Taz, 2-Thi, 3-Thi or (X1,X2,X3,X4,X5-)Phe;

A10 is Gln, Acc, Aib, Asn, Asp or Glu;

A11 is Arg, Apc, hArg, Dab, Dap, Lys, Orn or HN—CH((CH2)n—N(R12R13))—C(O);

A12 is Val, Abu, Acc, Aib, Ala, Cha, Nva, Gly, Ile, Leu, Nle, Tle or Cha;

A13 is Gln, Acc, Aib, Asn, Asp or Glu;

A14 is Gln, Acc, Aib, Asn, Asp or Glu;

A15 is Arg, hArg, Acc, Aib, Apc, Dab, Dap, Lys, Orn, Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R15), hCys(S—R16) or hCys(R17);

A16 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R9), hCys(S—R′6), hCys(R′7) or deleted;

A17 is Glu, Arg, Asn, Asp, Dab, Dap, Gln, Lys, Orn, Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R15), hCys(S—R16), hCys(R17), Lys(biotinyl) or deleted;

A18 is Ser, Abu, Acc, Act, Aib, Ala, Thr, Val, Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R15), hCys(S—R16), hCys(R17) or deleted;

A19 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R15), hCys(S—R16), hCys(R17) or deleted;

A20 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R15), hCys(S—R′6), hCys(R17) or deleted;

A21 is Pro, Dhp, Dmt, Inc, 3-Hyp, 4-Hyp, Ktp, Oic, Pip, Thz, Tic or deleted;

A22 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic or deleted;

A23 is Abu, Acc, Act, Aib, Ala, Apc, Gly, Nva, Val or deleted;

A24 is Lys, Acc, Aib, Apc, Arg, hArg, Dab, Dap, Orn, HN—CH((CH2)n—N(R12R13))—C(O) or deleted;

A25 is Leu, Abu, Acc, Aib, Ala, Cha, Ile, hLeu, Nle, Nva, Phe, Tle, Val or deleted;

A26 is Gln, Aib, Asn, Asp, Glu or deleted;

A27 is Pro, Dhp, Dmt, 3-Hyp, 4-Hyp, Inc, Ktp, Oic, Pip, Thz, Tic or deleted;

A28 is Acc, Aib, Apc, Arg, hArg, Dab, Dap, Lys, Orn, HN—CH((CH2)n—N(R12R13))—C(O) or deleted;

R1 is —OH, —NH2, —(C1-C30)alkoxy or NH—X6—CH2—Z0, wherein X6 is a (C1-C12)alkyl, (C2-C12)alkenyl and Z0 is —H, —OH, —CO2H or —C(O)—NH2;

R2 and R3 is, independently for each occurrence thereof, selected from the group consisting of H, (C1-C30)alkyl, (C1-C30)heteroalkyl, (C1-C30)acyl, (C2-C30)alkenyl, (C2-C30)alkynyl, aryl(C1-C30)alkyl, aryl(C1-C30)acyl, substituted (C1-C30)alkyl, substituted (C1-C30)heteroalkyl, substituted (C2-C30)acyl, substituted (C2-C30)alkenyl, substituted aryl(C1-C30)alkyl and substituted aryl(C1-C30)acyl;

R4, R5, R6, R7, R8, R9, R10, R11, R14, R15, R16 and R17 is, independently for each occurrence thereof, selected from the group consisting of (C1-C40)alkyl, (C2-C40)alkenyl, substituted (C1-C40) alkyl, substituted (C2-C40) alkenyl, alkylaryl, substituted alklyaryl, aryl and substituted aryl;

R12 and R13 is, independently for each occurrence thereof, selected from the group consisting of H, (C1-C40)alkyl, (C1-C40)acyl, (C1-C30)alkylsulfonyl, biotinyl and —C(NH)—NH2,

X1, X2, X3, X4, and X5 is, independently for each occurrence thereof, selected from the group consisting of H, F, Cl, Br, I, (C1-10)alkyl, substituted (C1-10)alkyl, aryl, substituted aryl, OH, NH2, NO2 and CN; and

n is, independently for each occurrence thereof, 1, 2, 3, 4 or 5;

provided that:

(I). when R2 is (C1-C30)acyl, aryl(C1-C30)acyl, substituted (C2-C30)acyl, or substituted aryl(C1-C30)acyl, R3 is H, (C1-C30)alkyl, (C1-C30)heteroalkyl, (C2-C30)alkenyl, aryl(C1-C30)alkyl, substituted (C1-C30)alkyl, substituted (C1-C30)heteroalkyl, substituted (C2-C30)alkenyl or substituted aryl(C1-C30)alkyl;

(II). when R12 is (C1-C40)acyl, (C1-C30)alkylsulfonyl, biotinyl or —C(NH)—NH2, then R13 is H or (C1-C40)alkyl;

(III). at least one of A15, A16, A17, A18, A19 or A20 must be selected from the group consisting of Ser(C(O)—R4), Thr(C(O)—R5), Glu(O—R6), Glu(NH—R7), Asp(O—R8), Asp(NH—R9), Dap(S(O)2—R10), Dab(S(O)2—R11), HN—CH((CH2)n—N(R12R13))—C(O), Cys(S—R14), Cys(R15), hCys(S—R16) and hCys(R17); and

(IV). when any of the group consisting of A15, A16, A17, A19 and A20 is HN—CH((CH2)n—N(R12R13))—C(O), then R12 must be biotinyl;

or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention provides a preferred group of compounds according to formula (III), where in:

each of R2 and R3 is, independently for each occurrence thereof, selected from the group consisting of H, acyl, n-butyryl, isobutyryl and n-octanoyl;

R4 is heptyl;

R6 is hexyl;

R7 is hexyl;

R10 is octyl;

R11 is heptyl; and

provided that when Acc is substituted for one of the naturally-occurring residues, it is, independently for each occurrence, A3c, A4c, A5c or A6c;

or pharmaceutically acceptable salts thereof.

In yet another aspect, the invention provides a preferred group of compounds according to formula (III), where the compound is:

(SEQ ID NO: 162) (Ser(n-octanoyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 163) (Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 164) (Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 165) (Glu(NH-hexyl)3,Ser(n-octanoyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 166) (Aib2,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 167) (Aib2,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 168) (Aib2,8,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 169) (Aib2,8,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 170) (Aib2,10,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 171) (Aib2,10,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 172) (Ser(n-octanoyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 173) (Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 174) (Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 175) (Glu(NH-hexyl)3,Ser(n-octanoyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 176) (Aib2,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 177) (Aib2,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 178) (Aib2,8,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 179) (Aib2,8,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 180) (Aib2,10,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 181) (Aib2,10,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 182) (Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 183) (Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 184) (Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 185) (Glu(NH-hexyl)3,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 186) (Dap(octanesulfonyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 187) (Dap(octanesulfonyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 188) (Dap(octanesulfonyl)3,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 189) (Dap(octanesulfonyl)3,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 190) (Glu(NH-hexyl)3,Dap(octanesulfonyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 191) (Cys(S—(CH2)9CH3)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 192) (Cys(S—(CH2)9CH3)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 193) (Glu(NH-hexyl)3,Cys(S—(CH2)9CH3)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 194) (Cys(S—(CH2)9CH3)3,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 195) (Cys(S—(CH2)9CH3)3,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 196) (Aib2,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 197) (Aib2,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 198) (Aib2,Thz7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 198) (Aib2,4-Hyp7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 198) (Aib2,Dhp7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 198) (Aib2,Pip7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 198) (Aib2,Tic7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 199) (Aib2,Glu(NH-hexyl)3,17,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 200) (Aib2,Glu(NH-hexyl)3,17,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 200) (Aib2,Glu(NH-hexyl)3,17,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 200) (Aib2,Glu(NH-hexyl)3,17,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 200) (Aib2,Glu(NH-hexyl)3,17,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 201) (Aib2,8,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; Example #16 (SEQ ID NO: 202) (Aib2,8,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 203) (Aib2,3-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 203) (Aib2,4-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 203) (Aib2,Taz9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 203) (Aib2,2-Thi9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 204) (Aib2,Glu(NH-hexyl)3,17,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 204) (Aib2,Glu(NH-hexyl)3,17,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 204) (Aib2,Glu(NH-hexyl)3,17,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 204) (Aib2,Glu(NH-hexyl)3,17,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 205) (Aib2,10,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 206) (Aib2,10,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 207) (Aib8,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 208) (Taz9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 208) (3-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 208) (4-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 208) (2-Thi9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 209) (Glu(NH-hexyl)3,17,Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 210) (Glu(NH-hexyl)3,17,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 210) (Glu(NH-hexyl)3,17,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 210) (Glu(NH-hexyl)3,17,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 210) (Glu(NH-hexyl)3,17,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 211) (Aib1,2,10,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 212) (Aib1,2,10,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 196) (A5c2,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 197) (A5c2,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 184) (Glu(1-heptanol)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 213) (Asp(1-heptanol)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 184) (Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 213) (Asp(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 197) (Aib2,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 214) (Lys(biotinyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 215) (Ser(n-octanoyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 216) (Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 217) (Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 218) (Glu(NH-hexyl)3,Ser(n-octanoyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 219) (Aib2,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 220) (Aib2,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 221) (Aib2,8,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 222) (Aib2,8,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 223) (Aib2,10,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 224) (Aib2,10,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 225) (Ser(n-octanoyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 226) (Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 227) (Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 228) (Glu(NH-hexyl)3,Ser(n-octanoyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 229) (Aib2,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 230) (Aib2,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 231) (Aib2,8,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 232) (Aib2,8,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 233) (Aib2,10,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 234) (Aib2,10,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 235) (Ser(n-octanoyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 236) (Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 237) (Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 238) (Glu(NH-hexyl)3,Ser(n-octanoyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 239) (Aib2,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 240) (Aib2,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 241) (Aib2,8,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 242) (Aib2,8,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 243) (Aib2,10,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 244) (Aib2,10,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 245) (Ac-Gly1,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 246) (Ac-Gly1,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 247) (Ac-Gly1,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 248) (Ac-Gly1,Glu(NH-hexyl)3,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 249) (Ac-Gly1,Dap(octanesulfonyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 250) (Ac-Gly1,Dap(octanesulfonyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 251) (Ac-Gly1,Dap(octanesulfonyl)3,Glu(NH-Hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 252) (Ac-Gly1,Dap(octanesulfonyl)3,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 253) (Ac-Gly1,Glu(NH-hexyl)3,Dap(octanesulfonyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 254) (Ac-Gly1,Cys(S—(CH2)9CH3)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 255) (Ac-Gly1,Cys(S—(CH2)9CH3)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 256) (Ac-Gly1,Glu(NH-hexyl)3,Cys(S—(CH2)9CH3)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 257) (Ac-Gly1,Cys(S—(CH2)9CH3)3,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 258) (Ac-Gly1,Cys(S—(CH2)9CH3)3,Ser(n-octanoyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 259) (Ac-Gly1,Aib2,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 260) (Ac-Gly1,Aib2,Thz7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 260) (Ac-Gly1,Aib2,4-Hyp7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 260) (Ac-Gly1,Aib2,Dhp7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 260) (Ac-Gly1,Aib2,Pip7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 260) (Ac-Gly1,Aib2,Tic7,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 261) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 261) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 261) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 261) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 261) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 262) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 263) (Ac-Gly1,Aib2,3-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 263) (Ac-Gly1,Aib2,4-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 263) (Ac-Gly1,Aib2,Taz9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 263) (Ac-Gly1,Aib2,2-Thi9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 264) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 264) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 264) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 264) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,17,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 265) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 266) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 267) (Ac-Gly1,Aib8,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 268) (Ac-Gly1,Taz9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 268) (Ac-Gly1,3-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 268) (Ac-Gly1,4-Pal9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 268) (Ac-Gly1,2-Thi9,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 269) (Ac-Gly1,Glu(NH-hexyl)3,17,Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 270) (Ac-Gly1,Glu(NH-hexyl)3,17,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 270) (Ac-Gly1,Glu(NH-hexyl)3,17,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 270) (Ac-Gly1,Glu(NH-hexyl)3,17,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 270) (Ac-Gly1,Glu(NH-hexyl)3,17,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 271) (Ac-Aib1,Aib2,10,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 272) (Ac-Aib1,Aib2,10,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 259) (Ac-Gly1,A5c2,Glu(NH-hexyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 273) (Ac-Gly1,A5c2,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 247) (Ac-Gly1,Glu(1-heptanol)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 274) (Ac-Gly1,Asp(1-heptanol)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 247) (Ac-Gly1,Glu(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 274) (Ac-Gly1,Asp(NH-hexyl)3,17)hGhrelin(1-28)-NH2; (SEQ ID NO: 275) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,Lys(biotinyl)17)hGhrelin(1-28)-NH2; (SEQ ID NO: 276) (Ac-Gly1,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 277) (Ac-Gly1,Ser(n-octanoyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 278) (Ac-Gly1,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 279) (Ac-Gly1,Glu(NH-hexyl)3,Ser(n-octanoyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 280) (Ac-Gly1,Aib2,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 281) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 282) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 283) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 284) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)15)hGhrelin(1-28)-NH2; (SEQ ID NO: 285) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,15)hGhrelin(1-28)-NH2; (SEQ ID NO: 286) (Ac-Gly1,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 287) (Ac-Gly1,Ser(n-octanoyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 288) (Ac-Gly1,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 289) (Ac-Gly1,Glu(NH-hexyl)3,Ser(n-octanoyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 290) (Ac-Gly1,Aib2,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 291) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 292) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 293) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 294) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)16)hGhrelin(1-28)-NH2; (SEQ ID NO: 295) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,16)hGhrelin(1-28)-NH2; (SEQ ID NO: 296) (Ac-Gly1,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 297) (Ac-Gly1,Ser(n-octanoyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 298) (Ac-Gly1,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 299) (Ac-Gly1,Glu(NH-hexyl)3,Ser(n-octanoyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 300) (Ac-Gly1,Aib2,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 301) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 302) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 303) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 304) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)18)hGhrelin(1-28)-NH2; (SEQ ID NO: 305) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,18)hGhrelin(1-28)-NH2; (SEQ ID NO: 306) (Ac-Gly1,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 307) (Ac-Gly1,Ser(n-octanoyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 308) (Ac-Gly1,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 309) (Ac-Gly1,Glu(NH-hexyl)3,Ser(n-octanoyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 310) (Ac-Gly1,Aib2,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 311) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 312) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 313) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 314) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)19)hGhrelin(1-28)-NH2; (SEQ ID NO: 315) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,19)hGhrelin(1-28)-NH2; (SEQ ID NO: 316) (Ac-Gly1,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 317) (Ac-Gly1,Ser(n-octanoyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 318) (Ac-Gly1,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 319) (Ac-Gly1,Glu(NH-hexyl)3,Ser(n-octanoyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 320) (Ac-Gly1,Aib2,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 321) (Ac-Gly1,Aib2,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 322) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 323) (Ac-Gly1,Aib2,8,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2; (SEQ ID NO: 324) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)20)hGhrelin(1-28)-NH2; (SEQ ID NO: 325) (Ac-Gly1,Aib2,10,Glu(NH-hexyl)3,20)hGhrelin(1-28)-NH2;

or pharmaceutically acceptable salts thereof.

In yet another aspect, the invention provides amethod of treating gastrointestinal conditions such as gastroesophageal reflux disease, IBS, constipation, ileus, emesis, gastroparesis, and colonic pseudo-obstruction and the like, by administering a therapeutically effective amount of the following peptidyl ghrelin analogs which do not correspond to any one of formula (I), (II) or (III):

Example #86 (SEQ ID NO: 326) (Asp3(NH-heptyl))hGhrelin(1-28)-NH2 Example #104 (SEQ ID NO: 327) (des-Ser2)hGhrelin(1-28)-NH2; or Example #117 (SEQ ID NO: 328) (des-Gly1,des-Ser2)hGhrelin(1-28)-NH2; Example #6 (SEQ ID NO: 329) (Aib1)hGhrelin(1-28)-NH2; Example #40 (SEQ ID NO: 326) (Asp3(O-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 329) (Aib1,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (A5c5,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 330) (Aib2,4,Ser3,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 95) (n-octanoyl-Gly1,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 95) (isobutyryl-Gly1,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 95) (n-butyryl-Gly1,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 331) (Aib1,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 330) (Aib2,4,Thr3,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 332) (n-octanoyl-Gly1,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 332) (isobutyryl-Gly1,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 332) (n-butyryl-Gly1,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 95) (Ac-Gly1)hGhrelin(1-28)-NH2; (SEQ ID NO: 95) (Ac-Gly1,Ser3)hGhrelin(1-28)-NH2, (SEQ ID NO: 333) Aib2,Lys(Myristyl)17)hGhrelin-(1-28)-NH2; or (SEQ ID NO: 334) Gly(myristyl)1-(Aib2,Lys(Myristyl)17]hGhrelin- (1-28)-NH2;

or pharmaceutically acceptable salts thereof.

The peptidyl analog of ghrelin or prodrug thereof may be administered parenterally, e.g., administered intravenously, subcutaneously, or by implantation of a sustained release formulation. The peptidyl analog of ghrelin may also be administered intracerebroventricular (icy) injection. In another embodiment, the peptidyl analog of ghrelin is administered via oral administration. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above, as well as each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

Accordingly, in one aspect, the invention features a method of treating ileus in a patient, which includes identifying a patient suffering from or at risk for ileus and administering to the patient a pharmaceutical composition comprising an effective amount of a peptidyl analog of ghrelin. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention features a method of treating post-surgical ileus in a patient. The method includes identifying a patient suffering from post-surgical ileus and administering to the patient a pharmaceutical composition comprising an effective amount of a peptidyl analog of ghrelin effective to treat ileus in the patient. The ileus can be ileus of any part of the gastrointestinal tract, e.g., the stomach, small intestine, and/or large intestine (e.g., the colon). The pharmaceutical composition can be administered to the patient via any route described herein, e.g., via inhalation (of gaseous compositions); orally; and/or by direct administration to the abdominal cavity of the patient. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

The invention also features a method of treating ileus in a patient suffering from or at risk for ileus not caused by abdominal surgery, e.g., ileus caused by any factor described herein other than abdominal surgery. The method includes identifying a patient suffering from or at risk for ileus not caused by abdominal surgery and administering to the patient a pharmaceutical composition comprising an effective amount of a peptidyl analog of ghrelin effective to treat ileus in the patient. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention provides a method of performing surgery on a patient. The method includes identifying a patient in need of surgery, and before, during, and/or after the surgery, administering to the patient an effective amount of a peptidyl analog of ghrelin sufficient to treat ileus in the patient. The surgery can be any surgery that causes and/or puts the patient at risk for ileus. For example, the surgery can involve manipulation (e.g., touching (directly or indirectly)) of the gastrointestinal tract, e.g., the stomach and/or intestines, e.g., small or large intestine (e.g., the colon), and can be a surgery involving laparotomy or not involving laparotomy (e.g., surgeries involving laparoscopy). In certain embodiments, the surgery can be transplant surgery or non-transplant surgery, e.g., surgery involving any organ(s) or tissue(s) in the abdomen, e.g., surgery of the urogenital system (e.g., kidneys, ureter, and/or bladder; and reproductive organs (e.g., uterus, ovaries, and/or fallopian tubes)); the digestive system (e.g., the stomach, small intestine, large intestine (e.g., the colon), appendix, gallbladder, liver, spleen, and/or pancreas); the lymphatic system; the respiratory system (e.g., the lungs); the diaphragm; surgery to treat cancer of any organ or tissue within the abdomen; endometrial surgery; and orthopedic surgeries, e.g., hip surgery. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula III as well as each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In still another aspect, the invention provides a method of treating ileus in a patient, which includes identifying a patient suffering from or at risk for ileus and administering to the patient an effective amount of a peptidyl analog of ghrelin for treatment or prevention of ileus. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention features a method of treating emesis in a patient, which includes identifying a patient suffering from or at risk for emesis and administering to the patient a pharmaceutical composition comprising an effective amount of a peptidyl analog of ghrelin. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention features a method of treating emesis provoked by or associated with the administration of anti-cancer chemotherapeutic agents in a patient, which includes identifying a patient suffering from or at risk for emesis provoked by or associated with the administration of anti-cancer chemotherapeutic agents and administering to the patient a pharmaceutical composition comprising a therapeutically effective amount of a peptidyl analog of ghrelin. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In another aspect, the invention features a method of treating gastroparesis in a patient, which includes identifying a patient suffering from or at risk for gastroparesis and administering to the patient a pharmaceutical composition comprising an effective amount of a peptidyl analog of ghrelin. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In yet another aspect, the invention features a method of treating gastroparesis resulting from diabetes in a patient, which includes identifying a patient suffering from or at risk for diabetic gastroparesis and administering to the patient a pharmaceutical composition comprising an effective amount of a peptidyl analog of ghrelin. The diabetes may be Type I or Type II diabetes. Particularly preferred peptidyl analogs of ghrelin are those compounds of formula (I) or formula (II) or formula (III), as well as the non-conforming compounds indicated above and each of the compounds that are specifically enumerated herein and below in the Examples section of the present disclosure, or a pharmaceutically acceptable salt thereof.

In a further aspect, the present invention provides the use of a therapeutically effective amount of a peptidyl ghrelin analog compound according formula (I) or formula (II) or formula (III) as defined hereinabove, as well as the non-conforming compounds indicated above and each of the compounds specifically enumerated herein and below, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament useful to treat gastrointestinal conditions such as gastroesophageal reflux disease, IBS, constipation, ileus, emesis, gastroparesis, and colonic pseudo-obstruction and the like. In yet another embodiment, the gastrointestinal conditions treated are ileus, emesis and gastroparesis. In yet another embodiment, the ilieus is post-operative ileus, the emesis is associated with the administration of anti-cancer chemotherapeutic agents and the gastroparesis is associated with diabetes.

In yet another aspect, the present invention provides a method of eliciting an agonist or an antagonist effect from a ghrelin receptor in a subject in need thereof which comprises administering to said subject an effective amount of a compound of formula (I) or formula (II) or formula (III) as defined hereinabove, as well as the non-conforming compounds indicated above and each of the compounds specifically enumerated herein and below or pharmaceutically acceptable salts thereof.

BRIEF DESCRIPTION OF THE DRAWINGS

FIG. 1: shows the schematic presentation of the methods used to study gastric emptying in a rat model;

FIG. 2: shows the effect on gastric emptying in normal rats for native ghrelin and Example 19;

FIG. 3: shows the percent decrease in gastric emptying due to post-operative ileus alone and in combination with morphine; and

FIG. 4: shows the effect on gastric emptying in post-operative ileus rat model for native ghrelin and Example 19;

FIG. 5: shows the effect on gastric emptying in post-operative ileus and morphine rat model for native ghrelin and Example 19.

DETAILED DESCRIPTION

Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. Suitable methods and materials are described below, although methods and materials similar or equivalent to those described herein can be used in the practice or testing of the present invention. All publications, patent applications, patents, and other references mentioned herein are incorporated by reference in their entirety. In case of conflict, the present specification, including definitions, will control. The materials, methods, and examples are illustrative only and not intended to be limiting.

Other features and advantages of the invention will be apparent from the following description of the preferred embodiments and from the claims. Certain amino acids present in compounds of the invention can be and are represented herein as follows:

NOMENCLATURE AND ABBREVIATIONS

Symbol Meaning Abu α-aminobutyric acid Acc 1-amino-1-cyclo(C3-C9)alkyl carboxylic acid A3c 1-amino-1-cyclopropanecarboxylic acid A4c 1-amino-1-cyclobutanecarboxylic acid A5c 1-amino-1-cyclopentanecarboxylic acid A6c 1-amino-1-cyclohexanecarboxylic acid Act 4-amino-4-carboxytetrahydropyran having the structure: Aib α-aminoisobutyric acid Aic 2-aminoindan-2-carboxylic acid Ala or A alanine β-Ala beta-alanine Apc denotes the structure: Arg or R arginine hArg homoarginine Asn or N asparagine Asp or D aspartic acid Ava 5-amino-n-valeric acid D-Bal D-3-benzothienylalanine having the structure: D-Bip D-4,4′-biphenylalanine having the structure: D-Bpa D-4-benzoylphenylalanine having the structure: Cha β-cyclohexylalanine Cys or C cysteine hCys L-homocysteine Dab 2,4-diaminobutyric acid Dap 2,3-diaminopropionic acid Dap(octartoyl) denotes the structure: Dhp 3,4-dehydroproline Dip β,β-diphenylalanine having the structure: Dmt 5,5-dimethylthiazolidine-4-carboxylic acid 2-Fua β-(2-furyl)-alanine Gln or Q glutamine Glu or E glutamic acid Gly or G glycine His or H histidine 3-Hyp trans-3-hydroxy-L-proline, i.e., (2S,3S)-3-hydroxypyrrolidine-2-carboxylic acid 4-Hyp 4-hydroxyproline, i.e., (2S,4R)-4-hydroxypyrrolidine-2-carboxylic acid Ile or I isoleucine Inc indoline-2-carboxylic acid Inp isonipecotic acid Ktp 4-ketoproline Leu or L leucine hLeu homoleucine Lys or K lysine Lys (biotinyl) lysine biotinyl having the structure: Met or M methionine 1-Nal β-(1-naphthyl)-L-alanine 2-Nal β-(2-naphthyl)-L-alanine Nle norleucine Nva norvaline Oic octahydroindole-2-carboxylic acid Orn ornithine 2-Pal β-(2-pyridiyl)alanine 3-Pal β-(3-pyridiyl)alanine 4-Pal β-(4-pyridiyl)alanine Phe or F phenylalanine hPhe homophenylalanine Pff pentafluorophenylalanine having the structure: Pip pipecolic acid Pim 2′-(4-phenyl)imidazolyl having the structure: Pro or P proline Ser or S serine Taz β-(4-thiazolyl)alanine having the structure: 2-Thi β-(2-thienyl)alanine 3-Thi β-(3-thienyl)alanine Thr or T threonine Thz thiazolidine-4-carboxylic acid Tic 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid Tle tert-leucine Trp or W tryptophan Tyr or Y tyrosine Val or V valine

When a non-amino acid imidazole moiety (e.g., Pim, defined above) is present at the C-terminus of a compound of the invention, it is understood that the imidazole moiety is attached to the adjacent amino acid via a pseudo-peptide bond (w), wherein a bond is form between the position 2 carbon of the imidazole ring and the alpha carbon of the amino acid. For example, in the case where the adjacent amino acid is D-trptophan (D-Trp) and the imidazole moiety is Pim, the C-terminus of the peptide would appear as follows:

As used herein, Acc encompases an amino acid selected from the group of 1-amino-1-cyclopropanecarboxylic acid (A3c); 1-amino-1-cyclobutanecarboxylic acid (A4c); 1-amino-1-cyclopentanecarboxylic acid (A5c); 1-amino-1-cyclohexanecarboxylic acid (A6c); 1-amino-1-cycloheptanecarboxylic acid (A7c); 1-amino-1-cyclooctanecarboxylic acid (A8c); and 1-amino-1-cyclononanecarboxylic acid (A9c).

As used herein, a “peptidyl analog of ghrelin” encompasses ghrelin analogues and peptidyl analogs thereof which can be used to practice the therapeutic method of the present invention including, but not limited to, the following compounds:

(SEQ ID NO: 1) (Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,6)hGhrelin(1-28)-NH2; (SEQ ID NO: 5) (Aib2,A5c12)hGhrelin(1-28)-NH2; (SEQ ID NO: 6) (Aib2,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 7) (Aib2,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 10) (A5c2)hGhrelin(1-28)-NH2; (SEQ ID NO: 10) (Act2)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,6)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 11) (Aib2,8)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,9)hGhrelin(1-28)-NH2; (SEQ ID NO: 12) (Aib2,10)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Aib6)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (Aib5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 3) (Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 13) (Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 16) (Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Aib9)hGhrelin(1-28)-NH2; (SEQ ID NO: 17) (Aib10)hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(Octanesulfonyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(Octanesulfonyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 20) (Aib2,6,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 21) (Aib2,Dap3(Octanesulfonyl),A5c12)hGhrelin(1-28)-NH2; (SEQ ID NO: 22) (Aib2,Dap3(Octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 23) (Aib2,Dap3(Octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 20) (Aib2,Dap3(Octanesulfonyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 25) (Aib2,Dap3(Octanesulfonyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 25) (Aib2,Dap3(Octanesulfonyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 26) (A5c2,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 26) (Act2,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(Octanesulfonyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,5,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(Octanesulfonyl),hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 18) (Aib2,Dap3(Octanesulfonyl),Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 20) (Aib2,6,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 20) (Aib2,Dap3(Octanesulfonyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 20) (Aib2,Dap3(Octanesulfonyl),Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 25) (Aib2,Dap3(Octanesulfonyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 25) (Aib2,Dap3(Octanesulfonyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 25) (Aib2,Dap3(Octanesulfonyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 25) (Aib2,Dap3(Octanesulfonyl),Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 27) (Aib2,8,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,Dap3(Octanesulfonyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 24) (Aib2,9,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 28) (Aib2,10,Dap3(Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(Octanesulfonyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(Octanesulfonyl),Aib6)hGhrelin(1-28)-NH2; (SEQ ID NO: 30) (Dap3(Octanesulfonyl),A5c12)hGhrelin(1-28)-NH2; (SEQ ID NO: 31) (Dap3(Octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 32) (Dap3(Octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(Octanesulfonyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(Octanesulfonyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(Octanesulfonyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(Octanesulfonyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(Octanesulfonyl),Aib5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(Octanesulfonyl),hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 19) (Dap3(Octanesulfonyl),Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(Octanesulfonyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 29) (Dap3(Octanesulfonyl),Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(Octanesulfonyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(Octanesulfonyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(Octanesulfonyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 34) (Dap3(Octanesulfonyl),Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 35) (Dap3(Octanesulfonyl),Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 33) (Dap3(Octanesulfonyl),Aib9)hGhrelin(1-28)-NH2; (SEQ ID NO: 36) (Dap3(Octanesulfonyl),Aib10)hGhrelin(1-28)-NH2; (SEQ ID NO: 31) (Dap3(Octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 31) (Dab3(Octanesulfonyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,Act6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Dmt7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Thz7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,A5c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,hLeu5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,Cha5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,Thr6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 39) (Aib2,Abu6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,4-Hyp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Pip7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Dhp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 41) (Aib2,Ktp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 42) (Aib2,8,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,2-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,4-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,Taz9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,2-Thi9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,2-Fua9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,Apc9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 40) (Aib2,9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 43) (Aib2,10,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 32) (Dap3(Octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 32) (Dab3(Octanesulfonyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,A6c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (A6c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,Act6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Dmt7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Thz7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,A5c5,12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,hLeu5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 44) (Aib2,Cha5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,Thr6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 46) (Aib2,Abu6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,4-Hyp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Pip7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Dhp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 48) (Aib2,Ktp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 49) (Aib2,8,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,2-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,4-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,Taz9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,2-Thi9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,2-Fua9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,Apc9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 47) (Aib2,9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 50) (Aib2,10,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Aib6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Act6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Dmt7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Thz7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (A5c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (Aib5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (hLeu5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 38) (Cha5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Aib6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Thr6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 51) (Abu6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (4-Hyp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Pip7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Dhp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 53) (Ktp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 54) (Aib8,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (2-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (4-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (Taz9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (2-Thi9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (2-Fua9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (Apc9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 52) (Aib9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 55) (Aib10,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Aib6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (A5c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Act6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Dmt7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Thz7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (Aib5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (hLeu5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 45) (Cha5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Thr6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 56) (Abu6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (4-Hyp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Pip7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Dhp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 58) (Ktp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 59) (Aib8,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (2-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (4-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (Taz9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (2-Thi9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (2-Fua9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (Apc9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 57) (Aib9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 60) (Aib10,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,Glu3(NH-Hexyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-Hexyl),A6c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,6,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,Glu3(NH-Hexyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-Hexyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-Hexyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,Glu3(NH-Hexyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,5,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 61) (Aib2,Glu3(NH-Hexyl),hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,6,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,Glu3(NH-Hexyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 63) (Aib2,Glu3(NH-Hexyl),Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-hexyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-Hexyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-Hexyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 65) (Aib2,Glu3(NH-Hexyl),Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 27) (Aib2,8,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,Glu3(NH-Hexyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 64) (Aib2,9,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 28) (Aib2,10,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-Hexyl),Aib6)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-Hexyl),A5c5)hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-Hexyl),Act6)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-Hexyl),Dmt7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-Hexyl),Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-Hexyl),Aib5)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-Hexyl),hLeu5)hGhrelin(1-28)-NH2; (SEQ ID NO: 62) (Glu3(NH-Hexyl),Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-Hexyl),Thr6)hGhrelin(1-28)-NH2; (SEQ ID NO: 66) (Glu3(NH-Hexyl),Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-Hexyl),4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-Hexyl),Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-Hexyl),Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 68) (Glu3(NH-Hexyl),Ktp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 35) (Glu3(NH-hexyl),Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),2-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),2-Fua9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),Apc9)hGhrelin(1-28)-NH2; (SEQ ID NO: 67) (Glu3(NH-Hexyl),Aib9)hGhrelin(1-28)-NH2; (SEQ ID NO: 36) (Glu3(NH-Hexyl),Aib10)hGhrelin(1-28)-NH2; (SEQ ID NO: 69) (Aib2,Glu3(NH-Hexyl),A6c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 70) (A6c5,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 71) (Aib2,6,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 71) (Aib2,Glu3(NH-Hexyl),Act6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-Hexyl),Dmt7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-Hexyl),Thz7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 69) (Aib2,Glu3(NH-Hexyl),A5c5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 69) (Aib2,5,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 37) (Aib2,hLeu5,A5c12,Orn5)hGhrelin(1-28)-NH2; (SEQ ID NO: 69) (Aib2,Glu3(NH-Hexyl),Cha5,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 71) (Aib2,6,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 71) (Aib2,Glu3(NH-Hexyl),Thr6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 71) (Aib2,Glu3(NH-Hexyl),Abu6,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-Hexyl),4-Hyp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-Hexyl),Pip7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-Hexyl),Dhp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 73) (Aib2,Glu3(NH-Hexyl),Ktp7,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 74) (Aib2,8,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),2-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),3-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),4-Pal9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),Taz9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),2-Thi9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),2-Fua9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,Glu3(NH-Hexyl),Apc9,A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 72) (Aib2,9,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 75) (Aib2,12,Glu3(NH-Hexyl),4-Pal9,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 76) (Aib2,10,Glu3(NH-Hexyl),A5c12,Orn15)hGhrelin(1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-Hexyl),A6c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 78) (Glu3(NH-Hexyl),A6c5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 79) (Aib2,6,Glu3(NH-Hexyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 79) (Aib2,Glu3(NH-Hexyl),Act6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-Hexyl),Dmt7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-Hexyl),Thz7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-Hexyl),A5c5,12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 77) (Aib2,5,Glu3(NH-Hexyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-Hexyl),hLeu5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 77) (Aib2,Glu3(NH-Hexyl),Cha5,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 79) (Aib2,6,Glu3(NH-Hexyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 79) (Aib2,Glu3(NH-Hexyl),Thr6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 79) (Aib2,Glu3(NH-Hexyl),Abu6,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-Hexyl),4-Hyp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-Hexyl),Pip7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-Hexyl),Dhp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 81) (Aib2,Glu3(NH-Hexyl),Ktp7,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 82) (Aib2,8,Glu3(NH-Hexyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),2-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),3-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),4-Pal9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),Taz9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),2-Thi9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),2-Fua9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,Glu3(NH-Hexyl),Apc9,A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 80) (Aib2,9,Glu3(NH-Hexyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 83) (Aib2,10,Glu3(NH-Hexyl),A5c12,Apc16)hGhrelin(1-28)-NH2; (SEQ ID NO: 1) (Glu3(O-hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 10) (Aib2)hGhrelin(1-28)-NH2; (SEQ ID NO: 1) (Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 84) (Aib2,Glu3(O-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 85) (Aib1,Glu3(O-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 84) (Aib2,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 1) (Dap3(1-Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 84) (Aib2,Dap3(1-Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 85) (Aib1,Dap3(1-Octanesulfonyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 86) (Ava2,Dap3(1-Octanesulfonyl))hGhrelin(2-28)-NH2; (SEQ ID NO: 87) (Ac-Gly1)hGhrelin(1-5)-NH2; (SEQ ID NO: 88) (Ac-Gly1)hGhrelin(1-6)-NH2; (SEQ ID NO: 89) (Ac-Gly1)hGhrelin(1-7)-NH2; (SEQ ID NO: 90) (Ac-Gly1,Aib2)hGhrelin(1-28)-NH2; (SEQ ID NO: 91) (Ac-Gly1,Aib2,Glu3(NH-Hexyl))hGhrelin(1-5)-NH2; (SEQ ID NO: 92) (Ac-Gly1,Aib2,Glu3(NH-Hexyl))hGhrelin(1-6)-NH2; (SEQ ID NO: 93) (Ac-Gly1,Aib2,Glu3(NH-Hexyl))hGhrelin(1-7)-NH2; (SEQ ID NO: 335) (Ac-Gly1,Aib2,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 94) (Ac-Gly1,Aib2,Glu3(NH-Hexyl),Arg8)hGhrelin(1-8)-NH2; (SEQ ID NO: 94) (Ac-Gly1,Aib2,Glu3(NH-Hexyl),Lys8)hGhrelin(1-8)-NH2; (SEQ ID NO: 95) (n-Butyryl-Gly1)hGhrelin(1-28)-NH2; (SEQ ID NO: 335) (n-Butyryl-Gly1,Aib2,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; (SEQ ID NO: 95) (Isobutyryl-Gly1)hGhrelin(1-28)-NH2; or (SEQ ID NO: 95) (n-Octanoyl-Gly1)hGhrelin(1-28)-NH2, or a pharmaceutically acceptable salt thereof. (SEQ ID NO: 1) Cys3(S(CH2)9CH3)hGhrelin(1-28)-NH2; (SEQ ID NO: 10) (Aib2,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,6,Ser3)hGhrelin(1-28)-NH2 (SEQ ID NO: 8) (Aib2,Ser3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 2) (Aib2,Ser3,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 4) (Aib2,Ser3,Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Ser3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 11) (Aib2,8,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 96) (Ac-Gly1,Aib2,10,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 12) (Aib2,10,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 97) (n-Butyryl-Gly1,Aib2,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 97) (Ac-Gly1,Aib2,Ser3)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 98) (Ac-Gly1,Aib2,Ser3,Arg8)hGhrelin(1-28)-NH2; (SEQ ID NO: 16) (Ser3,Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 8) (Aib2,Ser3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 14) (Ser3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 15) (Ser3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 9) (Aib2,Ser3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 99) (Aib2,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 99) (Aib2,6,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 100) (A5c5,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 101) (Aib2,Thr3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Thz7)hGhrelin(1-28)-NH2; (SEQ ID NO: 103) (Aib2,Thr3,Cha5)hGhrelin(1-28)-NH2; (SEQ ID NO: 99) (Aib2,Thr3,Abu6)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 101) (Aib2,Thr3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Dhp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 11) (Aib2,8,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Pip7)hGhrelin(1-28)-NH2; (SEQ ID NO: 104) (Ac-Gly1,Aib2,10,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 106) (Aib2,10,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 105) (n-Butyryl-Gly1,Aib2,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 105) (Ac-Gly1,Aib2,Thr3)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 90) (Ac-Gly1,Aib2,Thr3,Arg8)hGhrelin(1-28)-NH2; (SEQ ID NO: 107) (Thr3,Aib8)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,Taz9)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,3-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,4-Pal9)hGhrelin(1-28)-NH2; (SEQ ID NO: 101) (Aib2,Thr3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 108) (Thr3,2-Thi9)hGhrelin(1-28)-NH2; (SEQ ID NO: 109) (Thr3,4-Hyp7)hGhrelin(1-28)-NH2; (SEQ ID NO: 102) (Aib2,Thr3,Tic7)hGhrelin(1-28)-NH2; (SEQ ID NO: 110) (Ac-Gly1,Glu3(NH-Hexyl))hGhrelin(1-28)-NH2; or (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Pal-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-4-Pal-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Orn-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bip-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Dip-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bpa-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 114) H-Inp-D-2-Nal-D-Bpa-Phe-Lys-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 117) H-Inp-D-Bip-D-Trp-Phe-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 117) H-Inp-D-Dip-D-Trp-Phe-NH2; (SEQ ID NO: 118) H-Inp-D-2-Nal-D-Dip-Phe-NH2; (SEQ ID NO: 119) H-Inp-D-Bal-D-Trp-Phe-NH2; (SEQ ID NO: 118) H-Inp-D-2-Nal-D-Bal-Phe-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Pal-Lys-NH2; (SEQ ID NO: 120) H-Inp-D-Trp-D-2-Nal(Ψ)-Pim; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 122) H-Inp-D-2-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 122) H-Inp-D-1-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 122) H-Inp-D-Bal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 123) H-Apc-D-2-Nal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 125) H-Apc-D-1-Nal-D-Trp-Phe-NH2; (SEQ ID NO: 126) H-Inp-D-2-Nal-D-Trp(Ψ)-Pim; (SEQ ID NO: 126) H-Inp-D-1-Nal-D-Trp(Ψ)-Pim; (SEQ ID NO: 126) H-Inp-D-Bal-D-Trp(Ψ)-Pim; (SEQ ID NO: 127) H-Aib-D-Ser(Bzl)-D-Trp(Ψ)-Pim; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 123) H-Apc-D-Bal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-1-Nal-Phe-Apc-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 131) H-Apc-D-1-Nal-D-1-Nal-Phe-Lys-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-1-Nal-Phe-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-1-Nal-Phe-Lys-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-2-Nal-Phe-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 125) H-Apc-D-Bal-D-Trp-Phe-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-2-Thi-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-Taz-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 135) H-Inp-D-1-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 135) H-Inp-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-1-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Pal-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 137) H-Apc-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Pal-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-3-Pal-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-4-Pal-NH2; (SEQ ID NO: 138) H-Apc-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 136) H-Apc-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 139) H-Apc-D-2-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-2-Fua-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Fua-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Pal-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-2-Thi-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-2-Thi-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-3-Pal-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-3-Thi-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-3-Thi-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-4-Pal-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-Pff-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Pff-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-Bal-Phe-Apc-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Phe-NH2; (SEQ ID NO: 140) H-Apc-D-Bal-D-Bal-Taz-Apc-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 142) H-Apc-D-Bal-D-Bal-Taz-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-2-Fua-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-2-Pal-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-3-Pal-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-3-Thi-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-4-Pal-NH2; (SEQ ID NO: 143) H-Apc-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 144) H-Apc-D-Bal-D-Trp-Pff-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 146) H-Inp-D-1-Nal-D-Bal-2-Fua-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 146) H-Inp-D-1-Nal-D-Bal-Pff-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 145) H-Inp-D-1-Nal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 146) H-Inp-D-1-Nal-D-Bal-Taz-NH2; (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 147) H-Inp-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 116) H-Inp-D-1-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-2-Fua-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-3-Thi-NH2; (SEQ ID NO: 148) H-Inp-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 135) H-Inp-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-2-Fua-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-Pff-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 150) H-Inp-D-Bal-D-Bal-Taz-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-2-Fua-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-Pff-NH2; (SEQ ID NO: 152) H-Inp-D-Bal-D-Trp-Taz-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-2-Fua-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-Pff-NH2; or (SEQ ID NO: 153) H-Inp-D-Bip-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 154) H-Inp-D-Bip-D-Bal-Taz-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-2-Fua-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-Pff-NH2; (SEQ ID NO: 155) H-Inp-D-Bip-D-Trp-Taz-Lys-NH2; or (SEQ ID NO: 156) H-Inp-D-Bip-D-Trp-Taz-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Pal-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-4-Pal-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Orn-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bip-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Dip-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bpa-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 114) H-Inp-D-2-Nal-D-Bpa-Phe-Lys-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Thr(Bzl)-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Pff-NH2; (SEQ ID NO: 115) H-Inp-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 118) H-Inp-D-2-Nal-D-Dip-Phe-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Pal-Lys-NH2; (SEQ ID NO: 120) H-Inp-D-Trp-D-2-Nal(Ψ)-Pim; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 111) H-Inp-D-Bal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 122) H-Inp-D-2-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 122) H-Inp-D-1-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 122) H-Inp-D-Bal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 123) H-Apc-D-2-Nal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 126) H-Inp-D-2-Nal-D-Trp(Ψ)-Pim; (SEQ ID NO: 126) H-Inp-D-1-Nal-D-Trp(Ψ)-Pim; (SEQ ID NO: 126) H-Inp-D-Bal-D-Trp(Ψ)-Pim; (SEQ ID NO: 127) H-Aib-D-Ser(Bzl)-D-Trp(Ψ)-Pim; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Taz-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Thi-Lys-NH2; (SEQ ID NO: 123) H-Apc-D-Bal-D-Trp-Phe-Lys-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-Trp-Phe-Apc-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-1-Nal-Phe-Apc-NH2; (SEQ ID NO: 129) H-Apc-D-1-Nal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 131) H-Apc-D-1-Nal-D-1-Nal-Phe-Lys-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-1-Nal-Phe-Apc-NH2; (SEQ ID NO: 130) H-Apc-D-Bal-D-2-Nal-Phe-Apc-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-1-Nal-Phe-Lys-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-2-Nal-Phe-Lys-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-Phe-NH2; (SEQ ID NO: 133) H-Apc-D-1-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-2-Thi-NH2; (SEQ ID NO: 157) H-Apc-D-Bal-D-Trp-Taz-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-2-Thi-NH2; (SEQ ID NO: 134) H-Apc-D-2-Nal-D-Trp-Taz-NH2; (SEQ ID NO: 135) H-Inp-D-1-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 135) H-Inp-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-1-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 136) H-Apc-D-Bal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 113) H-Inp-D-2-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 121) H-Inp-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 151) H-Inp-D-Bal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 128) H-Apc-D-Bal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 149) H-Inp-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 132) H-Apc-D-Bal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 141) H-Apc-D-Bal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 112) H-Inp-D-1-Nal-D-Trp-Pff-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-Phe-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-2-Thi-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-3-Thi-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-Taz-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-2-Fua-Lys-NH2; (SEQ ID NO: 158) H-Inp-D-1-Nal-D-Bal-Pff-Lys-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-2-Thi-Apc-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 135) H-Inp-D-2-Nal-D-Trp-Taz-Apc-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 159) H-Inp-D-2-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 160) H-Inp-D-1-Nal-D-Trp-3-Thi-Apc-NH2; (SEQ ID NO: 160) H-Inp-D-1-Nal-D-Trp-2-Fua-Apc-NH2; (SEQ ID NO: 160) H-Inp-D-1-Nal-D-Trp-Pff-Apc-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-3-Thi-Lys-NH2; (SEQ ID NO: 124) H-Apc-D-1-Nal-D-Trp-2-Fua-Lys-NH2; (SEQ ID NO: 124)