Abstract: This disclosure concerns the discovery of (R,R)- and (R,S)-fenoterol analogs which are highly effective at binding ?2-adrenergic receptors. Exemplary chemical structures for these analogs are provided. Also provided are pharmaceutical compositions including the disclosed (R,R)-fenoterol and fenoterol analogs, and methods of using such compounds and compositions for the treatment of cardiac disorders such as congestive heart failure and pulmonary disorders such as asthma or chronic obstructive pulmonary disease.

Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: Several classes of in vivo carbon monoxide-releasing compounds are useful for the treatment and/or prevention of diseases, such as chronic inflammatory, e.g., rheumatoid arthritis, and of diseases with a strong inflammatory component, such as atherosclerosis, stroke, coronary disease, and Alzheimers disease. The in vivo carbon monoxide-releasing compounds can be attached to known drug vectors and/or known anti-inflammatory drugs, such as aspirin.

Abstract: Methods of using an ETB receptor agonist, such as IRL-1620, for the treatment of stroke or cerebrovascular accidents are disclosed. The ETB receptor agonist is used alone or in combination with a second agent useful in the treatment of stroke or other cerebrovascular accident.

Abstract: A preparation is disclosed for producing enhanced blood flow in tissue thus causing beneficial effects such as promoting hair growth on scalp tissue lacking sufficient hair, restoring normal sexual function in males with erectile dysfunction. Specifically, this is a preparation which provides local delivery of the amino acid L-arginine, an important biological precursor to the main substance which is responsible for relaxation of blood vessels permitting enhancement of blood flow. In the preferred embodiments, the L-arginine is provided so that it can be topically applied to the scalp or penis. The preparation also contains an agent which aids in the transfer of L-arginine into the tissue. In the preferred embodiments this agent overcomes the resistance to transfer caused by the high charge density of L-arginine. In the preferred embodiments this means is high ionic strength created by addition of choline chloride, magnesium chloride and sodium chloride.

Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.

Abstract: The invention provides methods for treating an obstructed biological conduit that include administering to the conduit an agent that can degrade extracellular matrix of obstructing tissue. Particular methods include delivery of an enzyme or a mixture of several enzymes to the area or region of obstruction wherein the enzyme(s) have the capability to degrade extracellular matrix components within the obstruction thereby restoring the normal flow of transported fluid through the conduit. The invention also includes prophylactically dilating a section of conduit to minimize the risk of obstruction formation. The invention further includes methods for prolonging patency of hemodialysis access.

Abstract: A composition for increasing blood flow is provided, wherein side effects such as lowering of blood pressure are reduced and blood flow is effectively increased in the capillaries. A composition containing arginine in an amount from 25 mg/kg body weight to 150 mg/kg body weight is also provided. A food composition or a feeding stuff containing the composition is also provided. Method of using the above compositions to increase blood flow is also provided.

Abstract: The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.

Abstract: The invention provides compositions for releasing nitric oxide (NO) comprising a matrix that encapsulates nitric oxide. Nitric oxide is released when the composition is exposed to an aqueous environment. The invention further provides methods of preparing the compositions and uses of the compositions for treating infections and disorders.

Abstract: The present invention relates to a pharmaceutical composition and method for treating and preventing musculoskeletal and connective tissue diseases of unknown etiology, such as different forms of arthritis and other rheumatic conditions, comprising a combination of therapeutic agents that improve the processes of blood circulation and angiogenesis in the affected tissues, as well as other supporting therapies. Among the components of herein proposed pharmaceutical composition, are: vitamin K, polyunsaturated fatty acids (blood thinner), and niacin (vasodilator and hypolipidemic agent).

Abstract: The present invention relates to methods and formulations for inhibiting, treating and preventing a malignant cell phenotype, cell, tumor and/or disease. Administration of nitric oxide mimetics, such as low doses, is sufficient to increase, restore or maintain nitric oxide-mediated signaling in cells so that malignant cell phenotypes, cells, tumors and/or diseases are inhibited or prevented. These methods and formulations are particularly useful in treating and preventing cancer in animals.

Abstract: Several classes of in vivo carbon monoxide-releasing compounds are useful for the treatment and/or prevention of diseases, such as chronic inflammatory, e.g., rheumatoid arthritis, and of diseases with a strong inflammatory component, such as atherosclerosis, stroke, coronary disease, and Alzheimers disease. The in vivo carbon monoxide-releasing compounds can be attached to known drug vectors and/or known anti-inflammatory drugs, such as aspirin.

Abstract: The present invention relates to a method for the prevention or the treatment of heart failure comprising administration of a therapeutically effective amount of an anticholinergic 1, medicaments for the prevention or treatment of heart failure comprising one or more, preferably one anticholinergic 1, and methods for the preparation of these medicaments.

Abstract: The invention provides methods to for treating a an obstructed biological conduit that include administering to the conduit an agent that can degrade extracellular matrix of obstructing tissue. Particular methods include delivery of an enzyme or a mixture of several enzymes to the area or region of obstruction wherein the enzyme(s) have the capability to degrade extracellular matrix components within the obstruction thereby restoring the normal flow of transported fluid through the conduit. The invention also includes prophylactically dilating a section of conduit to minimize the risk of obstruction formation.

Abstract: It is intended to find a compound that is structurally simpler than yohimbine, a pentacyclic condensed heterocyclic compound, and has an effect similar to that of yohimbine. The present invention relates to a pharmaceutical or food composition for ?2 receptor blockage comprising a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: (wherein R1 represents a hydrogen, alkyl group, alkenyl group, alkynyl group, aromatic group, aralkyl group, acyl group, arylsulfonyl group, alkylsulfonyl group, or hydroxyl group; R2 represents a hydrocarbon group; R3, R4, R5, R6, and R7 are the same or different and represent a hydrogen, halogen, alkyl group, or alkoxy group; R8 represents a hydrogen or acyl group; n represents an integer of 1 to 6; and a and b are the same or different and represent 1 or 0).

Abstract: The present invention relates to a preventive or therapeutic agent for a glomerular disease which comprises an anti-thrombocytic agent and an HMG-CoA reductase inhibitor as active ingredients. The above agent is useful for prevention and therapy of various glomerular diseases including chronic glomerular nephritis.

Abstract: The present invention relates to methods and formulations for inhibiting, treating and preventing a malignant cell phenotype, cell, tumor and/or disease. Administration of nitric oxide mimetics, such as low doses, is sufficient to increase, restore or maintain nitric oxide-mediated signaling in cells so that malignant cell phenotypes, cells, tumors and/or diseases are inhibited or prevented. These methods and formulations are particularly useful in treating and preventing cancer in animals.

Abstract: The application of L-arginine and its derivatives to the skin causes beneficial effects of wound healing, increasing erectile function and increased growth of hair when applied in sufficient quantity to the skin. A hostile biophysical agent may be combined with the L-arginine to increase its absorption into the skin. The desired concentrations of the hostile biophysical agent is increased when concentration of L-arginine is less than 20% of the concentration of the substance applied to maximize its effect.

Abstract: The invention relates to a dietary supplement consisting of an aqueous extract of red vine leaves and an acceptable carrier which prevents and reduces the discomfort relating to mild-to-moderate chronic venous insufficiency of the legs.

Abstract: A composition for the treatment of impaired glucose tolerance (IGT) including a compound which binds to a receptor for glucagon-like peptide-1, and a pharmaceutical carrier. The amount of the compound present is an effective amount to improve pancreatic ?-cell sensitivity to blood glucose levels in a human with IGT. Also, a method for improving the pattern of insulin secretory responses in a human with IGT by administering to the human a composition comprising a compound which binds to a receptor for glucagon-like peptide-1 and a pharmaceutical carrier.

Abstract: Xenon or xenon-containing gases and, where appropriate, an NO source are employed as medicament for cerebral protection. Cerebral protection is defined as reducing or preventing impairments of cerebral function of various causes, but especially secondary to perfusion impairments of unclear etiology. The medicament can be used for cerebral protection for the prophylaxis of impairments of cerebral perfusion and for therapy after cerebral disorders have occurred, irrespective of the cause (e.g. cognitive, sensory or motor in nature).

Abstract: A pharmaceutical composition contains a nitric oxide donor and advantageously an optional corticosteroid and/or topical anesthetic. The composition is useful in a method for treating anal disorders such as anal fissure, anal ulcer, hemorrhoidal disease, levator spasm, and so forth, by topical application to or proximate the affected area.

Abstract: The present invention relates to screening methods that make use of Myosin Phosphatase-Rho interacting Protein (M-RIP) for the identification of novel therapeutics for hypertension and hypertensive conditions. Also disclosed are methods for treating or preventing hypertension or hypertensive conditions by administering to a mammal a therapeutically effective amount of an agent that reduces the level or activity of M-RIP. According to this invention, the agent decreases contractile and increases relaxant effects of smooth muscle cells, ultimately decreasing the systemic blood pressure of a mammal. For example, the agent may reduce binding of M-RIP to myosin phosphatase, RhoA, or both.

Abstract: Pulmonary disorders in which the GSNO pool or glutathione pool in the lung is depleted and where reactive oxygen species in lung are increased, are treated by delivering into the lung as a gas, agent causing repletion or increase of the GSNO pool or protection against toxicity and does so independently of reaction with oxygen. Agents include ethyl nitrite, NOCl, NOBr, NOF, NOCN, N2O3, HNO, and H2S. Optionally, N-acetylcysteine, ascorbate, H2S or HNO is administered in addition to other GSNO repleting agent to potentiate the effect of said agent.

Abstract: The invention relates to a dietary supplement consisting of an aqueous extract of red vine leaves and an acceptable carrier which prevents and reduces the discomfort relating to mild-to-moderate chronic venous insufficiency of the legs.

Abstract: Methods and formulations for inhibiting and preventing a malignant cell phenotype by administering to cells a low dose of a nitric oxide mimetic are provided.

Abstract: The invention provides compositions and methods suitable for ameliorating female sexual dysfunction, and in particular, female sexual arousal disorder. In one embodiment, the invention provides a semisolid composition suitable for topical application comprising: an effective amount of a vasoactive prostaglandin, a polysaccharide thickener, a lipophilic component, and an acidic buffer system.

Abstract: A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen or C1-6 alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl or heteroaryl C1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring  attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain.

Abstract: The present invention describes rapid noninvasive methods for measuring vasodilation or changes in blood flow in a patient following administration of at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The method comprises the administration of at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent to the patient followed by monitoring the temperature change of an area of interest using infrared thermography.

Abstract: Methods and compositions are disclosed utilizing the optically pure (−) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of amlodipine. The (−) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (−) amlodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.

Abstract: Therapeutic formulations and methods for treating erectile dysfunction with a misoprostol compound in a subject are provided, a method comprising: obtaining a therapeutic formulation having an effective dose of a misoprostol compound in an excipient carrier; and applying the therapeutic formulation topically to the subject.

Abstract: A composition for improving the fertility of a male, and/or for improving the quality of the semen produced by a male includes at least one source of folic acid, preferably 0.05-8 mg; at least one source of zinc, preferably 5-50 mg; and optionally one or more of vitamin B12, magnesium, betaine, choline, SAM, vitamin B2, and Vitamin B6; and/or optionally one or more carriers, excipients and/or adjuvants.

Abstract: A tocotrienol-containing powder prepared by a process wherein an oil containing a tocotrienol is treated with a lecithin, a cellulose and an emulsifying agent in water to form an emulsion, a powder substance is mixed with the formed emulsion to form a suspension and then the formed suspension is spray-dried. The powder containing tocotrienol, which has excellent storage stability and free flowability, can be used in preparing a tablet which comprises the powder compressed into a tablet form.

Abstract: The present invention relates to polynucleotide and polypeptide molecules for use as inhibitors in hemostasis and immune function. Such inhibitors are members of the family of proteins bearing a collagen-like domain and a globular domain. The inhibitors are useful for promoting blood flow in the vasculature by reducing thrombogenic and complement activity. The inhibitors are also useful for pacifying collagenous surfaces and modulating wound healing.

Abstract: The present invention is directed to nitrosated or nitrosylated &agr;-adrenergic receptor antagonists, compositions comprising &agr;-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.

Abstract: Topical gelled compositions comprising a drug which causes vasodilation, and optionally prostaglandin E1, dispersed within a polymer matrix, and methods of treating sexual dysfunction, including both male and female sexual dysfunction, using said compositions.

Abstract: The invention provides a composition suitable for topical application comprising: an effective amount of a prostaglandin, a polymer thickener, a lipophilic component, and a buffer system. In another embodiment, the invention provides a composition suitable for topical application comprising: an effective amount of a vasoactive agent, a polymer thickener, a lipophilic component, and a buffer system. The invention also provides methods of ameliorating female sexual dysfunction. Also provided are methods of increasing female sexual arousal and methods of enhancing female sexual response.

Abstract: The use of a compound of formula (I) wherein R1 is H; C1-C3 alkyl; C1-C3 perfluoroalkyl; or C3-C5 cycloalkyl; R2 is H; optionally substituted C1-C6 alkyl; C1-C3 perfluoroalkyl; or C3-C6 cycloalkyl; R3 is optionally substituted C1-C6 alkyl; C1-C6 perfluoroalkyl; C3-C5 cycloalkyl; C3-C6 alkenyl; or C3-C6 alkynyl; R4 is optionally substituted C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkanoyl, (hydroxy)C2-C4 alkyl or (C2-C3 alkoxy)C1-C2 alkyl; CONR5R6; CO2R7; halo; NR5R6; NHSO2NR5R6; NHSO2R8; SO2NR9R10; or phenyl, pyridyl, pyrimidinyl, imidazolyl, oxazolyl, thiazolyl, thienyl or triazolyl any of which is optionally substituted with methyl; R5 and R6 are each independently H or C1-C4 alkyl, or together with the nitrogen atom to which they are attached form an optionally substituted pyrrolidinyl, piperidino, morpholino, 4-N(R11)-piperazinyl or imidazolyl group; R7 is H or C1-C4 alkyl; R8 is optionally substituted C1-C3 alkyl; R9 and R10 together with the nitrogen atom to which they are attached form an o

Abstract: There are provided a method to screen agonist or antagonist of the maxadilan receptor participating in vasodilating action, wherein a receptor of maxadilan is used, compounds which specifically bind to the receptor, and a tissue preparation having the receptor. The compounds are variants of maxadilan from the salivary glands of the sand fly.

Abstract: The goal in the treatment of female dysfunction is to increase blood flow to the genitals. Heretofore, treatments/developments have focused on prostaglandin E-I creams, topical sildenafil, aminoacids, etc, ingested systemic medications such as sildenafil, phentolamine, etc and mechanical devices. Our invention is a direct, local topical vasodilator with plant estrogen added to eliminate genital dryness, N-methylnicotinate and DHEA which is precusor for, among others, the hormone testosterone. Testosterone is important in both male and female sexuality.

Abstract: A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen or C1-6 alkyl; R1 represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, haloC1-6alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl or heteroarylC1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring  attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain.

Abstract: The invention relates to compositions, methods, apparatus, and kits for alleviating or preventing vasoconstriction or vasospasm in a mammal. The compositions, methods, apparatus, and kits are also useful for alleviating or preventing ischemic tissue damage resulting from ischemia associated with cerebral vasoconstriction which follows aneurysmal subarachnoid hemorrhage, with embolic stroke, with coronary artery obstruction, and with other conditions. These compositions, methods, apparatus, and kits generally relate to adventitial (i.e. extra-luminal) administration of a nitric oxide donor compound to a blood vessel in a mammal.

Abstract: A composition and method for treating circulatory conditions by promoting systemic vascular relaxation and dilation. Exemplary circulatory conditions are disclosed and include wound healing and/or reduction of hypertension. The composition is a natural combination of L-arginine, ginseng and Zizyphi fructus in an orally or topically administered dosage. The combination works synergistically to synthesize NO and thereby promote systemic vascular relaxation and dilation. The mechanism works in the wound compartment to promote and sustain the wound healing process. Likewise, the combined constituents, when administered orally or topically in proper concentration, work to maintain a critical threshold level of NO in areas that cannot themselves produce it, thereby promoting systemic vascular relaxation and dilation in order to reduce hypertension.

Abstract: The present invention refers to a method for producing vasodilation or analgesia in a mammal, comprising the use of vegetal material derived from the bark of a Trichilia species.

Abstract: The present invention describes methods for preventing and treating sexual dysfunctions in patients by orally administering at least one &agr;-adrenergic receptor antagonist and at least one compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo. The present invention also describes orally administrable compositions comprising at least one &agr;-adrenergic receptor antagonist and at least one compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo. In the present invention, the &agr;-adrenergic receptor antagonist is preferably yohimbine or phentolamine, and the compound that elevates endogenous nitric oxide or endothelium-derived relaxing factor in vivo is preferably L-arginine.

Abstract: The present invention describes novel compositions and kits comprising alpha-adrenergic receptor antagonists and compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, or stimulate nitric oxide synthesis. In preferred embodiments, the alpha-adrenergic receptor antagonist is an alkaloid selected from the group consisting of rauwolscine, corynanthine, yohimbine, apoyohimbine, beta-yohimbine, yohimbol, pseudoyohimbine and epi-3&agr;-yohimbine, and the compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, or stimulates nitric oxide synthesis is selected from the group consisting of L-arginine, S-nitroso-N-acetylcysteine, S-nitroso-captopril, S-nitroso-homocysteine, S-nitroso-cysteine and S-nitroso-glutathione. In other embodiments, the present invention describes novel compositions comprising yohimbine and L-arginine.

Abstract: Disulfiram (tetraethylthiuram disulfide) is shown to inhibit angiogenesis and to be useful in the treatment of angiogenesis-dependent disorders, including neoplasms, and to prevent cell hyperproliferation and formation of clots along or around medical devices.

Abstract: The present invention relates to dialysis solutions for peritoneal dialysis, containing hydroxyethyl starch as the osmotically-active substance, electrolytes and, optionally, conventional additives, where the hydroxyethyl starch has a molecular weight Mw in the range from 10,000 to 150,000, a substitution MS in the range from 0.10 to 0.40, a substitution DS in the range from 0.09 to 0.35 and a substitution ratio C2/C6≧8. With this peritoneal dialysis solution it is possible, with an outstanding ultrafiltration, to maintain a longer dwell time, for example the dialysis solution can be utilized for a period of 12 hours in the CAPD without replacement. In addition, the inventive dialysis solution is also particularly advantageous for patients with residual kidney function. The resorption of the osmotically active substance is clearly diminished and even after a dwell time of 12 hours it amounts to a maximum of 60-70%.