Abstract: Novel peptides that bind to human PAC1 are provided. These peptides that are antagonists of PAC1 are useful in a number of PAC1 related disorders, including the treatment and/or prevention of headache disorders, including migraine, such as acute migraine.

Abstract: The present invention relates to the treatment or prevention of tinnitus. More precisely, the present invention relates to a compound modulating chloride co-transporter NKCC1 (chloride co-transporter modulator) for use in the treatment of tinnitus. In addition, the present invention concerns pharmaceutical compositions comprising such an NKCC1 chloride co-transporter modulator as an active agent, a method for the treatment or prevention of tinnitus by administering such a chloride co-transporter modulator, and a screening method for the identification and characterization of compounds capable of modulating chloride co-transporter NKCC1.

Abstract: The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention.

Abstract: The present invention is directed to therapeutic compounds, treatment methods, and kits affecting the NCCa-ATP channel of neural tissue, including neurons, glia and blood vessels within the nervous system, and methods of using same. The NCCa-ATP channel is newly expressed in neural tissue following injury such as ischemia, and is regulated by the sulfonylurea receptor SUR1, being inhibited by sulfonylurea compounds, e.g., glibenclamide and tolbutamide, and opened by diazoxide. Antagonists of the NCCa-ATP channel, including SUR1 antagonists, are useful in the prevention, diminution, and treatment of injured or diseased neural tissue, including astrocytes, neurons and capillary endothelial cells, that is due to ischemia, tissue trauma, brain swelling and increased tissue pressure, or other forms of brain or spinal cord disease or injury. Agonists of the NCCa-ATP channel may be are useful in the treatment neural tissue where damage or destruction of the tissue, such as a gliotic capsule, is desired.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising potassium binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.

Abstract: Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.

Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.

Abstract: The present invention provides an artificial cerebrospinal fluid containing 120 to 160 mEq/L of sodium ion, 1 to 6 mEq/L of potassium ion, 75 to 155 mEq/L of chloride ion, and 5 to 45 mEq/L of bicarbonate ion, and provides an artificial cerebrospinal fluid further containing at least one component selected from the group consisting of 10 g/L or less of a reducing sugar, 5 mmol/L or less of phosphoric acid, 5 mEq/L or less of calcium ion, and 5 mEq/L or less of magnesium ion. The artificial cerebrospinal fluid of the present invention can prevent or reduce the incidence of cerebral edema and can further suppress brain cell disorders when used as an irrigation fluid or perfusion fluid in the field of neurosurgery, such as intracranial surgery, or when used as a replenishing fluid for lost cerebrospinal fluid.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising sodium-binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hypertension, chronic heart failure, end stage renal disease, liver cirrhosis, chronic renal insufficiency, fluid overload, or sodium overload.

Abstract: A protein which is composed N-terminally of one or several C-terminal parts of the amino acid sequence of the mature tumor necrosis factor and C-terminally of one or several N-terminal parts of the amino acid sequence of the mature tumor necrosis factor, which activates epithelial ion channels and improves the lung function and which can be used for the manufacture of medicaments for the treatment of diseases associated with the lung function, such as oedemas.

Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.

Abstract: The present invention is directed to therapeutic compositions targeting the NCCa-ATP channel of an astrocyte, neuron or capillary endothelial cell and methods of using same. More specifically, antagonists of the NCCa-ATP channel are contemplated. The compositions are used to prevent cell death and to treat secondary damage associated with spinal cord injury.

Abstract: A therapeutic method is provided to treat neutrophil-associated pulmonary diseases, such as chronic obstructive pulmonary disease, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising sodium-binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hypertension, chronic heart failure, end stage renal disease, liver cirrhosis, chronic renal insufficiency, fluid overload, or sodium overload.

Abstract: Compositions containing ?2 adrenergic agonists in combination with carbonates and carbonates of the formula and in combination with related steroid carbonates and carbonates are disclosed. The compositions are useful for treating bronchospasm, for inducing bronchodilator and for treating rhinitis, asthma, and chronic obstructive pulmonary disease (COPD) and inflammatory diseases, particularly by inhalation.

Abstract: A composition comprising a novel Ca2+-activated, [ATP]i-sensitive nonspecific cation (NCCa-ATP) channel is described. The channel is found in mammalian neural cells and exhibits a different sensitivity to block by various adenine nucleotides, and is activated by submicromolar [Ca]i. The NCCa-ATP channel is activated under conditions of ATP depletion, which causes severe cell depolarization, followed by cell swelling. The NCCa-ATP channel is regulated by a sulfonylurea receptor and is inhibited by sulfonylurea compounds glibenclamide and tolbutamide. Methods employing compositions comprising the NCCa-ATP channel to screen for compounds that block the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described. In addition, methods employing compositions comprising the Kir2.3 channel to screen for compounds that open the channel and the use of such antagonists as therapeutics in preventing brain swelling and damage are described.

Abstract: The present invention is directed to methods that can be used in the treatment of wounds, burns, and photodamaged skin. Methods can be used for both humans and animals and involve the administration of compositions containing selegiline and/or desmethylselegiline.

Abstract: A method of reducing inflammation in a variety of disorders by using an intraperitoneal solution of magnesium. The solution can be used for treating inflammatory and inflammation-related disorders in animals and/or humans. Application of the solution reduces inflammation and thereby assists in the healing process. An alternative method involves the intraperitoneal administration of a solution containing magnesium salts. Another alternative method provides for treatment of inflammatory and inflammation-related disorders in animals by way of intraperitoneal administration of a solution containing magnesium salts, methenamine or its salts and dextrose. The method further provides the use of methenamine or its salts and/or dextrose in combination with magnesium.

Abstract: A treatment for brain, spinal and nerve injury comprising use of a substance P receptor antagonist optionally in combination with a magnesium compound. There is also provided a formulation for use in this treatment comprising a substance P receptor antagonist and a magnesium compound.

Abstract: The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method includes administering to a mammal an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. The present invention also provides a method of treatment of cocaine, morphine, heroin, nicotine, amphetamine, methamphetamine, or ethanol addiction by treating a mammal with an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof.

Abstract: The present invention is directed to methods that can be used in the treatment of wounds, burns, and photodamaged skin. Methods can be used for both humans and animals and involve the administration of compositions containing selegiline and/or desmethylselegiline.

Abstract: Neural tissue edema is treated by circulating a hyperoncotic artificial cerebrospinal fluid in the cerebrospinal fluid pathway in the vicinity of edematous tissue to cause the edematous tissue to be dehydrated due to an oncotic gradient between the hypertonic artificial cerebrospinal fluid and intracellular fluid and withdrawing the fluid from the pathway after it has been so circulated.

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 present disclosure relates to novel nutritional compositions containing linoleic acid and/or linolenic acid which optimize child neurological development and provide improved nutritional support for women prior to and during lactation. The nutritional compositions are intended for use by women to optimize infant neurological development and provide improved nutritional support for women prior to, during and after lactation.

Abstract: The present invention comprises a selection of herbal, organic and inorganic materials with curative effects combined in a powdered form for human ingestion. The demonstrated benefits on human female hormone regulation or replacement include return from irregular to regular and less painful menstrual cycles, raising estrogen and progesterone levels to normal levels through menstrual cycles, return to regular menstrual cycle hormone levels with apparent infertility cure, and return to normative metabolic response from apparent circulatory abnormalities such as excessive sweating, edema, cold hand and feet, stiffness and other such symptoms.

Abstract: A cerebral function improving agent containing as the active ingredient a compound represented by the following formula: ##STR1## wherein R.sub.2 represents a hydrogen atom when R.sub.1 is a hydroxyl group;or R.sub.1 or R.sub.1 are combined together to form an oxo group;R.sub.3 represents a hydrogen atom, an alkali metal, or a monohydric, dihydric or trihydric alcohol residue,which may be an oligomer composed of 2-10 molecules when R.sub.1 represents a hydroxyl group and R.sub.2 and R.sub.3 represent hydrogen atoms.The agent suppresses cerebral edema, protects cerebral function, impaired cerebral energy metabolism, and reduces the extent of cerebral infarction.

Abstract: The present invention relates to a composition for treating or preventing brain edemas which comprises containing an endothelin antagonist as an active ingredient, for example, the compound of the following formula (I): ##STR1## or pharmaceutically acceptable salts or hydrates thereof, bosentan, cyclo?D-aspartyl-L-?3-(4-phenylpiperazin-1-ylcarbonyl)!-alanyl-L-aspartyl- D-?2-(2-thienyl)!glycyl-L-leucyl-D-tryptophyl!disodium or cyclo ?D-Asp-L-Pro-D-Val-L-Leu-D-Trp!.Furthermore, the present invention provides a method for treating or preventing brain edemas, which comprises administering an effective amount of an endothelin antagonist and use of an endothelin antagonist for the manufacture of a medicament for treating or preventing brain edemas.An endothelin antagonist exhibits an inhibitory effect, on all brain edemas regardless of the onset mechanism and thus is highly useful in the treatment or prevention of brain edemas.

Abstract: The present invention provides an epidermal gel secretion of Arabian Gulf catfish which is useful in enhancing wound healing, alleviating muscle spasms and pain, and treating dermatological disorders.

Abstract: The use of carotenoids for producing drugs for the treatment of inflammatory disorders not caused by the action of light or an infection with microorganisms.

Abstract: A magnesium-taurine compound and its method of synthesis. The compound is synthesized by reacting taurine and magnesium in a 2:1 molar ratio. The resulting mixture is diluted with methanol and the remaining clear filtrate is crystallized from methanol. This compound may be administered orally as a nutritional supplement or may be administered orally or intravenously for the therapeutic or prophylactic treatment of pre-eclampsia/eclampsia and acute cardiac conditions.

Abstract: The invention concerns the identification on eosinophils of the A3 adenosine receptor subtype and the blockade of said receptor in order to achieve inhibition of eosinophil activation and degranulation.

Abstract: A novel pharmaceutical use of a dihydropyridine derivative of the formula (I) ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each is an alkyl or the like; R.sub.4 is a hydrogen atom or the like; R.sub.5 is nitro, a halogenated alkyl, cyano or the like; X is a vinylene or an azomethine; A is an alkylene; and B is --N(R.sub.6) (R.sub.7) or a group of the formula ##STR2## wherein R.sub.6 and R.sub.7 are the same or different and each is an alkyl, an aralkyl, an aryl or the like; R.sub.8 and Ar are aryl or the like; and n is 0, 1 or 2, or an acid addition salt thereof for promoting PGI.sub.2 production, and for the treatment and prevention of hyperlipemia, arteriosclerosis and cerebral diseases.

Abstract: A novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R.sup.3, R.sup.4 and R.sup.5 are an optionally acylated hydroxyl optionally substituted amino group, alkoxy group or aliphatic group, or two of R.sup.3, R.sup.4 and R.sup.5 may be linked together to form a carbocyclic group; R.sup.6 and R.sup.7 are an aliphatic group and at least: one of them has a methylene group at the .alpha.-position; R.sup.8 and R.sup.9 are a hydrogen atom or an aliphatic group or aromatic group, or a salt thereof is useful for medicines for treating various diseases such as arterial sclerosis, hepatopathy, cerebrovascular diseases and the like.

Abstract: Unique methods for treating edemas in living subjects are provided comprising administering an effective amount of an antamanide or an antamanide analogue to the subject. The methods offer prophylactic and therapeutic modes of treatment for both localized and systemic edemas. The antamanides and antamanide analogues may be applied topically or given parenterally; and may be employed with other diverse agents for treatment of both inflammatory and non-inflammatory edemas.

Abstract: A method of treating a mammal for the presence or the activity of H. pylori in the gastrointestinal tract is disclosed. The method encompasses orally administering to said mammal a sufficient amount of a scavenging, reacting or inactivating compound to remove bicarbonate ions, ammonium ions or urea which are present in combination with the microorganisms which colonize and infect the gastric mucosa. Such microorganisms have been implicated in gastritis, gastric ulcer disease and as a risk factor in gastric carcinoma.Also, the invention encompasses a method, utilizing similar compounds, for the treatment or prevention of dermatitis such as diaper rash wherein these compounds are preapplied to the skin or used to treat the diaper prior to use.Also included are compositions which are used for the methods described above.

Abstract: Unique methods for treating interleukin-mediated edemas in living subjects are provided comprising administering an effective amount of a composition selected from the group consisting of phallotoxins, phallotoxin analogues, antamanide, or an antamanide analogue to the subject. The methods offer prophylactic and therapeutic modes of treatment for both localized and systemic interleukin-mediated edemas. The compositions of choice may be applied topically or given parenterally; and may be employed with other diverse agents for treatment of both inflammatory and non-inflammatory edemas.

Abstract: Process for the preparation of pearls based on a pharmaceutical active substance exhibiting an indefinite crystallization point. The said active substance is mixed in molten form which a pharmaceutical excipient promoting the solidification of the active substance, the melt is forced to pass through a nozzle which is subjected to a vibration, the pearls formed are allowed to fall in a tower countercurrentwise to a gas, and the pearls formed are collected in the bottom of the tower.

Abstract: A method of treating an osmotic disturbance in an animal which comprises administering to an animal an effective amount of an organic osmolyte, wherein the organic osmolyte is a polyol. Specific polyols include myo-inositol and sorbitol. Also included are precursors of organic osmolytes including precursors of polyols. Other polyol precursors are selected from the group consisting of glucose, glucose polymers, and glycerol. Also incluThis invention was funded by a research grant from the National Institutes of Health, 1RO1 DK36031, which provides to the United States Government certain rights in the invention.

Abstract: A method is described for treating and/or preventing pulmonary oedema in patients comprising administering a suphonylurea compound or a pharmaceutically acceptable salt thereof to patients who suffer from or are susceptible to oedema. Glucose may also be simultaneously administered to the patients to prevent hypoglycemia.

Abstract: A mouthwash is disclosed and claimed which comprises silver acetate, ammonium nitrate, and nitric acid which, when present as a residue in the oral cavity, will cause an adverse taste when the user smokes a tobacco product. The bitter taste experience causes the development of an aversion to smoking. The use of other non-toxic silver compounds is also disclosed.

Abstract: A quinone derivative of the formula (I): ##STR1## in which A is a group of the formula (IV): ##STR2## or a group of the formula (V): ##STR3## in which X and Y are either the same as or different from each other and each are hydroxy, methoxy or hydrogen; and n is an integer of 1 to 5,is disclosed. The compound is useful as a medicament.

Abstract: Compound of general formula I: ##STR1## in which: A is a single or double bond,R.sub.1 and R.sub.3, which may be identical or different, are each a hydrogen atom, an alkoxycarbonylmethylene radical of formula --CH.sub.2 CO.sub.2 R.sub.4 (in which R.sub.4 denotes an alkyl radical having 1 to 5 carbon atoms) or a radical of formula W: ##STR2## (in which n is equal to 0 or 1 and R.sub.5, R.sub.6 and R.sub.7, which may be identical or different, are each a hydrogen or halogen atom, a hydroxyl radical, a trifluoromethyl radical, a lower alkyl radical containing 1 to 5 carbon atoms or an alkoxy radical containing 1 to 5 carbon atoms),R.sub.2 is a hydrogen atom, an alkoxycarbonylmethylene radical of formula --CH.sub.2 CO.sub.2 R.sub.4, a radical of formula W, or a .beta.-glucose or rutinose molecule linked to the oxygen to which it is attached with a glycoside bond,on condition, however, that at least either R.sub.1 or R.sub.2 or R.sub.

Abstract: This invention provides a method of inhibiting osmotic water flow across mammalian cell membranes which involves contacting the water channels of the cell membranes with an effective amount of a glucose transport blocker or of digitonin so as to inhibit osmotic water flow across the membranes.Additionally, this invention provides a method of treating a subject afflicted with a condition associated with abnormal osmotic water flow across cell membranes which comprises administering to the subject an effective amount of a glucose transport blocker or of digitonin so as to contact the water channels of the subject's cell membranes and inhibit osmotic water flow across the membranes.

Abstract: Cosmetic Base composition exhibiting therapeutic properties comprising an acyl fatty acid alpha-hydroxy carboxylic acid ester or alkali metal salt thereof, a sucrose fatty acid ester, and a solvent.

Abstract: The present invention is a group of biologically active agents, di-hydroxy alkyl glycerols with vicinal hydroxyl groups and their acetyl-derivatives having the general formula: ##STR1## where R is selected from the group of H and CH.sub.3 CO-- and x+y is between 9 and 21; and methods for their synthesis. The compounds of the present invention are synthesized starting with an unsaturated 1-O-alkyl-glycerol of the formula: ##STR2## where R is an unsaturated alkyl group with a chain length of 12 to 24 carbon atoms and introducing a vicinal hydroxyl into the alkyl carbon chain using either osmium tetroxide or performic acid, produced by mixing formic acid with hydrogen peroxide.The new glycerol ether derivatives exert platelet activating factor (PAF)-like action in vitro in low concentrations, and, surprisingly, in higher doses act as selective antagonists of PAF, or 1-O-alkyl-2-O-acetyl-sn-glyceryl-3-phosphorylcholine (AGEPC), activities.

Abstract: Cosmetic Base composition exhibiting therapeutic properties includes an acyl fatty acid lactylate ester or alkali metal salt thereof, a sucrose fatty acid ester, and a solvent.

Abstract: An agent and method for treating vasomotor disorders, particularly migraine and menstrual pain is provided wherein the method comprises administering to said patient, intravenously or orally, an effective dose of the agent according to the invention, Vitamin B.sub.6. The effective dose of vitamin B.sub.6 is at least about 100 mg., preferably at least about 300 mg. and most preferably at least about 400 mg. Vitamin B.sub.2 may also be administered for particularly effective results.

Abstract: The uricosuric and diuretic properties of indacrinone, [6,7-dichloro-2,3-dihydro-2-methyl-1-oxo-2-phenyl-1H-inden-5-yl)oxy]acetic acid, are carefully balanced for maximum therapeutic benefit by manipulation of the proportion of (+) and (-) enantiomers in the final product within critical limits.