Abstract: This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D.sub.2 receptors without appreciably activating postsynaptic dopamine receptors which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting essentially of the stereoisomers of mixtures thereof of compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of pyridyl and ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3, R.sub.2 is H, R.sub.

Abstract: Certain novel compounds having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.

Abstract: Certain novel compounds having the structural formula ##STR1## wherein R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of hydrocarbyl radicals, e.g. lower alkyl radicals, i.e. methyl, ethyl, propyl, etc., or ##STR2## wherein R.sub.5 is selected from the group consisting of hydrocarbyl radicals, e.g. alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of organic radicals having fused aromatic rings, that is, radicals comprising at least two rings that share a pair of carbon atoms or share a carbon and nitrogen atom are useful for inducing a dopaminergic response and reducing the intraocular pressure in a mammal.

Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.

Abstract: The present invention relates generally to compounds having melatonin receptor activities and in particular to substituted 2-amidotetralin derivatives; to pharmaceutical preparations comprising such compounds; and to methods for using these compounds as therapeutic and diagnostic reagents.

Abstract: This invention provides a method for treating the symptoms of parkinsonism which comprises administering to a human or other mammal suffering from the symptoms of parkinsonism an effective amount of a compound selected from the group consisting of optically-active or racemic compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of organic radicals methyl, substituted or unsubstituted phenyls, pyridyl, hydroxphenyl, ##STR2## X is oxygen or sulfur, Y is selected from the group consisting of hydroxy, nitro, cyano, axido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3,R.sub.2, R.sub.3 and R.sub.

Abstract: Abnormalitites in the distribution of a dopamine D.sub.2 receptors in humans and other mammals are detected by(1) administering to a human or other mammal an amount of a .sup.18 F-radiolabelled compound sufficient to be detected by a positron emission sensitive means for imaging, said compound having affinity for said receptors selected from the group consisting of optically active or racemic compounds represented by the general formula: ##STR1## (2) forming at least one image showing the distribution of the radiolabelled compound within the human or other mammal using a positron emission-sensitive means for imaging; and(3) determining normality of the concentrations or distribution by comparing the image with an image showing the normal concentrations and distribution of the receptors in humans or mammals of the same species wherein R1-R4, n and m- are as set forth in the specification.

Abstract: This invention provides a method for treating the symptoms of parkinsonism which comprises administering to a human or other mammal suffering from the symptoms of parkinsonism an effective amount of a compound selected from the group consisting of optically-active or racemic compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of organic radicals methyl, substituted or unsubstituted phenyls, pyridyl, hydroxyphenyl, ##STR2## X is oxygen or sulfur, Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms. and a is an integer of from zero to 3,R.sub.2, R.sub.3 and R.sub.

Abstract: This invention provides a method for treating the symptoms of schizophrenia which comprises administering to a schizophrenic an effective amount of a compound selected from the group consisting of optically-active or racemic compounds represented by the general formula: ##STR1## wherein R.sub.1 is selected from the group consisting of organic radicals having fused rings, phenyl, pyridyl ##STR2## X is oxygen or sulfur, Y, if present, is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer between zero and 3. R.sub.2, R.sub.3 and R.sub.

Abstract: Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is selected from the group consisting of hydrocarbyl radicals; ##STR2## where X is S or O: and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.

Abstract: The invention provides compounds represented by the general formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is H or ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting ##STR3## wherein R.sub.6 is selected from the group consisting of halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl, comprising from 1 to 12 carbon atoms and wherein said hetero-atoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus; R.sub.7 is R.sub.6 or H and m equals 1, 2 or 3; with the proviso that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that at least one of R.sub.2, R.sub.3 and R.sub.4 is not H and that R.sub.2 and R.sub.4 are not both OA; and pharmaceutically-acceptable salts thereof. The compounds are dopamine receptor agonists and useful for the treatment of glaucoma in mammals.

Abstract: This invention provides a method for reducing the intraocular pressure in mammals which comprises administering an effective amount of a compound selected from the group consisting of compounds represented by the general formula: ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is H or ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of 3-hydroxyphenyl, 4-hydroxyphenyl, 3-pyridyl, 4-pyridyl, ##STR3## where X is S, O or NH, with the proviso that at least one of R.sub.2, R.sub.3 and R.sub.4 is H, that at least one of R.sub.2, R.sub.3 and R.sub.4 is not H and that R.sub.2 and R.sub.4 are not both OA; and pharmaceutically-acceptable salts thereof. This invention further provides compositions useful in such method of reducing the intraocular pressure in mammals.

Abstract: Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is H or ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of 3-hydroxyphenyl, 4-hydroxyphenyl, 3-pyridyl, 4-pyridyl, ##STR3## where X is S, O or NH; and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.

Abstract: A method for inducing an anticurare response by administering 2,4-diaminopyridine to a mammal is disclosed, together with pharmaceutical compositions containing an effective amount of 2,4-diaminopyridine either alone or in combination with an anticholinesterase agent. 2,4-Diaminopyridine is an antagonist of muscle relaxants used in anesthesiology and can increase neuromuscular transmission in certain disease states.

Abstract: Compounds are disclosed having the formula: ##STR1## wherein: R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR2## R.sub.2 is H, --CH.sub.3, or ##STR3## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl; R.sub.4 is H, --CH.sub.3, --CH.sub.2 OH, --CH.sub.2 --CN, --CH.sub.2 --S--Me, CH.sub.2 --S--CN, or ##STR4## R.sub.5 is H, 1-4 carbon alkyl, alkenyl, or alkynyl, or aralkyl having a 1-4 carbon alkylene moiety; and A is --CH.sub.2 --or --CH.sub.2 CH.sub.2 --, and pharmaceutically-acceptable salts thereof. Pharmaceutical preparations using these compounds and a method for inducing a dopaminergic response by administering these compounds are also disclosed.

Abstract: A method of selectively stimulating D-2 dopamine receptors in humans comprising administering to a human requiring D-2 dopamine receptor stimulation, a therapeutically effective amount of 2-(N-phenylethyl-N-propylamino)-5-hydroxytetralin or a pharmaceutically acceptable salt thereof.