Abstract: A method of training a smoker to cease smoking by administering tropane compounds is provided.

Abstract: The present application relates to novel opioid receptor antagonists and agonists, methods of making these compounds, and methods of use thereof.

Abstract: The 3&agr; isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a more rapid achievement of apparent equilibrium in the striatal-to-cerebellar ratio (compared to RTI-55) as the ratio peaks at about 30 min and is maintained for about 20 min thereafter. Such apparent equilibrium is useful in developing an approach to measuring the number of dopamine transporters present in tissues. Moreover, these results indicate that the utilization of 3&agr; isomers of a variety of 3&bgr;-(substituted phenyl)tropanes will result in greater selectivity for dopamine transporters and a more rapid of achievement of apparent equilibrium.

Abstract: The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases or in determining the doses of therapeutic agents that occupy significant numbers of receptors.

Abstract: The invention relates to a method of controlling an invertebrate pest, comprising contacting the pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a phenylethanolamine reuptake transporter as determined by radioactive octopamine reuptake inhibition assay is disclosed. Compositions comprising compounds capable of inhibiting the octopamine reuptake transporter include cocaine analogs. A process for inhibiting the feeding of an invertebrate pest comprising contacting said pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a phenylethanolamine reuptake transporter as determined by radioactive octopamine reuptake inhibition assay, with the proviso that said agent is not cocaine. A process for delaying the maturation of a juvenile invertebrate by contacting it with an inhibitory amount of a phenylethanolamine reuptake transporter blocker is also disclosed.

Abstract: The present invention provides a compound having the structure: ##STR1## wherein X, Y, and Z are independently H, Cl, Br, F, OCH.sub.3, I, or an alkyl group having 1 to 6 carbon atoms; and R is ##STR2## wherein n is 0 to 6, X' and Y' are independently H, Cl, F, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, OCH.sub.3, OH, CF.sub.3, OCF.sub.3, NO.sub.2, NH.sub.2, N(CH.sub.3).sub.2, NHCOCH.sub.3, NCS, NHCOCH.sub.2 Br, or N.sub.3, and (CH.sub.2).sub.n, if present, may be substituted with OH, OCH.sub.3, or an alkyl or alkenyl group having 1 to 3 carbon atoms. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present invention further provides a method for treating a disease characterized by a dopamine deficiency which comprises administering to a subject in need of such treatment an amount of the pharmaceutical composition above effective to treat the disease.

Abstract: Novel compounds useful as intermediates in the synthesis of compounds having high affinity for specific cocaine receptors in the brain have the formula ##STR1## wherein R is (CH.sub.2).sub.n CH.sub.2 Y, and wherein Y is H or F, X is a pharmaceutically acceptable anion, andwherein Sn (R.sup.1, R.sup.2, R.sup.3) is ortho, meta or para and wherein R.sup.1, R.sup.2, R.sup.3 are independently alkyl of 1-6 carbon atoms and n is an integer of 0-5.

Abstract: Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CONRR.sub.2, R.sub.1 =hydrogen, C.sub.1-5 alkyl,X=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido,R and R.sup.2 may be saturated or unsaturated substituents of 1-6 carbon atoms, aromatic, or combine to form pyrrolidinyl, morpholinyl or piperidinyl moieties, andZ=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl, NR.sub.4 R.sub.5, NHCOF.sub.5, NHCO.sub.2 R.sub.6,wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.

Abstract: 3.beta.-[4-iodophenyl]-tropan-2.beta.-carboxylic acid methyl ester tartrate is a high affinity binding ligand for cocaine receptors in mammalian brains. It and its congeners may be employed for imaging and other brain scanning techniques that allow the determination of the presence of cocaine receptors, such as dopamine and serotonin transporters and the like.

Abstract: Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CH.sub.2 R.sub.3, CO.sub.2 R.sub.2 or ##STR2## R.sub.1 =hydrogen, C.sub.1-5 alkyl, R.sub.2 =hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen or amine,R.sub.3 =OH, hydrogen, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, Cl Br, I, CN, NH.sub.2, NHC.sub.1-6 alkyl, NC.sub.1-6 alkyl, OCOC.sub.1-6 alkyl, OCOC.sub.1-3 alkylaryl,A=S, 0 or NHX=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido, andZ=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl , NR.sub.4 R.sub.5, NHCOR.sub.5, NHCO.sub.2 R.sub.6,wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.

Abstract: Substituted phosphorothioate derivatives and pharmaceutical compositions thereof as potential antiradiation agents are disclosed.

Abstract: 3.beta.-[4-iodophenyl]-tropan-2.beta.-carboxylic acid methyl ester tartrate is a high affinity binding ligand for neurotransmitters in mammalian brains. It and its congeners may be employed for imaging and other brain scanning techniques that allow the determination of the presence of cocaine receptors, such as neurotransmitters and the like.

Abstract: This invention relates to novel compositions, their preparation and the use thereof as anticholinergic agents in the treatment or prophylaxis of organophosphate or nerve gas poisoning in animals. These compositions and pharmaceutical preparations containing them in their free base form and acid addition salts thereof are represented by the formula ##STR1## wherein R represents lower alkyl groups containing 1 to 7 carbon atoms; R.sup.1 represents hydrogen, phenyl, cyclohexyl, and cyclopentyl; and R.sup.2 represents lower alkyl groups containing 1 to 7 carbon atoms, hydroxymethyl, and hydroxyl.

Abstract: A group of retinoids having "vitamin A type" activity which have the structure ##STR1## wherein R3 is a trimethylcyclohexenylethylene, tetramethyltetrahydronaphthalene or methoxytrimethylphenylethylene group;R1 and R2 which are different are selected from --OH, --OR4 and --NHR, provided one of R1 and R2 is OH; R4 is alkyl of 1 to 20 carbons; and R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, hydroxyalkyl of 1 to 4 carbons, alkylhydroxyalkyl of 1 to 4 carbons, phenyl, hydroxyphenyl and carboxyphenyl, and R5 is a lactone or lactam of the structure ##STR2## and X is oxygen or NR where R is as above, and the pharmaceutically acceptable salts thereof.

Abstract: 1,4-Bis(2,4,6-trialkylanilino)anthraquinone wherein the alkyls on each anilino group are selected from the group consisting of methyl and ethyl and one of the three alkyls on each anilino group is different from the other two, e.g. 1,4-bis(2,6-diethyl-4-methylanilino)anthraquinone, is disclosed as an unusually effective blue dye suitable for use as a visual leak indicator in halocarbon refrigerants or in refrigeration liquids comprising a halocarbon refrigerant in admixture with a refrigeration oil.

Abstract: Compounds of the class represented by 1,4-bis(2-methyl-6-ethylanilino)anthraquinone, 1,4-bis(2,6-dimethylanilino)anthraquinone, and 1,4-bis(2,4,6-trimethylanilino)anthraquinone are disclosed as being unusually stable blue dyes suitable for use as visual leak indicators in refrigerants; e.g., in halocarbon refrigerants, or in refrigeration liquids comprising a halocarbon refrigerant in admixture with a refrigeration oil.