Accession Number : ADB103280

Title :   Structure-Activity Relationships of Agents Modifying Cholinergic Transmissions.

Descriptive Note : Annual summary rept. no. 2, 1 Sep 83-31 Aug 84,

Corporate Author : IOWA UNIV IOWA CITY

Personal Author(s) : Long, J. P. ; Bhatnagar, R. K. ; Cannon, J. G.

Report Date : 01 SEP 1984

Pagination or Media Count : 47

Abstract : Structure activity relationship studies of hemicholinium (HC-3) analogs are directed toward better understanding both the spatial aspect of the receptor and interatomic distances between the 2 cationic heads. Two series of compounds involving 4,4' biphenyl and trans-cyclohexyl derivatives are being investigated and both series are potent inhibitors of acetylcholine synthesis. One compound, N-methyl 4-methyl piperdine derivative in the biphenyl series, is a very active inhibitor of ACh synthesis. The tertiary amine analog is an active inhibitor of synthesis of acetylcholine. It is much less active than the quaternary derivative.

Descriptors :   *ANTIDOTES, *CHOLINESTERASE INHIBITORS, *NERVE BLOCKING, ACETYLCHOLINE, ANALOGS, BIOASSAY, CHOLINERGIC NERVES, DESENSITIZING, HIGH RESOLUTION, IN VITRO ANALYSIS, INCUBATION, LIQUID CHROMATOGRAPHY, NEUROMUSCULAR TRANSMISSION, AMINES, CATIONS, SYNAPSE, PHRENIC NERVES, RATS, RABBITS.

Subject Categories : Pharmacology

Distribution Statement : APPROVED FOR PUBLIC RELEASE