Accession Number : ADB112227

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

Descriptive Note : Final rept. 1 Sep 82-30 Nov 86,

Corporate Author : IOWA UNIV IOWA CITY

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

Report Date : 30 NOV 1986

Pagination or Media Count : 70

Abstract : Structure activity relationship studies of hemicholinium (HC-3) analogs directed toward better understanding both the spatial aspect of the receptor and interatomic distances between the 2 cationic heads. Several series of compounds including 4,4' biphenyl and trans/trans-cyclohexyl derivatives are being investigated and both series are potent inhibitors of acetylcholine synthesis. One compound, N-methyl 4-methyl piperidine 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. Keywords: Cholinesterase inhibitors; Transport properties.

Descriptors :   *CHOLINESTERASE INHIBITORS, ACETYLCHOLINE, CHOLINERGIC NERVES, INHIBITORS, POTENCY, SPATIAL DISTRIBUTION, TRANSPORT PROPERTIES, SYNTHESIS, BIPHENYL, CHEMICAL DERIVATIVES, QUATERNARY COMPOUNDS, MOLECULAR STRUCTURE, NEUROCHEMICAL TRANSMISSION, NEUROCHEMISTRY.

Subject Categories : Pharmacology

Distribution Statement : APPROVED FOR PUBLIC RELEASE