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STEREOCHEMICAL REQUIREMENTS FOR CENTRAL AND PERIPHERAL MUSCARINIC AND ANTIMUSCARINIC ACTIVITY OF SOME ACETYLENIC COMPOUNDS RELATED TO OXOTREMORINE
Author(s) -
DAHLBOM R.,
JENDEN D.J.,
RESUL B.,
RINGDAHL B.
Publication year - 1982
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1982.tb09220.x
Subject(s) - oxotremorine , muscarinic acetylcholine receptor , chemistry , muscarinic agonist , agonist , muscarinic acetylcholine receptor m1 , pharmacology , muscarinic acetylcholine receptor m2 , muscarinic acetylcholine receptor m3 , enantiomer , in vivo , stereochemistry , muscarinic acetylcholine receptor m4 , partial agonist , receptor , endocrinology , biochemistry , biology , microbiology and biotechnology
1 The enantiomers of some analogues of the central muscarinic agent, oxotremorine, were prepared and investigated for tremorogenic and tremorolytic activity in intact mice and for muscarinic and antimuscarinic activity on the isolated ileum of the guinea‐pig. 2 The R‐isomers were more potent than the S‐isomers both in vivo and in vitro regardless of whether the compounds are agonists, partial agonists or competitive antagonists. 3 It is suggested that in the oxotremorine series, agonists and antagonists interact with a common receptor site, in contrast to classical muscarinic antagonists which are believed to bind also to accessory receptor areas, located close to the agonist binding site.