Article date: June 1982
By: R. DAHLBOM, D.J. JENDEN, B. RESUL, B. RINGDAHL in Volume 76, Issue 2, pages 299-304
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.
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.
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.
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.
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.
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.
DOI: 10.1111/j.1476-5381.1982.tb09220.x
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