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Muscarinic activity and receptor binding of the enantiomers of aceclidine and its methiodide

B Ringdahl, FJ Ehler and DJ Jenden

The agents (+)- and (-)-aceclidine (3-acetoxyquinuclidine), (+)- and (- )-N-methylaceclidine, and oxotremorine were compared in their ability to inhibit specific 3H-labeled (+/-)-3-quinuclidinyl benzilate binding to rat brain muscarinic receptors and to stimulate contractions of the isolated guinea pig ileum. A good correlation was observed between the high-affinity dissociation constant (KH) for binding and the muscarinic potency in the isolated ileum. The binding data for the enantiomers of aceclidine were also consistent with their central and peripheral pharmacological activity in vivo. Thus the enantiomeric potency ratios [ED50 of (-)-aceclidine/ED50 of (+)-aceclidine] for the tremorogenic, analgesic, and sialogogic effects in mice agreed well with the ratio KH of (-)-aceclidine/KH of (+)-aceclidine.

Volume 21, Issue 3, pp. 594-599, 05/01/1982
Copyright © 1982 by American Society for Pharmacology and Experimental Therapeutics




This article has been cited by other articles:


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A Simple Method for Estimation of Agonist Activity at Receptor Subtypes: Comparison of Native and Cloned M3 Muscarinic Receptors in Guinea Pig Ileum and Transfected Cells
J. Pharmacol. Exp. Ther., May 1, 1999; 289(2): 981 - 992.
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