Effects of verapamil on the binding characteristics of muscarinic receptor subtypes

The calcium channel antagonist verapamil inhibited [3H]N-methyl scopolamine ([3H]NMS ) binding to muscarinic receptors from both rat brain cortex, an area rich in M1 receptors, and from pons-medulla, an area rich in M2 receptors. Verapamil reduced the dissociation kinetics of [3H]NMS binding in cort...

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Bibliographic Details
Published in:	European journal of pharmacology Vol. 126; no. 1-2; p. 151
Main Author:	Baumgold, J
Format:	Journal Article
Language:	English
Published:	Netherlands 15-07-1986
Subjects:	Animals Cerebral Cortex - metabolism In Vitro Techniques Kinetics Male Medulla Oblongata - metabolism Myocardium - metabolism Pirenzepine - metabolism Pons - metabolism Rats Rats, Inbred Strains Receptors, Muscarinic - drug effects Receptors, Muscarinic - metabolism Verapamil - pharmacology
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Summary:	The calcium channel antagonist verapamil inhibited [3H]N-methyl scopolamine ([3H]NMS ) binding to muscarinic receptors from both rat brain cortex, an area rich in M1 receptors, and from pons-medulla, an area rich in M2 receptors. Verapamil reduced the dissociation kinetics of [3H]NMS binding in cortical receptors but had no detectable effects on the dissociation kinetics of receptors from the pons-medulla. These data suggest that receptors from the cortex have an allosteric site which regulates the binding kinetics, whereas receptors from the pons-medulla lack this site.
ISSN:	0014-2999
DOI:	10.1016/0014-2999(86)90752-1