The Binding of Agonists to Brain Muscarinic Receptors

The interaction of agonists with muscarinic receptors has been investigated by measuring the binding of [ 3 H]muscarinic agonists to membrane preparations from the rat cortex and by means of [ 3 H]agonist/agonist and [ 3 H]antagonist/agonist competition experiments. The binding data can be explained...

Full description

Saved in:
Bibliographic Details
Published inMolecular pharmacology Vol. 14; no. 5; p. 723
Main Authors Birdsall, N J, Burgen, A S, Hulme, E C
Format Journal Article
LanguageEnglish
Published United States American Society for Pharmacology and Experimental Therapeutics 01.09.1978
Subjects
Animals
Benzilates - pharmacology
Binding, Competitive - drug effects
Brain - metabolism
Cerebral Cortex - metabolism
Drug Interactions
In Vitro Techniques
Kinetics
Membranes - metabolism
Muscle, Smooth - metabolism
Oxotremorine - metabolism
Parasympathomimetics - metabolism
Rats
Receptors, Cholinergic - metabolism
Receptors, Muscarinic - metabolism
Rubidium - metabolism
Online AccessGet full text

Cover

More Information
Summary:The interaction of agonists with muscarinic receptors has been investigated by measuring the binding of [ 3 H]muscarinic agonists to membrane preparations from the rat cortex and by means of [ 3 H]agonist/agonist and [ 3 H]antagonist/agonist competition experiments. The binding data can be explained by the presence of two major populations of agonist binding sites which do not interconvert during the binding experiments and have the same affinity constants for antagonists. The ratio of the affinity constants of an agonist for the two sites can vary from 1 to about 275. There is quantitative agreement between the agonist affinity constants for the two sites and parameters derived from the action of muscarinic agonists on smooth muscle, A third (minor) population of "super-high" affinity agonist binding sites has been detected.
ISSN:0026-895X
1521-0111