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Molecular Pharmacology, Vol 14, 723-736, Copyright © 1978 by the American Society for Pharmacology and Experimental Therapeutics
1 Division of Molecular Pharmacology, National Institute for Medical Research, Mill Hill,
London NW7 1AA, UK
The interaction of agonists with muscarinic receptors has been investigated by measuring the binding of [3H]muscarinic agonists to membrane preparations from the rat cortex and by means of [3H]agonist/agonist and [3H]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.
Note:
ACKNOWLEDGMENTS
The authors wish to thank P. Mehta and R. Edees
for skilled technical assistance and Drs. C. R. Hiley
and J. M. Young for their permission to include some
of their unpublished results in Table 7.
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