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Molecular Pharmacology, Vol 14, 737-750, Copyright © 1978 by the American Society for Pharmacology and Experimental Therapeutics

The Binding of Antagonists to Brain Muscarinic Receptors

E. C. HULME 1, N. J. M. BIRDSALL 1, A. S. V. BURGEN 1, and P. MEHTA 1

1 Division of Molecular Pharmacology, National Institute for Medical Research, Mill Hill, London NW7 1AA

The equilibrium binding of muscarinic antagonists to a crude synaptosome fraction from rat cerebral cortex obeys the simple Langmuir isotherm. The affinity constants measured range from 105 to 1010 M-1 and in all cases agree within a factor of 3 with the corresponding values derived from measurements of anticholinergic potency on smooth muscle. The methodology which must be applied to obtain valid measurements of affinity constants from in vitro studies using radiolabelled ligands is discussed.

Note:
ACKNOWLEDGMENTS The authors wish to express their thanks to Dr. R. B. Barlow for measurement of the antimuscarinic potency of PrBCh, and for the gift of the following compounds: N-methyl-piperidin-3-yl-phenylacetate methiodide; N-methyl-piperidin-4-yl-phenylacetate methiodide; N-methyl-piperidin-4-yl-diphenylacetate methiodide; N-methyl-quinuclidin-3-yl-phenylacetate; N-methyl-quinuclidin-3-yl-diphenylacetate.

Submitted on December 9, 1977
Accepted on April 24, 1978




This article has been cited by other articles:


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