The Binding of Antagonists to Brain Muscarinic Receptors

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 10 5 to 10 10 M -1 and in all cases agree within a factor of 3 with the corresponding values derived from measurem...

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Published inMolecular pharmacology Vol. 14; no. 5; pp. 737 - 750
Main Authors Hulme, E C, Birdsall, N J, Burgen, A S, Mehta, P
Format Journal Article
LanguageEnglish
Published United States American Society for Pharmacology and Experimental Therapeutics 01.09.1978
Subjects
Animals
Atropine - metabolism
Benzilates - metabolism
Binding, Competitive
Brain - metabolism
Brain - ultrastructure
In Vitro Techniques
Kinetics
Male
Parasympatholytics - metabolism
Rats
Receptors, Cholinergic - metabolism
Receptors, Muscarinic - metabolism
Scopolamine Hydrobromide - metabolism
Subcellular Fractions - metabolism
Synaptosomes - metabolism
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Summary: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 10 5 to 10 10 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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0026-895X
1521-0111