Muscarinic cholinoceptors in the rabbit's myometrium: a study of the relationship between binding and response

• Published in: European journal of pharmacology Vol. 101; no. 1-2; p. 1
• Main Author: Crankshaw, D J
• Format: Journal Article
• Language: English
• Published: Netherlands 18-05-1984
• Subjects: Animals; Binding, Competitive; Female; In Vitro Techniques; Kinetics; Myometrium - metabolism; Parasympatholytics - metabolism; Parasympatholytics - pharmacology; Parasympathomimetics - metabolism; Parasympathomimetics - pharmacology; Quinuclidinyl Benzilate; Rabbits; Receptors, Muscarinic - metabolism; Stereoisomerism; Uterine Contraction - drug effects
• ISSN: 0014-2999
• DOI: 10.1016/0014-2999(84)90024-4

The relationship between [3H](-)-quinuclinidyl benzilate [( 3H](-)QNB) binding and muscarinic cholinoceptors in the myometrium of the oestrogen treated rabbit was studied. [3H](-)QNB binding was specific, saturable and reversible. The ability of muscarinic agonists and antagonists and some of their stereoisomers to inhibit [3H](-)QNB binding and to stimulate or inhibit contraction of the myometrium were almost identical suggesting that [3H](-)QNB binds specifically to the muscarinic cholinoceptor in this tissue. There appeared to be no receptor reserve in this tissue and whilst structural and stereospecific requirements for binding were almost identical to those for the muscarinic cholinoceptor in the guinea pig ileum requirements for activation were not. Competition binding experiments with pirenzepine suggested that antagonist binding sites were heterogeneous whilst those with 4-diphenylacetoxy-N-methyl-piperidine MeBr did not. Results were discussed with regard to simple and complex models of muscarinic cholinoceptor interactions.