Abstract
1. The affinity of the antagonist dicyclomine for subtypes of muscarinic receptors has been assessed in the myenteric plexus-longitudinal muscle preparation of the guinea-pig. 2. Dicyclomine had a high affinity (pA2 9.13) for the neuronal M1-receptor whose activation by pilocarpine causes an increase in acetylcholine release. Dicyclomine had a low affinity for both the prejunctional M2-receptor (pA2 7.61) mediating inhibition of the electrically-evoked acetylcholine release and the postjunctional M2-receptor (pA2 7.21). 3. It is concluded that dicyclomine distinguishes between M1- and M2-muscarinic receptors in functional experiments.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- ARUNLAKSHANA O., SCHILD H. O. Some quantitative uses of drug antagonists. Br J Pharmacol Chemother. 1959 Mar;14(1):48–58. doi: 10.1111/j.1476-5381.1959.tb00928.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Doods H. N., Mathy M. J., Davidesko D., van Charldorp K. J., de Jonge A., van Zwieten P. A. Selectivity of muscarinic antagonists in radioligand and in vivo experiments for the putative M1, M2 and M3 receptors. J Pharmacol Exp Ther. 1987 Jul;242(1):257–262. [PubMed] [Google Scholar]
- Downie J. W., Twiddy D. A., Awad S. A. Antimuscarinic and noncompetitive antagonist properties of dicyclomine hydrochloride in isolated human and rabbit bladder muscle. J Pharmacol Exp Ther. 1977 Jun;201(3):662–668. [PubMed] [Google Scholar]
- Eglen R. M., Whiting R. L. Muscarinic receptor subtypes: a critique of the current classification and a proposal for a working nomenclature. J Auton Pharmacol. 1986 Dec;6(4):323–346. doi: 10.1111/j.1474-8673.1986.tb00661.x. [DOI] [PubMed] [Google Scholar]
- Giachetti A., Giraldo E., Ladinsky H., Montagna E. Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986 Sep;89(1):83–90. doi: 10.1111/j.1476-5381.1986.tb11123.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kilbinger H., Halim S., Lambrecht G., Weiler W., Wessler I. Comparison of affinities of muscarinic antagonists to pre- and postjunctional receptors in the guinea-pig ileum. Eur J Pharmacol. 1984 Aug 17;103(3-4):313–320. doi: 10.1016/0014-2999(84)90492-8. [DOI] [PubMed] [Google Scholar]
- Kilbinger H., Nafziger M. Two types of neuronal muscarine receptors modulating acetylcholine release from guinea-pig myenteric plexus. Naunyn Schmiedebergs Arch Pharmacol. 1985 Jan;328(3):304–309. doi: 10.1007/BF00515558. [DOI] [PubMed] [Google Scholar]
- MCGRATH W. R., LEWIS R. E., KUHN W. L. THE DUAL MODE OF THE ANTISPASMODIC EFFECT OF DICYCLOMINE HYDROCHLORIDE. J Pharmacol Exp Ther. 1964 Dec;146:354–358. [PubMed] [Google Scholar]
- Nilvebrant L., Sparf B. Dicyclomine, benzhexol and oxybutynine distinguish between subclasses of muscarinic binding sites. Eur J Pharmacol. 1986 Apr 9;123(1):133–143. doi: 10.1016/0014-2999(86)90697-7. [DOI] [PubMed] [Google Scholar]
- North R. A., Slack B. E., Surprenant A. Muscarinic M1 and M2 receptors mediate depolarization and presynaptic inhibition in guinea-pig enteric nervous system. J Physiol. 1985 Nov;368:435–452. doi: 10.1113/jphysiol.1985.sp015867. [DOI] [PMC free article] [PubMed] [Google Scholar]