Anticholinergic action of disopyramide in intestinal smooth muscle of the guinea pig: inhibition of muscarinic receptors (M1 and M2).

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Ishida Y, Mizukami M, Taniguchi T, Satake N, Fujiwara M, Shibata S

Anticholinergic action of disopyramide in intestinal smooth muscle of the guinea pig: inhibition of muscarinic receptors (M1 and M2).

Jpn J Pharmacol. 1990 Feb;52(2):363-70.

PubMed ID

1690310 [ View in PubMed

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Abstract

Antimuscarinic actions of disopyramide were investigated by measuring the contractile responses of intestinal smooth muscles and ligand binding in cardiac and intestinal membrane preparations. Disopyramide caused a parallel shift of the dose-response curves for acetylcholine, McN-A-343, and carbachol to the right in the guinea pig taenia caeci; pA2 values were 5.4 for acetylcholine, 5.5 for McN-A-343 and 5.9 for carbachol. In the guinea pig ileum, disopyramide competitively antagonized acetylcholine in the contractile responses, having the pA2 value of 6.1. In microsomal fractions of the guinea pig taenia caecum and heart, disopyramide was capable of replacing 3H-QNB; K1 values were 7 x 10(-6) M for the taenia and 2 x 10(-6) M for the heart. These results suggest that disopyramide exerts antimuscarinic action through M1 and M2 receptors with a potency approximately 3 times greater for M2 than M1.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Disopyramide	Muscarinic acetylcholine receptor M1	Protein	Humans	Unknown	Antagonist	Details
Disopyramide	Muscarinic acetylcholine receptor M2	Protein	Humans	Unknown	Antagonist	Details