Anticholinergic action of disopyramide in intestinal smooth muscle of the guinea pig: Inhibition of muscarinic receptors (M1 and M2).
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概要
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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; pA<SUB>2</SUB> values were 5.4 for acetylcholine, 5.5 for McN-A343 and 5.9 for carbachol. In the guinea pig ileum, disopyramide competitively antagonized acetylcholine in the contractile responses, having the pA<SUB>2</SUB> value of 6.1. In microsomal fractions of the guinea pig taenia caecum and heart, disopyramide was capable of replacing <SUP>3</SUP>H-QNB; K<SUB>i</SUB> values were 7×10<SUP>-6</SUP> M for the taenia and 2×10<SUP>-6</SUP> M for the heart. These results suggest that disopyramide exerts antimuscarinic action through M<SUB>1</SUB> and M<SUB>2</SUB> receptors with a potency approximately 3 times greater for M<SUB>2</SUB> than M<SUB>1</SUB>.
- 公益社団法人 日本薬理学会の論文
著者
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Shibata Shoji
Department Of Pharmacology School Of Medicine University Of Hawaii
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Fujiwara Motohatsu
Department Of Pharmacology Faculty Of Medicine Kyoto University
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ISHIDA Yukisato
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo
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SATAKE Nobuhiro
Deparrment of Pharmacology, School of Medicine, University of Hawaii
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Taniguchi Takashi
Department of Biology, Kyoto Pharmaceutical University
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MIZUKAMI Masami
Deparrment of Pharmacology, School of Medicine, University of Hawaii
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