In vitro characterization of .ALPHA.-adrenergic receptor in rabbit detrusor muscle.
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概要
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In the isolated detrusor smooth muscle of the rabbit urinary bladder, acetylcholine, prostaglandin (PG) F<SUB>2α</SUB>, histamine and methoxamine produced dose-dependent contractions. The order of efficacy was acetylcholine>PGF<SUB>2α</SUB>>histamine>methoxamine. Acetylcholine and oxotremorine increased tension remarkably in the rabbit detrusor muscle; and McN-A-343 also developed tension, but with weaker sensitivity and efficacy. The contractile response to acetylcholine was competitively antagonized by atropine (pA<SUB>2</SUB> 9.24) and pirenzepine (pA<SUB>2</SUB> 6.96), respectively. Histamine and 2-pyridylethylamine caused dose-dependent contractions. On the other hand, dimaprit caused no response in this tissue. Mepyramine (pA<SUB>2</SUB> 8.80) competitively antagonized the contraction induced by histamine, whereas cimetidine failed to antagonize the contraction even at a high concentration of 10-5 M. Norepinephrine, phenylephrine and methoxamine have greater efficacies in the ability to contract than clonidine. R(-)- and S(+)-YM-12617 and YM-12617 (pA<SUB>2</SUB> 10.4, 8.31 and 9.75, respectively) and prazosin (pA<SUB>2</SUB> 8.13), phentolamine (pA<SUB>2</SUB> 7.55) and yohimbine (pA<SUB>2</SUB> 6.44) competitively an tagonized the contraction elicited by methoxamine. These results suggest that the contraction of rabbit detrusor muscle can be mediated by α<SUB>1</SUB>-adrenergic receptors as well as M<SUB>2</SUB>-muscarinic and H<SUB>1</SUB>-histaminergic receptors and suggest that the contractile force mediated by α<SUB>1</SUB>-adrenergic receptor agonist is smaller than those stimulated by the other receptor agonists.
著者
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HONDA Kazuo
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo
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NAKAGAWA Chieko
Department of Pharmacology, Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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HONDA Kazuo
Department of Pharmacology, Medicinal Research Laboratories, Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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MOMOSE Noriko
Department of Pharmacology, Medicinal Research Laboratories, Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.
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