Pharmacological Characterization of 5-Hydroxytryptamine-Receptor Subtypes in Circular Muscle from the Rat Stomach(Pharmacology)
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概要
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5-Hydroxytryptamine (5-HT) modulates gastric motility and gastric emptying via a variety of 5-HT receptor subtypes. However, regional and functional differences among 5-HT receptor subtypes in the rat stomach are not fully investigated. Thus, we aimed to characterize 5-HT receptor subtypes involved in the 5-HT-induced contractions in the isolated antral, corporal and fundic circular muscles of the rat stomach by measuring the contractile force. 5-HT induced concentration-dependent contractions in the antrum, corpus and fundus. 5-HT-induced antral contractions were partly blocked by atropine and enhanced by tetrodotoxin (TTX). Neither atropine nor TTX affected the corporal or the fundic contractions to 5-HT. In the antrum, 5-HT-induced contractions were inhibited by methysergide, tended to be inhibited by ketanserin, enhanced by SB-203186, but were not affected by WAY-100635, GR127935, RS-127445, ondansetron, or SB-269970. In the corpus, 5-HT-induced contractions were inhibited by ketanserin or methysergide. In the fundus, 5-HT-induced contractions were blocked by methysergide or RS-127445, but were enhanced by cinanserin or SB-203186. It is thus concluded that contractile responses to 5-HT in the antrum are mediated by 5-HT receptors on both smooth muscle and neurons whilst in the corpus and fundus responses are mainly mediated by 5-HT receptors on smooth muscle. Moreover, the antrum presents the contractile 5-HT_<2A> and 5-HT_<2B> receptors and the relaxant 5-HT_4 receptors. The corpus presents the contractile 5-HT_<2A> receptors, and the fundus presents the contractile 5-HT_<2B> receptors and the relaxant 5-HT_<2A> and 5-HT_4 receptors.
- 公益社団法人日本薬学会の論文
- 2007-03-01
著者
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Yano Shingo
Laboratory Of Molecular Pharmacology & Pharmacotherapeutics Graduate School Of Pharmaceutical Sc
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KOMADA Tohru
Discovery Biology Research, Global Research & Development, Nagoya Laboratories, Pfizer Japan Inc.
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Komada Tohru
Discovery Biology Research Global Research & Development Nagoya Laboratories Pfizer Japan Inc.:l
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YANO Shingo
Laboratory of Chemical Pharmacology, Department of Drug Evaluation and Toxicological Sciences, Faculty of Pharmaceutical Sciences, Chiba University
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