Pinacidil suppression on 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro

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	Pinacidil suppression on 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro
	Yuan, YM; Xu, DY; Hu, GY
刊名	ACTA PHARMACOLOGICA SINICA
	1998-01
卷号	19 期号:1 页码:31-35
关键词	serotonin receptors pinacidil ileum myenteric plexus carbachol GR65630
ISSN号	0253-9756
文献子类	Article
英文摘要	AIM: To study the effects of the K+ channel opener pinacidil on 5-HT3 receptor-mediated contractions of the isolated guinea pig ileum (GPI) longitudinal muscle-myenteric plexus strip preparations. METHODS: GPI contractions were recorded with a chart recorder through isometric transducers. The effect of pinacidil on binding properties of 5-HT3 receptors was assessed using [H-3] GR65630 binding assay in membrane preparations of rat entorhinal cortex. RESULTS: (1) A selective 5-HT3 receptor agonist 2-methyl-5-HT 0.1-300 mu mol.L-1 and 5-HT 0.001-50 mu mol.L-1 elicited GPI contractile responses in concentration-dependent manners, the EC50 values (and 95 % confidence limits) for 2-methyl-5-HT and 5-HT were 10.0 (8.9-11.2) mu mol.L-1 and 1.6 (1.3-1.9) mu mol.L-1, respectively. Selective 5-HT3 receptor antagonist tropisetron 0.1 mu mol.L-1 competitively inhibited the responses to 2-methyl-5-HT and 5-HT. (2) Pinacidil 0.5-5 mu mol.L-1 inhibited 5-HT3 receptor-mediated contractions. (3) Pinacidil 1 mu mol.L-1 enhanced the inhibitory effects of tropisetron 0.1 mu mol.L-1 or another selective 5-HT3 receptor antagonist benesetron 1 mu mol.L-1 on 5-HT-induced GPI contractile responses. (4) Pinacidil 1-5 mu mol.L-1 did not affect GPI contractile responses evoked by a selective M-ACh receptor agonist carbachol 1 mu mol.L-1. (5) Pinacidil 1-5 mu mol.L-1 had no effect on binding properties of 5-HT3 receptors with selective 5-HT3 receptor radioligand [H-3] GR65630 in the entorhinal cortex of rat brain. CONCLUSION: The inhibition by Pinacidil of 5-HT3 receptor-mediated GPI contractile responses may be mediated through activation of ATP-sensitive K+ channels located in prejunctional myenteric neurons.
WOS关键词	CHANNEL OPENERS ; ACETYLCHOLINE-RELEASE ; LONGITUDINAL MUSCLE ; SMALL-INTESTINE ; SMOOTH-MUSCLE ; CROMAKALIM
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000071424500008
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274867]
专题	药理学第一研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Hu, GY
作者单位	Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200031, Peoples R China
推荐引用方式 GB/T 7714	Yuan, YM,Xu, DY,Hu, GY. Pinacidil suppression on 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro[J]. ACTA PHARMACOLOGICA SINICA,1998,19(1):31-35.
APA	Yuan, YM,Xu, DY,&Hu, GY.(1998).Pinacidil suppression on 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro.ACTA PHARMACOLOGICA SINICA,19(1),31-35.
MLA	Yuan, YM,et al."Pinacidil suppression on 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro".ACTA PHARMACOLOGICA SINICA 19.1(1998):31-35.