Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro

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	Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro
	Yuan, YM; Yang, HH; Hu, GY
刊名	ACTA PHARMACOLOGICA SINICA
	1998-09
卷号	19 期号:5 页码:451-455
关键词	serotonin receptors tetraethylammonium compounds 4-aminopyridine ileum myenteric plexus carbachol serotonin agonists serotonin antagonists radioligand assay
ISSN号	0253-9756
文献子类	Article
英文摘要	AIM: To study the effects of tetraethylammonium (TEA) and 4-aminopyridine (4-AP) on 5-HT3 receptor-mediated contractions of the isolated guinea pig ileum longitudinal muscle-myenteric plexus strip preparations (GPI). METHODS: GPI contractions were recorded with a chart recorder through isometric transducers. The effect of TEA and 4-AP on binding properties of 5-HT3 receptors was assessed using [H-3]GR65630 binding assay in membrane preparation of rat entorhinal cortex. RESULTS: (1) Both TEA 0.5 mmol . L-1 and 4-AP 5 mu mol . L-1 increased the spontaneous activity, and elicited contractions of GPI; atropine 10 mu mol . L-1 or the selective 5-HT3 receptor antagonist MDL72222 100 mu mol . L-1 prevented these effects. (2) Both TEA 0.05 - 0.5 mmol . L-1 and 4-AP 1-10 mu mol . L-1 enhanced GPI contractions induced by the selective 5-HT3 receptor agonist 2-methyl-5-HT in concentration-dependent manners. (3) Roth TEA 0.5 mmol . L-1 and 4-AP 5 mu mol . L-1 attenuated the inhibitory effects of the selective 5-HT3 receptor antagonists tropisetron 0.1 mu mol . L-1 and benesetron 1 mu mol . L-1 on 5-HT3 receptor-mediated GPI contractions. (4) Neither TEA 0.1 - 0.5 mmol . L-1 nor 4-AP 5 10 mu mol . L-1 affected GPI contractions evoked by the selective M-ACh receptor agonist carbachol 1 mu mol . L-1. (5) TEA 0.5 mmol . L-1 and 4-AP 10 mu mol . L-1 had no effect on the properties of binding of the selective 5-HT3 receptor radioligand [H-3]GR65630 to 5-HT3 receptors. CONCLUSION: The enhancement by TEA and 4-AP of 5-HT3 receptor-mediated GPI contractile responses was due to blocking K+ channels in prejunctional myenteric neurons.
WOS关键词	RELEASE ; ACETYLCHOLINE ; CHANNELS ; CELLS
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
语种	英语
出版者	ACTA PHARMACOLOGICA SINICA
WOS记录号	WOS:000075784800014
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/274808]
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,Yang, HH,Hu, GY. Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro[J]. ACTA PHARMACOLOGICA SINICA,1998,19(5):451-455.
APA	Yuan, YM,Yang, HH,&Hu, GY.(1998).Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro.ACTA PHARMACOLOGICA SINICA,19(5),451-455.
MLA	Yuan, YM,et al."Tetraethylammonium and 4-aminopyridine enhancement of 5-HT3 receptor-mediated contraction of guinea pig ileum in vitro".ACTA PHARMACOLOGICA SINICA 19.5(1998):451-455.