HEF-19-induced relaxation of colonic smooth muscles and the underlying mechanisms

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	HEF-19-induced relaxation of colonic smooth muscles and the underlying mechanisms
其他题名	HEF-19-induced relaxation of colonic smooth muscles and the underlying mechanisms
	Wei YuanYuan 1; Sun LuLu 1; Fu ShouTing 2
	2013
发表期刊	WORLD JOURNAL OF GASTROENTEROLOGY
ISSN	1007-9327
卷号	19 期号:32 页码:5314-5319
摘要	AIM: To investigate the relaxant effect of chromane HEF-19 on colonic smooth muscles isolated from rabbits, and the underlying mechanisms.
其他摘要	AIM:To investigate the relaxant effect of chromane HEF-19 on colonic smooth muscles isolated from rabbits,and the underlying mechanisms.METHODS:The relaxant effect and action mechanisms of HEF-19 were investigated using descending colon smooth muscle of the rabbits.Preparations 1 cm long were mounted in 15-mL tissue baths containing Tyrode’s solution,maintained at 37±0.5℃and aerated with a mixture of 5%CO_2 in oxygen(Carbogen).The tension and amplitude of the smooth muscle strips were recorded after adding HEF-19(10~(-6),10~(-5) and 10~(-4) mol/L).After cumulative administration of four antispasmodic agents,including acetylcholine chloride(Ach)(10~(-4) mol/L),histamine(10~(-4) mol/L),high-K~+(60 mmol/L)and BaCl_2(8.2 mmol/L),HEF-19(3×10~(-7)-3×10~(-4) mol/L)was added to investigate the relaxant effect of HEF-19.CaCl_2(10~(-4)-2.5×10~(-3) mol/L)was added cumulatively to the smooth muscle preparations pretreated with and without HEF-19(1×10~(-6) or 3×10~(-6) mol/L)and verapamil(1×10~(-7) mol/L)to study the mechanisms involved.Finally,phasic contraction was induced with ACh(15×10~(-6) mol/L),and CaCl_2(4×10~(-3)mol/L)was added to the smooth muscle preparations pretreated with and without HEF-19(3×10~(-6)mol/L or 1×10~(-5)mol/L)and verapamil(1×10~(-7)mol/L)in calcium-free medium to further study the underlying mechanisms.RESULTS:HEF-19(1×10~(-6),1×10~(-5) and 1×10~(-4)mol/L)suppressed spontaneous contraction of rabbit colonic smooth muscles.HEF-19(3×10~(-7)-3×10~(-4)mol/L)relaxed in a concentration-dependent manner colonic smooth muscle preparations pre-contracted with BaCl_2,high-K+solution,Ach or histamine with respective EC50values of 5.15±0.05,5.12±0.08,5.58±0.16and 5.25±0.24,thus showing a spasmolytic activity.HEF-19(1×10~(-6)mol/L and 3×10~(-6)mol/L)shifted the concentration-response curves of CaCl_2 to the right and depressed the maximum response to CaCl_2.The two components contracted by Ach were attenuated with HEF-19(3×10~(-6) mol/L or 10~(-5) mol/L)in calcium-free medium.CONCLUSION:HEF-19 inhibited rabbit colonic smooth muscle contraction,probably through inhibiting opening of voltage-dependent Ca~(2+) channels.HEF-19 reduced inflow and intracellular release of Ca~(2+) ions.
关键词	GUINEA-PIG LONGITUDINAL MUSCLE CALCIUM CHANNELS IN-VITRO CONTRACTION ENTRY CA2+ INTESTINE HISTAMINE ILEUM Colonic smooth muscle Smooth muscle relaxation Ca2+ channels
收录类别	CSCD
语种	英语
CSCD记录号	CSCD:5009656
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/149577
专题	中国科学院金属研究所
作者单位	1.Capital Med University, Beijing Shijitan Hosp, Dept Pharm, Beijing 100038, Peoples R China 2.中国科学院金属研究所
推荐引用方式 GB/T 7714	Wei YuanYuan,Sun LuLu,Fu ShouTing. HEF-19-induced relaxation of colonic smooth muscles and the underlying mechanisms[J]. WORLD JOURNAL OF GASTROENTEROLOGY,2013,19(32):5314-5319.
APA	Wei YuanYuan,Sun LuLu,&Fu ShouTing.(2013).HEF-19-induced relaxation of colonic smooth muscles and the underlying mechanisms.WORLD JOURNAL OF GASTROENTEROLOGY,19(32),5314-5319.
MLA	Wei YuanYuan,et al."HEF-19-induced relaxation of colonic smooth muscles and the underlying mechanisms".WORLD JOURNAL OF GASTROENTEROLOGY 19.32(2013):5314-5319.