色满类化合物HEF-19对家兔离体肠管平滑肌的舒张作用  

Relaxant effect of a chromane HEF-19 on intestinal smooth muscles isolated from rabbits

作　　者：韦元元[1] 付守廷[1] 胡春[2] 朱岚[1] 王冰[1] 汪慧慧[1] 

机构地区：[1]沈阳药科大学生命科学与生物制药学院,辽宁省沈阳市110016 [2]沈阳药科大学制药工程学院,辽宁省沈阳市110016

出　　处：《世界华人消化杂志》2009年第18期1864-1867,共4页World Chinese Journal of Digestology

摘　　要：目的:探讨色满类化合物HEF-19对家兔离体小肠平滑肌的舒张作用及其机制.方法:采用家兔小肠离体实验法,观察HEF-19对家兔离体小肠自发活动的影响,研究BaCl2诱导收缩时格列苯脲(10-5mol/L)、维拉帕米(10-7mol/L)、酚妥拉明(10-7mol/L)和普奈洛尔(10-7mol/L)对HEF-19的舒张作用的影响.结果:HEF-19可以剂量依赖性地降低家兔离体小肠平滑肌自发性收缩的张力和振幅;分别加入格列苯脲和维拉帕米孵育后,HEF-19(10-6mol/L-10-3mol/L)的舒张量效曲线均发生明显变化,EC50值分别由4.36±0.12mol/L和4.43±0.19mol/L转变为4.16±0.22mol/L和3.96±0.24mol/L,差异具有统计学意义(P<0.05).酚妥拉明和普奈洛尔对HEF-19的舒张作用没有影响.结论:HEF-19具有舒张小肠平滑肌的作用并且其作用机制与ATP-敏感性钾通道和L型钙通道开放有关.而与α受体和β受体无关.AIM： To study the relaxant effect of a chromane HEF-19 on isolated small intestinal smooth muscle of rabbits and its underlying mechanism. METHODS： Routine experimental methods using isolated small intestine smooth muscle of rabbits, the effect of HEF-19 on automatic contraction of small intestinal smooth muscle was investigated. The relaxant effects of glibenclamide （10-5 mol/L）, Verapamil （10-7 mol/L） Phentolamine （10-7 mol/L） and Propranolol （10-7 mol/L） on HEF-19 with contraction induced by BaCl2 were studied. RESULTS： HEF-19 significantly attenuated the tension and amplitude of automatic contraction of isolated small intestinal smooth muscle in a dose-dependent manner. The relaxing concentration-response curves of HEF-19 （10-6-10-3 mol/L） were significantly different after incubation with glibenclamide （EC50： 4.16 ± 0.22 mol/L vs 4.36 ± 0.12 mol/L, P 〈 0.05 ）and Verapamil （EC50： 3.96 ± 0.24 mol/L vs 4.43 ± 0.19 mol/L, P 〈 0.05）. Phentolamine and Propranolol had no effect on relaxant effect of HEF-19. CONCLUSION： HEF-19 relaxes isolated small intestinal smooth muscle of rabbits and the mechanism may be related to K＋-ATP opening and L-calcium channel but not related to α- receptor and β- receptor.

关 键 词：家兔 肠管 平滑肌 舒张作用 

分 类 号：R965[医药卫生—药理学]