摘要
目的：研究HEF-05对家兔离体小肠平滑肌的作用及其机制。方法：采用常规离体小肠平滑肌实验方法。结果：HEF-05（3.0×10^-6,3.0×10^-5,3.0×10^-4mol·L^-1）可剂量依赖性地降低小肠平滑肌自主收缩的张力和振幅;经格列苯脲阻断后,HEF-05（10^-6-10^-3mol·L^-1）对氯化钡和高钾液诱导收缩的舒张量效曲线均发生明显变化,舒张作用被抑制;而经普萘洛尔和吲哚美辛阻断后,量效曲线均无明显变化;经维拉帕米阻断后,只有氯化钡诱导收缩的舒张量效曲线发生变化。结论：HEF-05具有舒张小肠平滑肌的作用,其机制与ATP-敏感性钾通道的开放有关,与β受体和前列腺素无关,可能与L型钙通道有关。
Objective： To investigate the effect of HEF-05,a chromane,in smooth muscles of rabbit small intestine and the mechanism.Methods： The smooth muscles of small intestine were isolated from rabbits by routine experiment methods.Results： HEF-05（3.0×10^-6,3.0×10^-5,3.0×10^-4 mol·L^-1） reduced the tension and amplitude of spontaneous contraction in a concentration-dependent manner.After incubation with glibenclamide,the concentration-response curves of relaxation by HEF-05（10-6-10^-3 mol·L^-1） significantly changed,and the relaxant effect of HEF-05 on BaCl2-or KCl-induced contraction was inhibited.However,propranolol and indomethacin did not apparently change the HEF-05 concentration-response curves.Verapamil only significantly altered the relaxant effect of HEF-05 on BaCl2-induced contraction.Conclusion： The relaxant effect of HEF-05 in smooth muscles of small intestine relates to the opening of ATP-sensitive K＋ channel（K＋-ATP） and probably to L-calcium channel,but not to β-receptor and prostaglandins.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2010年第16期1459-1462,共4页
Chinese Journal of New Drugs
