雌酚酮衍生物EA303对家兔离体血管平滑肌的舒张作用  

Relaxant effect of an estrone derivate EA303 on isolated aorta smooth muscle of rabbits

作　　者：张腾[1] 魏巍 付守廷[1] 陈国良[3] 

机构地区：[1]沈阳药科大学生命科学与生物制药学院,辽宁沈阳110016 [2]天津生物工程职业技术学院,天津300462 [3]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《安徽医药》2011年第12期1477-1479,共3页Anhui Medical and Pharmaceutical Journal

摘　　要：目的研究雌酚酮衍生物EA303对家兔离体血管平滑肌的作用及其机制。方法家兔离体主动脉条为标本,观察EA303对去甲肾上腺素(NE)、高钾液(KCl)引起的主动脉条收缩的影响;对氯化钙(CaCl2)累积收缩量效曲线的影响,并与维拉帕米(Ver)累积收缩量效曲线相比较。通过对比钾通道阻断剂格列苯脲孵育前后EA303对KCl、NE的舒张量效曲线,研究EA303对ATP敏感性钾通道的作用。结果 EA303(3×10-5～10-3mol·L-1可以剂量依赖性地抑制NE、KCl引起的兔主动脉条的收缩;EA303(10-5mol·L-1)使CaCl2累积收缩量效曲线呈剂量依赖性右移,这与Ver(10-7mol·L-1)进行孵育的结果十分相似;加入格列苯脲(10-5mol·L-1)孵育,EA303舒张KCl、NE引起收缩的量效曲线发生与未孵育相比变化明显,格列苯脲抑制了EA303对KCl、NE引起的舒张作用。结论 EA303具有舒张家兔离体血管平滑肌的作用,其作用机制与阻断钾通道和以抑制内钙释放的方式阻断钙通道有关。Aim To study the effect and mechanism of estrone EA303 on isolated ascular smooth muscle of rabbits.Methods we investigated the effect of EA303 on the isolate aorta contracted by noradrenalin（NE）,high-K＋ solution and CaCl2.Moreover,the activity of EA303 was investigated by comparing with verapamil,a well-known calcium antagonist.To assess whether the spasmolytic activity of EA303 was through ATP-sensitive potassium channels blockade,the smooth muscle preparations from rabbits were exposed to glibenclamide（10^-5mol·L^-1） and the effects on the preparations contracted by KCl and NE were observed.Results In concentration between 3×10^-5 and 3.0×10^-3mol·L^-1,EA303 concentration dependently relaxed NE and high-K＋ induced contractions.At the concentration of 1.0×10^-5mol·L^-1,EA303 caused a dose-dependent rightward shift in the Ca2＋ dose-response curve which was similar to verapamil.When exposed to glibenclamide,the relaxing effect of EA303 on the preparation contracted by KCl,NE was obviously inhibited.Conclusion EA303 has the effect of relaxing the isolated ascular smooth muscle of rabbits and it seems that EA303 may act on smooth muscle as a K＋ channel blocker and inhibiter of calcium release from calcium store.

关 键 词：家兔 雌酚酮 主动脉条 钙通道 钾通道 

分 类 号：R965[医药卫生—药理学]