CL 316243对孕大鼠离体子宫平滑肌收缩的作用  

Effects of CL 316243 on isolated term-pregnant rat myometrial strips in vitro

作　　者：晏飞[1] 董志[1] 傅洁民[2] 曾凡新[2] 

机构地区：[1]重庆医科大学生物化学与分子药理学重点实验室,重庆400016 [2]重庆医药工业研究院,重庆400061

出　　处：《重庆医科大学学报》2010年第8期1171-1174,共4页Journal of Chongqing Medical University

摘　　要：目的:探讨β3-肾上腺素受体(Adrenoreceptor,AR)激动剂CL316243对孕大鼠离体子宫平滑肌收缩的作用及其受体选择性。方法:以β2-AR激动剂沙丁胺醇(Salbutamo)l作阳性对照,观察累积加入CL316243和沙丁胺醇对未预处理和经美托洛尔(Metoprolol),ICI118.551或SR59230A预处理后的缩宫素诱导的孕大鼠子宫平滑肌收缩的影响。放射免疫法检测CL316243和沙丁胺醇对平滑肌中cAMP和cGMP浓度的影响。结果:CL316243对缩宫素诱导的收缩幅度具有浓度依赖性松弛作用。其松弛作用的Emax值(48.13%±5.61%)显著高于沙丁胺醇(35.52%±5.15%)(P<0.05)。CL316243的松弛作用能被SR59230A拮抗而不被美托洛尔或ICI118.551拮抗,沙丁胺醇则是被ICI118.551拮抗而不被美托洛尔或SR59230A拮抗。相比空白对照组,CL316243和沙丁胺醇能增加子宫平滑肌cAMP浓度,但cGMP浓度增加不显著。结论:CL316243激活β3-AR,增加细胞内cAMP浓度,进而松弛孕大鼠离体子宫平滑肌。Objective：To investigate the effects of the selective β3-adrenoreceptor （AR） agonist,CL 316243,on the contractions and levels of cAMP and cGMP of myometrial strips isolated from term-pregnant rats.Methods：Salbutamol,an agonist of β2-AR,was chosen as positive control.We evaluated the effect of increasing concentrations of CL 316243 and salbutamol on oxytocin-induced myometrialcontractions with or without metoprolol,ICI 118.551 and SR 59230A.Effects of CL 316243 and salbutamol on cAMP and cGMP levels in isolated myometrial strips were also evaluated by radioimmunoassay.Results：CL 316243 concentration-dependently decreased the amplitude of oxytocin-induced contractions with Emax value（48.13%±5.61%）ofCL316243,whichwas significantlylargerthanEmaxvalue（35.52%±5.15%）ofsalbutamol（P0.05）.The inhibition of contraction amplitude by CL 316243 was antagonized by SR 59230A but not by metoprolol or ICI 118.551;on the contrary,only ICI 118.551 antagonized effect of salbutamol.CL 316243 and salbutamol increased cAMP levels,compared with control,but the cGMP levels were not increased.Conclusion：CL 316243 induced relaxation of myometrial contractions in term-pregnant rat myometrial contractions through activation of β3-AR,and its effect was mediated through increaseing cAMP level.

关 键 词：β3-肾上腺受体 CL316243 沙丁胺醇 CAMP 

分 类 号：R71[医药卫生—妇产科学]