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

YAN Fei; et al

doi:10.13406/j.cnki.cyxb.2010.08.041

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

更新时间：2024-01-17

- Effects of CL 316243 on isolated term-pregnant rat myometrial strips in vitro
- Journal of Chongqing Medical University Vol. 35, Issue 8, Pages: 1171-1174(2010)
- 作者机构：
  
  1. 重庆医科大学生物化学与分子药理学重点实验室
  2. 重庆医药工业研究院
- 作者简介：
- 基金信息：
- DOI：10.13406/j.cnki.cyxb.2010.08.041
  CLC： R96
- Published：2010，
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[1]晏飞,董志,傅洁民,曾凡新.CL 316243对孕大鼠离体子宫平滑肌收缩的作用[J].重庆医科大学学报,2010,35(08):1171-1174.

YAN Fei, et al. Effects of CL 316243 on isolated term-pregnant rat myometrial strips in vitro. [J]. Journal of Chongqing Medical University 35(8):1171-1174(2010)
[1]晏飞,董志,傅洁民,曾凡新.CL 316243对孕大鼠离体子宫平滑肌收缩的作用[J].重庆医科大学学报,2010,35(08):1171-1174. DOI： 10.13406/j.cnki.cyxb.2010.08.041.

YAN Fei, et al. Effects of CL 316243 on isolated term-pregnant rat myometrial strips in vitro. [J]. Journal of Chongqing Medical University 35(8):1171-1174(2010) DOI： 10.13406/j.cnki.cyxb.2010.08.041.

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。

Abstract

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(P<0.05).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

Keywords

β3-adrenoreceptorCL316243SalbutamolcAMP

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