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β2肾上腺素能受体激动剂利托君对妊娠大鼠子宫肌层平滑肌细胞的影响。

Effects of ritodrine, a beta 2-adrenoceptor agonist, on smooth muscle cells of the myometrium of pregnant rats.

作者信息

Izumi H, Kishikawa T

出版信息

Br J Pharmacol. 1982 Jul;76(3):463-71. doi: 10.1111/j.1476-5381.1982.tb09241.x.

Abstract

1 Effects of ritodrine on the electrical and mechanical activities of the myometrium of pregnant rats were investigated in relation to cyclic adenosine 3',5'-monophosphate (cyclic AMP) production and the actions of isoprenaline. 2 In the longitudinal muscle cells of the 22nd day of gestation, ritodrine (greater than 10(-8) M) hyperpolarized the membrane, reduced the membrane resistance and suppressed the amplitude of contraction. Increased concentrations of ritodrine (greater than 10(-7) M) suppressed the generation of spikes and increased the amount of cyclic AMP produced. These actions of ritodrine were much the same as those of isoprenaline but the dose-response curves of all parameters were shifted to the right. 3 The effects of ritodrine on the circular muscle cells at the 22nd day of gestation were similar to those observed in the longitudinal muscle cells. 4 In the circular muscle cells at the 17-19th days of gestation, ritodrine produced neither a hyperpolarization nor an increase in cyclic AMP production (up to 10(-5) M) but did reduce the plateau potential and did relax the tissue (greater than 10(-7) M). 5 In the longitudinal muscle cells, during the 17-19th days of gestation, the responses of the tissues were similar to those observed in circular muscles on the 22nd day of gestation. These actions of ritodrine were suppressed by propranolol (10(-6) M). 6 These results indicate that ritodrine is a beta-adrenoceptor agonist and its mechanism of action similar to that of isoprenaline. However, the potency of ritodrine was approximately 100 times less than that of isoprenaline.

摘要
  1. 研究了利托君对妊娠大鼠子宫肌层电活动和机械活动的影响,并探讨了其与环磷腺苷(cAMP)生成及异丙肾上腺素作用的关系。2. 在妊娠第22天的纵行肌细胞中,利托君(浓度大于10⁻⁸M)使细胞膜超极化,降低膜电阻,并抑制收缩幅度。利托君浓度增加(大于10⁻⁷M)时,抑制锋电位的产生并增加cAMP的生成量。利托君的这些作用与异丙肾上腺素相似,但所有参数的剂量 - 反应曲线均右移。3. 利托君对妊娠第22天环行肌细胞的作用与在纵行肌细胞中观察到的相似。4. 在妊娠第17 - 19天的环行肌细胞中,利托君(浓度高达10⁻⁵M)既不引起超极化,也不增加cAMP的生成,但可降低平台电位并使组织松弛(浓度大于10⁻⁷M)。5. 在妊娠第17 - 19天的纵行肌细胞中,组织的反应与在妊娠第22天环行肌中观察到的相似。利托君的这些作用可被普萘洛尔(10⁻⁶M)抑制。6. 这些结果表明,利托君是一种β - 肾上腺素能受体激动剂,其作用机制与异丙肾上腺素相似。然而,利托君的效能约为异丙肾上腺素的1/100。

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