Acritopoulou-Fourcroy S, Clabaut M, Schrub J C
Eur J Pharmacol. 1984 Dec 15;107(1):59-64. doi: 10.1016/0014-2999(84)90091-8.
The effects of two adrenoceptor antagonists, nicergoline (alpha 1) and acebutolol (beta 1), on the contraction of myometrium in the proestrous rat were compared to those of noradrenaline and phentolamine. The spontaneous myometrial contractions of Wistar rats on the day of proestrus were recorded isometrically and the data were analysed using Wilcoxon non-parametric statistics. All drugs were administered i.v. and the doses are expressed as microgram/kg body weight. Noradrenaline (1200 micrograms/kg per h) induced a 32.5% reduction (P less than 0.001) of the uterine contraction amplitude. Nicergoline did not alter uterine motility significantly when administered alone at doses ranging from 400 to 1600 micrograms/kg. However, successive injections of nicergoline in the same range given during noradrenaline infusion at 600 micrograms/kg per h potentiated the relaxing action of the latter (38%, P less than 0.01). Phentolamine (120 micrograms/kg) reduced myometrial activity by 25% (P less than 0.05). This inhibitory response rose to 65% (P less than 0.001) when the dose of phentolamine was increased to 960 micrograms/kg. When a single injection of nicergoline (400 micrograms/kg) was followed by the administration of increasing doses of acebutolol (120, 1200, 2400 micrograms/kg) the slight inhibitory effect on uterine motility observed after administration of each of the two agents separately became more pronounced (P less than 0.05). It appears from these results that combining noradrenaline with nicergoline and nicergoline with acebutolol leads to potentiation of their relaxing effects. Furthermore the results confirm that nicergoline is a partial alpha-blocker.
比较了两种肾上腺素能受体拮抗剂尼麦角林(α1)和醋丁洛尔(β1)与去甲肾上腺素和酚妥拉明对动情前期大鼠子宫肌层收缩的影响。采用等长记录法记录动情前期Wistar大鼠子宫肌层的自发收缩,并使用Wilcoxon非参数统计方法分析数据。所有药物均静脉注射,剂量以微克/千克体重表示。去甲肾上腺素(1200微克/千克·小时)可使子宫收缩幅度降低32.5%(P<0.001)。单独给予尼麦角林时,剂量在400至1600微克/千克范围内,对子宫运动无明显影响。然而,在以600微克/千克·小时的速度输注去甲肾上腺素期间,连续注射相同范围内的尼麦角林可增强后者的舒张作用(38%,P<0.01)。酚妥拉明(120微克/千克)可使子宫肌层活性降低25%(P<0.05)。当酚妥拉明剂量增加到960微克/千克时,这种抑制反应升至65%(P<0.001)。当单次注射尼麦角林(400微克/千克)后,再给予递增剂量的醋丁洛尔(120、1200、2400微克/千克)时,分别给予这两种药物后观察到的对子宫运动的轻微抑制作用变得更加明显(P<0.05)。从这些结果看来,去甲肾上腺素与尼麦角林以及尼麦角林与醋丁洛尔联合使用可增强它们的舒张作用。此外,结果证实尼麦角林是一种部分α受体阻滞剂。