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氯丁醇对大鼠主动脉45Ca转运及收缩反应的影响及其与缩宫素作用的相关性。

Effects of chlorbutol on 45Ca movements and contractile responses of rat aorta and its relevance to the actions of Syntocinon.

作者信息

Barrigon S, Tejerina T, Delgado C, Tamargo J

出版信息

J Pharm Pharmacol. 1984 Aug;36(8):521-6. doi: 10.1111/j.2042-7158.1984.tb04443.x.

Abstract

The effects of chlorbutol (0.7, 1.4 and 2.8 mM) on the contractile responses induced by KCl and noradrenaline (NA) and on 45Ca movements have been studied on rat isolated thoracic aorta. Chlorbutol decreased, in a dose-dependent manner, contractions induced by KCl and NA and this effect was observed whether it was added before or after the induced contractions. Preincubation with chlorbutol inhibited the contractile responses elicited by addition of Ca (1-5 mM) to Ca-free high-potassium solution. It also inhibited in a dose-dependent manner the 45Ca influx but increased 45Ca efflux in rat aortic strips. These results suggest that chlorbutol decreases peripheral resistance by reducing the availability of intracellular Ca to the contractile machinery in vascular smooth muscle cells. The effects of synthetic oxytocin (Syntocinon) at concentrations containing the same chlorbutol concentration were quantitatively similar from those produced by chlorbutol alone. Therefore, the inhibitory cardiovascular effects ascribed previously to synthetic oxytocin may be attributed to its preservative, chlorbutol, and not to oxytocin itself.

摘要

研究了氯丁醇(0.7、1.4和2.8 mM)对大鼠离体胸主动脉由氯化钾(KCl)和去甲肾上腺素(NA)诱导的收缩反应以及对45Ca转运的影响。氯丁醇以剂量依赖的方式降低了由KCl和NA诱导的收缩,并且无论在诱导收缩之前还是之后添加,均观察到这种效应。用氯丁醇预孵育可抑制向无钙高钾溶液中添加钙(1 - 5 mM)所引发的收缩反应。它还以剂量依赖的方式抑制大鼠主动脉条带中的45Ca内流,但增加45Ca外流。这些结果表明,氯丁醇通过减少血管平滑肌细胞收缩机制中细胞内钙的可用性来降低外周阻力。含有相同氯丁醇浓度的合成催产素(缩宫素)的作用在数量上与单独使用氯丁醇产生的作用相似。因此,先前归因于合成催产素的抑制性心血管作用可能归因于其防腐剂氯丁醇,而非催产素本身。

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