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钙通道配体对小鼠乙醇麻醉特性的影响。

Effects of calcium channel ligands on anaesthetic properties of ethanol in mice.

作者信息

Biała G

机构信息

Department of Pharmacodynamics, Medical University School, Lublin, Poland.

出版信息

Pol J Pharmacol. 1999 Mar-Apr;51(2):125-30.

Abstract

This study has examined the effect of two calcium channel antagonists--nifedipine, verapamil and a calcium channel agonist BAY K 8644 on duration of ethanol-induced anaesthetic activity measured as the loss of the righting reflex (LORR) in mice. Nifedipine (5 and 10 mg/kg, i.p.) and verapamil (10 and 20 mg/kg, i.p.) potentiated the acute general anaesthetic effect of ethanol (3.5 g/kg, i.p.). BAY K 8644 (2 mg/kg, i.p.) shortened the duration of ethanol-induced LORR. This action of BAY K 8644 was prevented by the pretreatment with nifedipine (2.5 mg/kg, i.p.) but not with verapamil (5 mg/kg, i.p.). Injections of both calcium channel blockers--nifedipine (2.5 mg/kg) and verapamil (5 mg/kg) did not influence the ethanol-induced hypnotic activity themselves. Our results suggest that the calcium ions are involved in the central depressant effects of acute ethanol administration at high doses. It can be supposed that the modification of the activity of voltage-dependent calcium channels plays an important role in the anaesthetic action of ethanol.

摘要

本研究考察了两种钙通道拮抗剂——硝苯地平、维拉帕米以及一种钙通道激动剂BAY K 8644对以小鼠翻正反射消失(LORR)衡量的乙醇诱导麻醉活性持续时间的影响。硝苯地平(5和10毫克/千克,腹腔注射)和维拉帕米(10和20毫克/千克,腹腔注射)增强了乙醇(3.5克/千克,腹腔注射)的急性全身麻醉作用。BAY K 8644(2毫克/千克,腹腔注射)缩短了乙醇诱导的LORR持续时间。硝苯地平(2.5毫克/千克,腹腔注射)预处理可阻止BAY K 8644的这一作用,但维拉帕米(5毫克/千克,腹腔注射)预处理则不能。两种钙通道阻滞剂——硝苯地平(2.5毫克/千克)和维拉帕米(5毫克/千克)单独注射均不影响乙醇诱导的催眠活性。我们的结果表明,钙离子参与了高剂量急性乙醇给药的中枢抑制作用。可以推测,电压依赖性钙通道活性的改变在乙醇的麻醉作用中起重要作用。

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