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α1-肾上腺素能受体激动剂2-(2-氯-5-三氟甲基苯基亚氨基)咪唑烷对兔脑电图的同步化作用

Synchronizing effect of the alpha 1-adrenoceptor agonist 2-(2-chloro-5-trifluoromethylphenylimino)imidazolidine on rabbit electroencephalogram.

作者信息

Stumpf C, Pichler L

机构信息

Institute of Neuropharmacology, University of Vienna, Austria.

出版信息

Arzneimittelforschung. 1988 Jun;38(6):770-4.

PMID:3178916
Abstract

The selective alpha 1-adrenoceptor agonist St 587 (2-(2-chloro-5-trifluoromethylphenylimino)imidazolidine) was tested in conscious rabbits in the dose range of 0.125 to 8 mg/kg cumulatively i.v. In cardiovascular experiments St 587 increased mean arterial blood pressure and decreased heart rate in a dose dependent manner. In neuropharmacological experiments St 587 induced a biphasic EEG effect, an EEG synchronization preceded by a short period of cortical arousal. The duration of both EEG phenomena increased with increasing doses. There was no correlation between rise in blood pressure and EEG arousal reaction as periods of precentral spindling appeared also during maximal increase in blood pressure. Both, EEG synchronization and arousal reaction could be antagonized by the alpha 1-adrenoceptor antagonist prazosin, 1-2 mg/kg i.v. From these experiments it is concluded that the main effect of the alpha 1-adrenoceptor agonist St 587 in rabbits is EEG synchronization, i.e. sedation. Furthermore a barbiturate antagonism by high doses of St 587 was shown and this is explained by the initial arousal reaction as observed after injection of St 587.

摘要

选择性α1肾上腺素能受体激动剂St 587(2-(2-氯-5-三氟甲基苯基亚氨基)咪唑烷)以0.125至8mg/kg的累积静脉注射剂量在清醒兔中进行测试。在心血管实验中,St 587以剂量依赖性方式增加平均动脉血压并降低心率。在神经药理学实验中,St 587诱导双相脑电图效应,即在短暂的皮质唤醒之前出现脑电图同步。两种脑电图现象的持续时间随剂量增加而增加。由于在血压最大升高期间也出现中央前回纺锤波期,因此血压升高与脑电图唤醒反应之间没有相关性。静脉注射1-2mg/kg的α1肾上腺素能受体拮抗剂哌唑嗪可拮抗脑电图同步和唤醒反应。从这些实验得出结论,α1肾上腺素能受体激动剂St 587在兔中的主要作用是脑电图同步,即镇静作用。此外,高剂量的St 587显示出巴比妥类拮抗作用,这是由注射St 587后观察到的初始唤醒反应所解释的。

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