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可乐定对两种苯二氮䓬受体激动剂按程序控制的行为作用的影响

[Effect of clonidine on the schedule-controlled performance action of two benzodiazepine receptor agonists].

作者信息

Yang X M, Luo Z P, Zhou J H

出版信息

Yao Xue Xue Bao. 1989 Jan;24(1):11-5.

PMID:2552745
Abstract

Effect of clonidine, a presynaptic adrenoceptor agonist, on the schedule-controlled performance action of two benzodiazepine receptor agonists was assessed in rats in a fixed-ratio (FR6) procedure. Diazepam (0.03 approximately 1.0 mg/kg), an agonist of both type I and II benzodiazepine receptors, decreased the FR performance in a dose-dependent manner. Clonidine (10 micrograms/kg) significantly potentiated the action of diazepam when the dose of diazepam was increased to 0.1 mg/kg. However, clonidine did not show any potentiating effect on the mild depressive action of CL 218,872, a special agonist of type I benzodiazepine receptor until its dose was increased to 10 mg/kg. The Potentiating effect of clonidine on the depressive action of diazepam was significantly antagonized by yohimbine. Bicuculline (3.0 mg/kg) significantly antagonized the depressive action of diazepam (1.0 mg/kg). Our results suggest that the depressive action of benzodiazepines on the function of central noradrenaline system may be one of the benzodiazepine sedative mechanisms, which may be related to the type II benzodiazepine receptors.

摘要

采用固定比率(FR6)程序,在大鼠中评估了突触前肾上腺素能受体激动剂可乐定对两种苯二氮䓬受体激动剂的程序控制行为表现的影响。地西泮(0.03至1.0毫克/千克),一种I型和II型苯二氮䓬受体的激动剂,以剂量依赖的方式降低了FR表现。当将地西泮的剂量增加到0.1毫克/千克时,可乐定(10微克/千克)显著增强了地西泮的作用。然而,直到可乐定的剂量增加到10毫克/千克时,它才对I型苯二氮䓬受体的特殊激动剂CL 218,872的轻度抑制作用表现出任何增强作用。可乐定对氯氮䓬抑制作用的增强作用被育亨宾显著拮抗。荷包牡丹碱(3.0毫克/千克)显著拮抗了地西泮(1.0毫克/千克)的抑制作用。我们的结果表明,苯二氮䓬类药物对中枢去甲肾上腺素能系统功能的抑制作用可能是苯二氮䓬类药物的镇静机制之一,这可能与II型苯二氮䓬受体有关。

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