杨晓敏, 罗质璞, 周金黄. 可乐定对两种苯二氮受体激动剂程控操作效应的影响J. 药学学报, 1989, 24(1): 11-11.
引用本文: 杨晓敏, 罗质璞, 周金黄. 可乐定对两种苯二氮受体激动剂程控操作效应的影响J. 药学学报, 1989, 24(1): 11-11.
XM Yang, ZP Luo , JH Zhou, . EFFECT OF CLONIDINE ON THE SCHEDULE-CONTROLLED PERFORMANCE ACTION OF TWO BENZODIAZEPINE RECEPTOR AGONISTSJ. Acta Pharmaceutica Sinica, 1989, 24(1): 11-11.
Citation: XM Yang, ZP Luo , JH Zhou, . EFFECT OF CLONIDINE ON THE SCHEDULE-CONTROLLED PERFORMANCE ACTION OF TWO BENZODIAZEPINE RECEPTOR AGONISTSJ. Acta Pharmaceutica Sinica, 1989, 24(1): 11-11.

可乐定对两种苯二氮受体激动剂程控操作效应的影响

EFFECT OF CLONIDINE ON THE SCHEDULE-CONTROLLED PERFORMANCE ACTION OF TWO BENZODIAZEPINE RECEPTOR AGONISTS

  • 摘要: Ⅰ,Ⅱ型苯二氮受体激动剂安定和可乐定均可剂量依赖性抑制大鼠程控操作。可乐定可协同安定的抑制。育亨宾可拮抗之。Ⅰ型苯二氮受体激动剂GL218,872对大鼠程控操作无显著影响。增加其剂量至10mg/kg,使程控操作速率最大降低32%。可乐定可显著加强该剂量的抑制作用,对其余小剂量组无显著影响。结果提示,苯二氮激活Ⅱ型受体对去甲肾上腺素系统功能抑制,可能是其镇静作用机理之一。

     

    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 (0.03~1.0 mg/kg), an agonist of both type Ⅰ and Ⅱ benzodiazepine receptors, decreased the FR performance in a dose-dependent manner. Clonidine (10μg/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. Bicueulline (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.

     

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