Yang X M, Luo Z P, Zhou J H
Department of Psychopharmacology and Toxicology, Institute of Pharmacology & Toxicology, Beijing, China.
J Pharmacol Exp Ther. 1989 Jul;250(1):358-63.
The role of noradrenaline in the anxiogenic action of the inverse benzodiazepine receptor agonist methyl-4-ethyl-6,7-dimethoxy-beta-carboline-3-carboxylate (DMCM) was assessed in a drug discrimination procedure using yohimbine as the stimulus cue and a conflict procedure using a conditioned behavioral suppression paradigm in rats. The yohimbine cue was antagonized by clonidine (0.03-0.5 mg/kg) and diazepam (0.1-10.0 mg/kg). DMCM (0.1-0.7 mg/kg) only partially substituted for the yohimbine stimulus cue. However, DMCM, in a smaller dose (0.1 mg/kg), significantly shifted the dose-effect curve of the yohimbine cue to the left. This potentiating effect of DMCM on the yohimbine cue was antagonized by Ro 15-1788, a benzodiazepine receptor antagonist, and by the type I benzodiazepine receptor agonist CL218,872. In the conditioned behavioral suppression paradigm, both clonidine (0.03 mg/kg) and diazepam (3 mg/kg) had an anticonflict effect by increasing responses in the conditioned fear period, whereas DMCM (0.1, 0.5 mg/kg) decreased the responses of rats in the conditioned fear period. This proconflict effect of DMCM was antagonized by muscimol (0.5 mg/kg), a type A gamma-aminobutyric acid receptor agonist, Ro 15-1788 (3 mg/kg) and clonidine (0.01 mg/kg). Our results suggest that the depressive effect of DMCM on the function of the gamma-aminobutyric acid-benzodiazepine receptor complex may cause increased noradrenergic activity, which may, in turn, be one of the anxiogenic mechanisms in DMCM.
在一项药物辨别程序中,使用育亨宾作为刺激线索,以及在一项冲突程序中,采用条件性行为抑制范式,在大鼠中评估了去甲肾上腺素在反向苯二氮䓬受体激动剂甲基 - 4 - 乙基 - 6,7 - 二甲氧基 - β - 咔啉 - 3 - 羧酸酯(DMCM)致焦虑作用中的角色。育亨宾线索可被可乐定(0.03 - 0.5毫克/千克)和地西泮(0.1 - 10.0毫克/千克)拮抗。DMCM(0.1 - 0.7毫克/千克)仅部分替代育亨宾刺激线索。然而,较小剂量(0.1毫克/千克)的DMCM可使育亨宾线索的剂量 - 效应曲线显著左移。DMCM对育亨宾线索的这种增强作用可被苯二氮䓬受体拮抗剂Ro 15 - 1788以及I型苯二氮䓬受体激动剂CL218,872拮抗。在条件性行为抑制范式中,可乐定(0.03毫克/千克)和地西泮(3毫克/千克)通过增加条件性恐惧期的反应而具有抗冲突作用,而DMCM(0.1、0.5毫克/千克)则减少了大鼠在条件性恐惧期的反应。DMCM的这种促冲突作用可被A型γ - 氨基丁酸受体激动剂蝇蕈醇(0.5毫克/千克)、Ro 15 - 1788(3毫克/千克)和可乐定(0.01毫克/千克)拮抗。我们的结果表明,DMCM对γ - 氨基丁酸 - 苯二氮䓬受体复合物功能的抑制作用可能导致去甲肾上腺素能活性增加,这反过来可能是DMCM致焦虑机制之一。