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吡唑并吡啶和三唑并哒嗪对戊巴比妥辨别刺激的影响。

Effects of pyrazolopyridines and a triazolopyridazine on the pentobarbital discriminative stimulus.

作者信息

Young R, Glennon R A, Dewey W L

机构信息

Department of Medicinal Chemistry, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0001.

出版信息

Psychopharmacology (Berl). 1987;93(4):494-7. doi: 10.1007/BF00207241.

Abstract

Rats were trained to discriminate injections of racemic pentobarbital (5.0 mg/kg) from saline in a two-lever drug discrimination task. After stable discrimination performance was attained, stimulus generalization studies were conducted with another barbiturate (barbital), benzodiazepine derivatives (diazepam and chlordiazepoxide), pyrazolopyridine derivatives (etazolate, cartazolate, and tracazolate), and a triazolopyridazine (CL 218, 872). The pentobarbital stimulus generalized to all of these compounds, except cartazolate. In addition, the administration of the benzodiazepine receptor antagonist flumazepil prior to benzodiazepine or triazolopyridazine administration produced a dose-related antagonism of each generalization. In contrast, the administration of flumazepil before barbiturate or pyrazolopyridine (i.e., etazolate or tracazolate) injection resulted in no attenuation of these generalizations. The results indicate that while certain barbiturates, benzodiazepines, pyrazolopyridines and triazolopyridazines are capable of producing similar stimulus effects, the behavioral actions of these agents can be differentiated on the basis of their susceptibility to antagonism by flumazepil.

摘要

在一项双杠杆药物辨别任务中,训练大鼠区分注射外消旋戊巴比妥(5.0毫克/千克)和注射生理盐水。在获得稳定的辨别表现后,用另一种巴比妥类药物(巴比妥)、苯二氮䓬衍生物(地西泮和氯氮卓)、吡唑并吡啶衍生物(依他唑酯、卡他唑酯和曲卡唑酯)以及一种三唑并哒嗪(CL 218,872)进行刺激泛化研究。戊巴比妥刺激可泛化至所有这些化合物,但卡他唑酯除外。此外,在给予苯二氮䓬或三唑并哒嗪之前给予苯二氮䓬受体拮抗剂氟马西尼,会产生与剂量相关的对每种泛化的拮抗作用。相比之下,在注射巴比妥类药物或吡唑并吡啶(即依他唑酯或曲卡唑酯)之前给予氟马西尼,这些泛化作用不会减弱。结果表明,虽然某些巴比妥类药物、苯二氮䓬类药物、吡唑并吡啶类药物和三唑并哒嗪类药物能够产生相似的刺激效应,但这些药物的行为作用可以根据它们对氟马西尼拮抗作用的敏感性来区分。

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