一种非典型苯二氮䓬类药物Ro 5-4864的特性

Characteristics of an atypical benzodiazepine, Ro 5-4864.

作者信息

Pellow S, File S E

出版信息

Neurosci Biobehav Rev. 1984 Fall;8(3):405-13. doi: 10.1016/0149-7634(84)90060-5.

Abstract

Ro 5-4864 is a 1,4 benzodiazepine which, atypically, does not bind to the classical CNS benzodiazepine receptors, but has high affinity for the peripheral type of binding site found both in the periphery and in the brain. Biochemical evidence for alternative sites of action for this compound is discussed. We review the behavioral profile of Ro 5-4864 (sedative, convulsant and anxiogenic in rodents) and also describe the behavioral effects of combining Ro 5-4864 treatment with benzodiazepines (e.g., diazepam, chlordiazepoxide) and with other drugs that modify the activity of benzodiazepines (Ro 15-1788, CGS 8216, picrotoxin, PK 11195, phenytoin). In the light of these interactions and electrophysiological evidence we conclude that the actions of Ro 5-4864 are most likely to be mediated at the GABA-benzodiazepine receptor complex in the CNS.

摘要

Ro 5-4864是一种1,4-苯二氮䓬类药物，其不同寻常之处在于它不与经典的中枢神经系统苯二氮䓬受体结合，但对在周围组织和大脑中均发现的外周型结合位点具有高亲和力。本文讨论了该化合物作用于其他位点的生化证据。我们回顾了Ro 5-4864的行为特征（在啮齿动物中具有镇静、惊厥和致焦虑作用），还描述了将Ro 5-4864与苯二氮䓬类药物（如地西泮、氯氮卓）以及与其他改变苯二氮䓬类药物活性的药物（Ro 15-1788、CGS 8216、印防己毒素、PK 11195、苯妥英）联合使用时的行为效应。鉴于这些相互作用和电生理证据，我们得出结论，Ro 5-4864的作用很可能是在中枢神经系统的GABA-苯二氮䓬受体复合物上介导的。