Sanger D J
Life Sci. 1985 Apr 22;36(16):1503-13. doi: 10.1016/0024-3205(85)90374-1.
Much recent research has shown that benzodiazepine binding sites in the central nervous system are associated with GABA receptors. It is therefore possible that the pharmacological and therapeutic effects of benzodiazepines and drugs with similar profiles are mediated through GABAergic mechanisms. In this paper the evidence is considered for a possible involvement of GABA in the behavioral effects of anxiolytic drugs. There are a number of reports that the behavioral actions of anxiolytics can be antagonised by GABA antagonists such as bicuculline or picrotoxin but there are many contradictory findings and these drugs are difficult to use effectively in behavioral studies. In general, GABA agonists do not exert anxiolytic-like behavioral effects after systemic injection but intracerebral administration of muscimol has been shown to produce benzodiazepine-like actions. Although a number of questions remain unanswered, current evidence does not provide strong support for a role for GABA in the behavioral effects of anxiolytic drugs.
近期大量研究表明,中枢神经系统中的苯二氮䓬结合位点与γ-氨基丁酸(GABA)受体相关。因此,苯二氮䓬类药物及具有类似特性的药物的药理和治疗作用可能是通过GABA能机制介导的。本文探讨了GABA可能参与抗焦虑药物行为效应的证据。有多项报告称,抗焦虑药物的行为作用可被GABA拮抗剂(如荷包牡丹碱或印防己毒素)拮抗,但也有许多相互矛盾的研究结果,且这些药物在行为学研究中难以有效应用。一般来说,全身性注射GABA激动剂不会产生类似抗焦虑的行为效应,但脑内注射蝇蕈醇已被证明可产生类似苯二氮䓬的作用。尽管仍有许多问题未得到解答,但目前的证据并不有力支持GABA在抗焦虑药物行为效应中起作用这一观点。