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新 GABA 药理学的兴起。

The rise of a new GABA pharmacology.

机构信息

Institute of Pharmacology, University of Zurich and Department of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology (ETH) Zurich, Winterthurerstr. 190, CH-8057 Zurich, Switzerland.

出版信息

Neuropharmacology. 2011 Jun;60(7-8):1042-9. doi: 10.1016/j.neuropharm.2010.10.020. Epub 2010 Oct 28.

Abstract

Key developments in GABA pharmacology over the last 30 years are reviewed with special reference to the advances pioneered by Erminio Costa. His passion for innovative science, and his quest for novel therapies for psychiatric disorders are particularly apparent in his fundamental contributions to the field of GABA research, with a focus on anxiety disorders and schizophrenia. He was a cofounder of the GABAergic mechanism of action of benzodiazepines. He envisaged partial agonists as novel anxiolytics. He identified DBI (diazepam binding inhibitor) as endogenous agonist of neurosteroidogenesis with multiple CNS effects and he pointed to the developmental origin of GABAergic dysfunctions in schizophrenia through his discovery of a reelin deficit, all this in collaboration with Sandro Guidotti. Today, the GABA pharmacology comprises selective hypnotics, non-sedative anxiolytics, memory enhancers and powerful analgesics. This article is part of a Special Issue entitled 'Trends in neuropharmacology: in memory of Erminio Costa'.

摘要

回顾过去 30 年 GABA 药理学的主要发展,特别提到 Erminio Costa 开创的进展。他对创新科学的热情,以及他对精神疾病新型疗法的追求,在他对 GABA 研究领域的基础贡献中尤为明显,重点是焦虑症和精神分裂症。他是苯二氮䓬类药物 GABA 能作用机制的共同发现者。他设想部分激动剂为新型抗焦虑药。他将 DBI(地西泮结合抑制剂)鉴定为具有多种中枢神经系统作用的内源性神经甾体生成激动剂,并通过发现 reelin 缺乏指出精神分裂症中 GABA 能功能障碍的发育起源,所有这些都是与桑德罗·圭多蒂合作完成的。如今,GABA 药理学包括选择性催眠药、非镇静性抗焦虑药、记忆增强剂和强效镇痛药。本文是题为“神经药理学趋势:纪念 Erminio Costa”的特刊的一部分。

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