GABA_A receptors are pentameric ligand-gated ion channels that mediate most fast neuronal inhibition in the brain. In addition to their important physiological roles, they are noteworthy in their rich pharmacology; prominent drugs used for anxiety, insomnia, and general anesthesia act through positive modulation of GABA_A receptors. Direct structural information for how these drugs work was absent until recently. Efforts in structural biology over the past few years have revealed how important drug classes and natural products interact with the GABA_A receptor, providing a foundation for studies in dynamics and structure-guided drug design. Here, we review recent developments in GABA_A receptor structural pharmacology, focusing on subunit assemblies of the receptor found at synapses.

GABA _A受体是五聚体配体门控离子通道，可介导大脑中最快速的神经元抑制。它们除了具有重要的生理作用外，还具有丰富的药理作用。用于焦虑、失眠和全身麻醉的主要药物通过 GABA _A受体的正向调节起作用。直到最近还没有关于这些药物如何发挥作用的直接结构信息。过去几年在结构生物学方面的努力揭示了药物类别和天然产物与 GABA _A受体相互作用的重要性，为动力学和结构导向药物设计的研究提供了基础。_{在这里，我们回顾了 GABA A 的}最新发展受体结构药理学，侧重于在突触处发现的受体的亚基组装。