Department of Biochemistry, German University in Cairo, New Cairo 11835, Egypt.
ACS Chem Neurosci. 2020 Jun 17;11(12):1706-1725. doi: 10.1021/acschemneuro.0c00054. Epub 2020 Jun 3.
The inhibitory glycine receptor is a member of the Cys-loop superfamily of ligand-gated ion channels. It is the principal mediator of rapid synaptic inhibition in the spinal cord and brainstem and plays an important role in the modulation of higher brain functions including vision, hearing, and pain signaling. Glycine receptor function is controlled by only a few agonists, while the number of antagonists and positive or biphasic modulators is steadily increasing. These modulators are important for the study of receptor activation and regulation and have found clinical interest as potential analgesics and anticonvulsants. High-resolution structures of the receptor have become available recently, adding to our understanding of structure-function relationships and revealing agonistic, inhibitory, and modulatory sites on the receptor protein. This Review presents an overview of compounds that activate, inhibit, or modulate glycine receptor function in vitro and in vivo.
抑制性甘氨酸受体是配体门控离子通道 Cys 环超家族的成员。它是脊髓和脑干中快速突触抑制的主要介导者，在包括视觉、听觉和疼痛信号在内的高级脑功能的调节中发挥着重要作用。甘氨酸受体的功能仅受少数激动剂控制，而拮抗剂和阳性或双相调节剂的数量正在稳步增加。这些调节剂对于研究受体的激活和调节很重要，并且作为潜在的镇痛药和抗惊厥药具有临床意义。最近获得了该受体的高分辨率结构，这增加了我们对结构-功能关系的理解，并揭示了受体蛋白上的激动剂、抑制剂和调节剂结合位点。本综述介绍了在体外和体内激活、抑制或调节甘氨酸受体功能的化合物概述。
