Department of Pharmaceutical Biology, Kiel University, Gutenbergstraße 76, 24118 Kiel, Germany.
Molecules. 2018 Jun 22;23(7):1512. doi: 10.3390/molecules23071512.
GABA(A) receptors are ligand-gated ion channels consisting of five subunits from eight subfamilies, each assembled in four hydrophobic transmembrane domains. This pentameric structure not only allows different receptor binding sites, but also various types of ligands, such as orthosteric agonists and antagonists, positive and negative allosteric modulators, as well as second-order modulators and non-competitive channel blockers. A fact, that is also displayed by the variety of chemical structures found for both, synthetic as well as nature-derived GABA(A)-receptor modulators. This review covers the literature for natural GABA(A)-receptor modulators until the end of 2017 and discusses their structure-activity relationship.
GABA(A) 受体是配体门控离子通道，由八个亚家族的五个亚基组成，每个亚基由四个疏水性跨膜结构域组成。这种五聚体结构不仅允许不同的受体结合位点，而且还允许各种类型的配体，如正位激动剂和拮抗剂、正变和负变变构调节剂以及二级调节剂和非竞争性通道阻滞剂。事实上，这也反映在合成和天然 GABA(A)受体调节剂的各种化学结构中。本综述涵盖了截至 2017 年底的天然 GABA(A)受体调节剂的文献，并讨论了它们的结构-活性关系。
