Structure-Dependent Activity of Natural GABA(A) Receptor Modulators

被引：27
|
作者：
Cicek, Serhat Sezai [1 ]
机构：
[1] Univ Kiel, Dept Pharmaceut Biol, Gutenbergstr 76, D-24118 Kiel, Germany
来源：
MOLECULES | 2018年 / 23卷 / 07期
关键词：
gamma-aminobutyric acid; natural product; plant origin; benzodiazepine binding site; anxiolytic; sedative; anesthetic; anticonvulsant; CENTRAL BENZODIAZEPINE-RECEPTOR; SCUTELLARIA-BAICALENSIS GEORGI; POSITIVE ALLOSTERIC MODULATION; ELEVATED PLUS-MAZE; PENTOBARBITAL-INDUCED SLEEP; CL-CHANNEL ACTIVATION; BLOOD-BRAIN-BARRIER; ANXIOLYTIC-LIKE; IN-VITRO; HIPPOCAMPAL-NEURONS;
D O I：
10.3390/molecules23071512
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
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页数：44
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