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Molecules 2018, 23(7), 1512; https://doi.org/10.3390/molecules23071512

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

Department of Pharmaceutical Biology, Kiel University, Gutenbergstraße 76, 24118 Kiel, Germany
Academic Editor: Antonio Evidente
Received: 30 May 2018 / Revised: 19 June 2018 / Accepted: 20 June 2018 / Published: 22 June 2018
(This article belongs to the Special Issue Structure-Activity Relationship of Natural Products 2018)
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Abstract

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. View Full-Text
Keywords: γ-aminobutyric acid; natural product; plant origin; benzodiazepine binding site; anxiolytic; sedative; anesthetic; anticonvulsant γ-aminobutyric acid; natural product; plant origin; benzodiazepine binding site; anxiolytic; sedative; anesthetic; anticonvulsant
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Çiçek, S.S. Structure-Dependent Activity of Natural GABA(A) Receptor Modulators. Molecules 2018, 23, 1512.

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