GABA-A receptor subtypes in the brain: a paradigm for CNS drug discovery?
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Updated: Sep 25, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
1Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK CM20 2QR. paul_whiting@merck.com
Abstract:
The clinical importance of benzodiazepines, barbiturates and general anesthetics, all of which act through the gamma-aminobutyric acid (GABA)-A neurotransmitter receptor, is testament to its significance as a CNS drug target. These drugs were all developed before there was any understanding of the diversity of this receptor gene family. Recent studies using genetically modified mice and GABA-A receptor-subtype-selective compounds have helped to delineate the function of some of these subtypes, and have revealed that it might be possible to develop a new generation of selective drugs with improved profiles or novel applications.
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