GABA-A receptor subtypes in the brain: a paradigm for CNS drug discovery?
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.
Whiting
Paul J
PJ
Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK CM20 2QR. paul_whiting@merck.com
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002490:Central Nervous System / Q000187:drug effects / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D058785:GABA-A Receptor Agonists; D058787:GABA-A Receptor Antagonists; D006801:Humans; D011963:Receptors, GABA-A / Q000378:metabolism*; D013678:Technology, Pharmaceutical / Q000379:methods
D058785:GABA-A Receptor Agonists; D058787:GABA-A Receptor Antagonists; D011963:Receptors, GABA-A