Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2009 Jan;56(1):141-8.
doi: 10.1016/j.neuropharm.2008.07.045. Epub 2008 Aug 8.

GABA A receptors: subtypes provide diversity of function and pharmacology

Affiliations
Review

GABA A receptors: subtypes provide diversity of function and pharmacology

Richard W Olsen et al. Neuropharmacology. 2009 Jan.

Abstract

This mini-review attempts to update experimental evidence on the existence of GABA(A) receptor pharmacological subtypes and to produce a list of those native receptors that exist. GABA(A) receptors are chloride channels that mediate inhibitory neurotransmission. They are members of the Cys-loop pentameric ligand-gated ion channel (LGIC) superfamily and share structural and functional homology with other members of that family. They are assembled from a family of 19 homologous subunit gene products and form numerous receptor subtypes with properties that depend upon subunit composition, mostly hetero-oligomeric. These vary in their regulation and developmental expression, and importantly, in brain regional, cellular, and subcellular localization, and thus their role in brain circuits and behaviors. We propose several criteria for including a receptor hetero-oligomeric subtype candidate on a list of native subtypes, and a working GABA(A) receptor list. These criteria can be applied to all the members of the LGIC superfamily. The list is divided into three categories of native receptor subtypes: "Identified", "Existence with High Probability", and "Tentative", and currently includes 26 members, but will undoubtedly grow, with future information. This list was first presented by Olsen & Sieghart (in press).

PubMed Disclaimer

Similar articles

Cited by

References

    1. Atack JR. The benzodiazepine binding site of GABAA receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005;14:599–616. - PubMed
    1. Atack JR, Hutson PH, Collinson N, Marshall G, Bentley G, Moyes C, Cook SM, Collins I, Wafford K, McKernan RM, Dawson GR. Anxiogenic properties of an inverse agonist selective for alpha3 subunit-containing GABAA receptors. Br J Pharmacol. 2005;144:357–366. - PMC - PubMed
    1. Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, Ragan I, Kerby J, Street L, Carling R, Castro JL, Whiting P, Dawson GR, McKernan RM. TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluor ophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates. J Pharmacol Exp Ther. 2006;316:410–422. - PubMed
    1. Bali M, Akabas MH. Defining the propofol binding site location on the GABAA receptor. Mol Pharmacol. 2004;65:68–76. - PubMed
    1. Bali M, Jansen M, Akabas MH. Spatial relationship between the GABAA receptor β2 M3 region and the α1 subunit preM1 region. SfN abstracts. 2007 #441.8.

MeSH terms

LinkOut - more resources