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Pharmaceuticals 2010, 3(11), 3461-3477;

Allosteric Modulation of αβδ GABAA Receptors

McGovern Institute for Brain Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA
Received: 13 September 2010 / Revised: 1 November 2010 / Accepted: 2 November 2010 / Published: 3 November 2010
(This article belongs to the Special Issue Allosteric Modulation)
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GABAA receptors mediate the majority of the fast inhibition in the mature brain and play an important role in the pathogenesis of many neurological and psychiatric disorders. The αβδ GABAA receptor localizes extra- or perisynaptically and mediates GABAergic tonic inhibition. Compared with synaptically localized αβγ receptors, αβδ receptors are more sensitive to GABA, display relatively slower desensitization and exhibit lower efficacy to GABA agonism. Interestingly, αβδ receptors can be positively modulated by a variety of structurally different compounds, even at saturating GABA concentrations. This review focuses on allosteric modulation of recombinant αβδ receptor currents and αβδ receptor-mediated tonic currents by anesthetics and ethanol. The possible mechanisms for the positive modulation of αβδ receptors by these compounds will also be discussed. View Full-Text
Keywords: GABAA receptors; δ subunit; modulation; kinetics GABAA receptors; δ subunit; modulation; kinetics

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Feng, H.-J. Allosteric Modulation of αβδ GABAA Receptors. Pharmaceuticals 2010, 3, 3461-3477.

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