Allosteric Modulation of αβδ GABAA Receptors

Pharmaceuticals

关键词: GABA_A receptors;    δ subunit;    modulation;    kinetics;   

DOI  :  10.3390/ph3113461

来源: mdpi

【 摘 要 】

GABA_A 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 GABA_A 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.

【 授权许可】

CC BY   
© 2010 by the authors; licensee MDPI, Basel, Switzerland.