Diversity and Functions of GABA Receptors: A Tribute to Hanns Möhler

0458030 - ÚEM 2016 RIV US eng M - Monography Chapter
Raveh, A. - Tureček, Rostislav - Bettler, B.
Chapter Six – Mechanisms of Fast Desensitization of GABAB.
Diversity and Functions of GABA Receptors: A Tribute to Hanns Möhler. Vol. B. New York: Academic Press, 2015 - (Rudolph, U.), s. 145-165. Advances in Pharmacology, 73. ISBN 978-0-12-802658-8
Institutional support: RVO:68378041
Keywords : GABAB * G protein-coupled receptor * RGS * G protein-coupled receptor kinase * KCTD12
Subject RIV: FP - Other Medical Disciplines

GABAB receptors (GABABRs) regulate the excitability of most neurons in the central nervous system by modulating the activity of enzymes and ion channels. In the sustained presence of the neurotransmitter γ-aminobutyric acid, GABABRs exhibit a time-dependent decrease in the receptor response—a phenomenon referred to as homologous desensitization. Desensitization prevents excessive receptor influences on neuronal activity. Much work focused on the mechanisms of GABABR desensitization that operate at the receptor and control receptor expression at the plasma membrane. Over the past few years, it became apparent that GABABRs additionally evolved mechanisms for faster desensitization. These mechanisms operate at the G protein rather than at the receptor and inhibit G protein signaling within seconds of agonist exposure. The mechanisms for fast desensitization are ideally suited to regulate receptor-activated ion channel responses, which influence neuronal activity on a faster timescale than effector enzymes. Here, we provide an update on the mechanisms for fast desensitization of GABABR responses and discuss physiological and pathophysiological implications

Permanent Link: http://hdl.handle.net/11104/0258344