Extrasynaptic GABAA Receptors: Form, Pharmacology, and Function

GABA is the principal inhibitory neurotransmitter in the CNS and acts via GABA(A) and GABA(B) receptors. Recently, a novel form of GABA(A) receptor-mediated inhibition, termed "tonic" inhibition, has been described. Whereas synaptic GABA(A) receptors underlie classical "phasic" G...

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Bibliographic Details
Published in:The Journal of neuroscience 2009-10, Vol.29 (41), p.12757-12763
Main Authors: Belelli, Delia, Harrison, Neil L, Maguire, Jamie, Macdonald, Robert L, Walker, Matthew C, Cope, David W
Format: Article
Language:English
Subjects:
Animals
Biophysical Phenomena - drug effects
Biophysical Phenomena - physiology
Central Nervous System - drug effects
Central Nervous System - physiology
Female
gamma-Aminobutyric Acid - metabolism
gamma-Aminobutyric Acid - pharmacology
Humans
Male
Neural Inhibition - drug effects
Neural Inhibition - physiology
Pregnancy
Presynaptic Terminals - drug effects
Presynaptic Terminals - metabolism
Protein Subunits - physiology
Receptors, GABA-A - physiology
Symposia and Mini-Symposia
Synaptic Transmission - drug effects
Synaptic Transmission - physiology
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Summary:GABA is the principal inhibitory neurotransmitter in the CNS and acts via GABA(A) and GABA(B) receptors. Recently, a novel form of GABA(A) receptor-mediated inhibition, termed "tonic" inhibition, has been described. Whereas synaptic GABA(A) receptors underlie classical "phasic" GABA(A) receptor-mediated inhibition (inhibitory postsynaptic currents), tonic GABA(A) receptor-mediated inhibition results from the activation of extrasynaptic receptors by low concentrations of ambient GABA. Extrasynaptic GABA(A) receptors are composed of receptor subunits that convey biophysical properties ideally suited to the generation of persistent inhibition and are pharmacologically and functionally distinct from their synaptic counterparts. This mini-symposium review highlights ongoing work examining the properties of recombinant and native extrasynaptic GABA(A) receptors and their preferential targeting by endogenous and clinically relevant agents. In addition, it emphasizes the important role of extrasynaptic GABA(A) receptors in GABAergic inhibition throughout the CNS and identifies them as a major player in both physiological and pathophysiological processes.
ISSN:0270-6474
1529-2401
DOI:10.1523/JNEUROSCI.3340-09.2009