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GABA is the principal inhibitory neurotransmitter in the CNS and
acts via GABAA and GABAB receptors. Recently, a novel form of GABAA
receptor-mediated inhibition, termed "tonic" inhibition, has been
described. Whereas synaptic GABAA receptors underlie classical
"phasic" GABAA receptor-mediated inhibition (inhibitory
postsynaptic currents), tonic GABAA receptor-mediated inhibition
results from the activation of extrasynaptic receptors by low
concentrations of ambient GABA. Extrasynaptic GABAA 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 book highlights ongoing work examining the
properties of recombinant and native extrasynaptic GABAA receptors
and their preferential targeting by endogenous and clinically
relevant agents. In addition, it emphasizes the important role of
extrasynaptic GABAA receptors in GABAergic inhibition throughout
the CNS and identifies them as a major player in both physiological
and pathophysiological processes.
GABA is the principal inhibitory neurotransmitter in the CNS and
acts via GABAA and GABAB receptors. Recently, a novel form of GABAA
receptor-mediated inhibition, termed "tonic" inhibition, has been
described. Whereas synaptic GABAA receptors underlie classical
"phasic" GABAA receptor-mediated inhibition (inhibitory
postsynaptic currents), tonic GABAA receptor-mediated inhibition
results from the activation of extrasynaptic receptors by low
concentrations of ambient GABA. Extrasynaptic GABAA 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 book highlights ongoing work examining the
properties of recombinant and native extrasynaptic GABAA receptors
and their preferential targeting by endogenous and clinically
relevant agents. In addition, it emphasizes the important role of
extrasynaptic GABAA receptors in GABAergic inhibition throughout
the CNS and identifies them as a major player in both physiological
and pathophysiological processes.
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