Are Extrasynaptic GABAA Receptors Important Targets for Sedative/Hypnotic Drugs?

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چکیده

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Are extrasynaptic GABAA receptors important targets for sedative/hypnotic drugs?

High-affinity extrasynaptic GABA(A) receptors are persistently activated by the low ambient GABA levels that are known to be present in extracellular space. The resulting tonic conductance generates a form of shunting inhibition that is capable of altering cellular and network behavior. It has been suggested that this tonic inhibition will be enhanced by neurosteroids, antiepileptics, and sedat...

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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" GABA(A) receptor-mediated inhibition (inhibitory postsynaptic currents), tonic GABA(A) receptor-mediated inhibition re...

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ژورنال

عنوان ژورنال: Journal of Neuroscience

سال: 2012

ISSN: 0270-6474,1529-2401

DOI: 10.1523/jneurosci.5406-11.2012