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Review
. 2018 Jul;39(7):659-671.
doi: 10.1016/j.tips.2018.03.006. Epub 2018 Apr 30.

The Benzodiazepine Binding Sites of GABAA Receptors

Erwin Sigel  1 , Margot Ernst  2
Affiliations
Review

The Benzodiazepine Binding Sites of GABAA Receptors

Erwin Sigel et al. Trends Pharmacol Sci. 2018 Jul.

Abstract

Everyday activity is based on a subtle equilibrium of excitatory and inhibitory neuronal systems. The most prominent players in neuronal inhibition are synaptic and extrasynaptic GABAA receptors. Benzodiazepines are popular drugs that act as positive allosteric modulators of a subset of these receptors. Benzodiazepines have sedative, hypnotic, muscle-relaxant, and anticonvulsive effects, and are of outstandingly low overdose risk. The discovery of a large number of subtypes of GABAA receptors has raised hopes for a clear separation of this spectrum of actions. We discuss here how far this separation has been achieved, and outline recent progress towards the discovery of novel ligands for canonical and non-canonical binding sites.

Keywords: GABA; GABA(A) receptor; benzodiazepine; receptor subtypes.

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