Target intelligence / Profile preview

GABA~A~ receptor (GABA~A~R)

Target
GABA~A~R
Molecular classification
Ion channel, Ligand-gated ion channel, Receptor
01

Overview

The GABA~A~ receptor is an ionotropic receptor and ligand-gated ion channel that plays a crucial role in inhibitory neurotransmission in the central nervous system. It is composed of various subunits (α, β, γ, δ, ε, θ, π, ρ) that form a heteropentameric structure. The receptor is selectively permeable to chloride ions and is modulated by a variety of drugs, including benzodiazepines and ethanol, which act at allosteric binding sites to enhance GABA's inhibitory effects[1][4][5].

Other names
GABA~A~ receptorGABA~A~R
02

Mechanism of action

Allosteric modulation, Potentiation of GABA-mediated chloride influx, Inhibition of neuronal excitability

03

Biological functions

Signal transductionInhibition of neuronal activityRegulation of chloride ion flow
04

Disease associations

Neurodegenerative diseaseEpilepsyAnxiety disordersSleep disorders
05

Safety considerations

DependenceWithdrawal symptomsSedationRespiratory depression
06

Interacting drugs

Benzodiazepines

3 more in the full profile.

07

Biomarkers

None specifically identified for patient selection or efficacy monitoring

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