Target intelligence / Profile preview

Gamma-aminobutyric acid (GABA)-gated chloride channel (GABAA receptor)

Target
GABAA receptor
Molecular classification
Ligand-gated ion channel, Receptor
01

Overview

The GABA-gated chloride channel, primarily referring to the GABAA receptor, is a ligand-gated ion channel mediating fast inhibitory neurotransmission in the central nervous system. Activated by GABA, the primary inhibitory neurotransmitter, it is a pentameric complex with varying subunit compositions (α, β, γ, δ, ε, π, θ, and ρ). GABA binding induces conformational changes that open a chloride-selective pore, allowing Cl− ions to flow down their electrochemical gradient, hyperpolarizing or stabilizing the neuronal membrane and inhibiting action potential firing. Allosteric modulators like benzodiazepines and barbiturates enhance or inhibit channel opening.

Other names
GABA receptorGABAA-gated chloride channelGABAA receptor chloride channelGABAA receptor
02

Mechanism of action

Binding of GABA opens chloride-selective pore, leading to Cl- influx and hyperpolarization/stabilization of membrane potential.

03

Biological functions

Synaptic inhibitionRegulation of neuronal excitabilityNeurotransmission
04

Disease associations

EpilepsyAnxiety disordersInsomniaNeurodevelopmental disordersFragile X syndromeRett syndrome
05

Safety considerations

Tolerance and dependence with chronic use of benzodiazepines and barbituratesRespiratory depression at high doses of barbituratesParadoxical reactions to benzodiazepines (e.g., agitation, aggression)
06

Interacting drugs

Benzodiazepines

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