Target intelligence / Profile preview

GABA-A Receptor Subunit Alpha 1 (GABRA1)

Target
GABRA1
Molecular classification
Ligand-gated ion channel, Receptor, GABA-A receptor subunit
01

Overview

The GABA-A receptor subunit alpha-1 (GABRA1) is a protein encoded by the GABRA1 gene. It is a subunit of the GABA-A receptor, a ligand-gated chloride channel that mediates fast inhibitory neurotransmission in the central nervous system. Activation of the receptor by GABA allows chloride ions to flow into neurons, hyperpolarizing the neuron membrane and inhibiting action potential firing. The alpha 1 subunit is crucial for the sedative/hypnotic effects of benzodiazepines and is a primary target of Z-drugs for sleep aids. Dysfunctions or mutations in GABRA1 have been linked to epilepsy syndromes.

Other names
GABA A Receptor Alpha1 SubunitGABA(A) Receptor Alpha 1Gamma-aminobutyric acid receptor subunit alpha-1
02

Mechanism of action

Binding to the GABA-A receptor, enhancing GABA-mediated chloride ion influx, leading to neuronal hyperpolarization and inhibition of neuronal firing.

03

Biological functions

Inhibitory neurotransmissionNeuronal excitability regulationSynaptic transmissionChloride ion conductance
04

Disease associations

EpilepsyAnxiety disordersSleep disordersNeurodevelopmental disorders
05

Safety considerations

ToleranceDependenceWithdrawal symptomsRespiratory depression (with high doses or in combination with other CNS depressants)Cognitive impairment
06

Interacting drugs

GABA

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