Target intelligence / Profile preview

Gamma-aminobutyric acid A receptor alpha 5 subunit (GABRA5)

Target
GABRA5
Molecular classification
Ligand-gated ion channel, GABA receptor subunit, Receptor
01

Overview

The gamma-aminobutyric acid (GABA) A receptor alpha 5 subunit (GABRA5) is a subunit of the GABA(A) receptor, the primary mediator of fast inhibitory neurotransmission in the mammalian central nervous system. α5-containing GABA(A) receptors are predominantly found extrasynaptically in the hippocampus and contribute significantly to tonic inhibition. Activated by GABA, these receptors open their chloride channel pore, allowing Cl⁻ ions to flow into neurons, hyperpolarizing the cell membrane and reducing neuronal excitability. Altered function or expression of α5-containing GABA(A) receptors has been implicated in various neurological conditions, making it a target for nootropics and cognitive disorder therapies.

02

Mechanism of action

Allosteric modulation of chloride channel opening probability

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Biological functions

Inhibitory neurotransmissionRegulation of neuronal excitabilityLearning and memory processesTonic inhibition
04

Disease associations

Down syndrome-related cognitive deficitsSchizophrenia spectrum disordersEpilepsyAlzheimer's disease
05

Safety considerations

Cognitive impairmentAnterograde amnesia
06

Interacting drugs

Benzodiazepines

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