GABRA5

Gamma-aminobutyric acid (GABA) A receptor, alpha 5, also known as GABRA5, is a protein which in humans is encoded by the GABRA5 gene.

Function

GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA_A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA_A receptor. At least 16 distinct subunits of GABA_A receptors have been identified. Transcript variants utilizing three different alternative non-coding first exons have been described.

Subunit selective ligands

Recent research has produced several ligands which are moderately selective for GABA_A receptors containing the α₅ subunit. These have proved to be useful in investigating some of the side effects of benzodiazepine and nonbenzodiazepine drugs, particularly the effects on learning and memory such as anterograde amnesia. Inverse agonists at this subunit have nootropic effects and may be useful for the treatment of cognitive disorders such as Alzheimer's disease.

Agonists

• QH-ii-066
• SH-053-R-CH3-2′F

Inverse agonists

• α₅IA
• Basmisanil (RG-1662, RO5186582): derivative of Ro4938581, negative allosteric modulator at GABA_A α₅, in human trials for treating cognitive deficit in Down syndrome.
• L-655,708
• MRK-016
• PWZ-029: moderate inverse agonist
• Pyridazines
• Ro4938581
• TB-21007

See also

• GABA_A receptor

External links

• GABRA5 protein, human at the US National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.