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.^[5][6]

GABRA5
Identifiers
Aliases	GABRA5, gamma-aminobutyric acid type A receptor alpha5 subunit, EIEE79, gamma-aminobutyric acid type A receptor subunit alpha5, DEE79
External IDs	OMIM: 137142; MGI: 95617; HomoloGene: 20219; GeneCards: GABRA5; OMA:GABRA5 - orthologs
Gene location (Human) Chr. Chromosome 15 (human)[1] Band 15q12 Start 26,866,911 bp[1] End 26,949,208 bp[1]
Gene location (Mouse) Chr. Chromosome 7 (mouse)[2] Band 7 B5|7 33.52 cM Start 57,057,420 bp[2] End 57,159,807 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in nucleus accumbens prefrontal cortex Brodmann area 10 cingulate gyrus anterior cingulate cortex orbitofrontal cortex dorsolateral prefrontal cortex hippocampus proper Region I of hippocampus proper Brodmann area 9 Top expressed in subdivision of hippocampus Region I of hippocampus proper hippocampus proper Subplate dentate gyrus dentate gyrus of hippocampal formation granule cell ventromedial nucleus lumbar subsegment of spinal cord subiculum arcuate nucleus More reference expression data BioGPS n/a
Gene ontology Molecular function GABA-A receptor activity transporter activity ion channel activity chloride channel activity extracellular ligand-gated ion channel activity transmembrane signaling receptor activity signaling receptor activity GABA receptor binding inhibitory extracellular ligand-gated ion channel activity benzodiazepine receptor activity GABA-gated chloride ion channel activity transmitter-gated ion channel activity involved in regulation of postsynaptic membrane potential Cellular component integral component of membrane cell body GABA-A receptor complex postsynaptic membrane membrane receptor complex synapse integral component of plasma membrane chloride channel complex neuronal cell body membrane dendrite nucleoplasm cytosol plasma membrane cell junction GABA-ergic synapse integral component of postsynaptic membrane integral component of presynaptic membrane integral component of postsynaptic specialization membrane dendrite membrane neuron projection postsynapse Biological process gamma-aminobutyric acid signaling pathway negative regulation of neuron apoptotic process cochlea development associative learning regulation of neuron apoptotic process neuron development chloride transmembrane transport hearing ion transport behavioral fear response brain development inner ear receptor cell development chloride transport innervation signal transduction chemical synaptic transmission ion transmembrane transport regulation of membrane potential nervous system process synaptic transmission, GABAergic regulation of postsynaptic membrane potential Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 2558 110886 Ensembl ENSG00000186297 ENSMUSG00000055078 UniProt P31644 Q8BHJ7 RefSeq (mRNA) NM_000810 NM_001165037 NM_176942 NM_001362161 NM_001362162 RefSeq (protein) NP_000801 NP_001158509 NP_795916 NP_001349090 NP_001349091 Location (UCSC) Chr 15: 26.87 – 26.95 Mb Chr 7: 57.06 – 57.16 Mb PubMed search [3] [4]
Wikidata
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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.^[5]

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

Antagonists

• 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.^[7]
• L-655,708
• MRK-016
• PWZ-029: moderate inverse agonist^[8]
• Pyridazines^[9]
• Ro4938581^[10]
• TB-21007^[11][12]

See also

• GABA_A receptor