Biology:GABRA5

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Short description: Protein-coding gene in the species Homo sapiens


A representation of the 3D structure of the protein myoglobin showing turquoise α-helices.
Generic protein structure example

Gamma-aminobutyric acid (GABA) A receptor, alpha 5, also known as GABRA5, is a protein which in humans is encoded by the GABRA5 gene.[1][2]

Function

GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABAA receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABAA receptor. At least 16 distinct subunits of GABAA receptors have been identified. Transcript variants utilizing three different alternative non-coding first exons have been described.[1]

Subunit selective ligands

Recent research has produced several ligands which are moderately selective for GABAA 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

Antagonists

See also

References

  1. ↑ 1.0 1.1 "Entrez Gene: GABRA5 gamma-aminobutyric acid (GABA) A receptor, alpha 5". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2558. 
  2. ↑ "Cloning and expression of a cDNA encoding the human GABA-A receptor alpha 5 subunit". Biochem. Soc. Trans. 20 (1): 18S. February 1992. doi:10.1042/bst020018s. PMID 1321750. 
  3. ↑ McCabe, L. L.; McCabe, E. R. B. (2013). "Down syndrome and personalized medicine: Changing paradigms from genotype to phenotype to treatment". Congenital Anomalies 53 (1): 1–2. doi:10.1111/cga.12000. PMID 23480351. 
  4. ↑ "PWZ-029, a compound with moderate inverse agonist functional selectivity at GABA(A) receptors containing alpha5 subunits, improves passive, but not active, avoidance learning in rats". Brain Res. 1208: 150–159. 2008. doi:10.1016/j.brainres.2008.02.020. PMID 18394590. 
  5. ↑ "A new pyridazine series of GABAA alpha5 ligands". J. Med. Chem. 48 (19): 6004–6011. 2005. doi:10.1021/jm050249x. PMID 16162003. 
  6. ↑ "RO4938581, a novel cognitive enhancer acting at GABA(A) alpha5 subunit-containing receptors". Psychopharmacology 202 (1–3): 207–223. 2008. doi:10.1007/s00213-008-1357-7. PMID 18936916. 
  7. ↑ "6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists". J. Med. Chem. 45 (6): 1176–1179. 2002. doi:10.1021/jm010471b. PMID 11881985. 
  8. ↑ "Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition". J. Med. Chem. 46 (11): 2227–2240. 2003. doi:10.1021/jm020582q. PMID 12747794. 

Further reading

External links

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

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See also
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