Biology:Alpha-2A adrenergic receptor

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

Generic protein structure example

The alpha-2A adrenergic receptor (α_2A adrenoceptor), also known as ADRA2A, is an α₂ adrenergic receptor, and also denotes the human gene encoding it.

Receptor

α₂ adrenergic receptors include 3 highly homologous subtypes: α_2A, α_2B, and α_2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mice revealed that both the α_2A and α_2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the α_2A subtype inhibited transmitter release at high stimulation frequencies, whereas the α_2C subtype modulated neurotransmission at lower levels of nerve activity

Gene

This gene encodes α_2A subtype and it contains no introns in either its coding or untranslated sequences.

Ligands

Agonists

• 4-NEMD
• Brimonidine
• Clonidine
• Dexmedetomidine
• Guanfacine
• Lofexidine
• Myrcene
• Medetomidine
• PS75
• Tizanidine
• Xylazine

Antagonists

• Idazoxan
• 1-PP (active metabolite of buspirone and gepirone)
• Asenapine
• BRL-44408
• Clozapine
• Lurasidone
• Mianserin
• Mirtazapine
• Paliperidone
• Risperidone
• Yohimbine

See also

• Adrenergic receptor

External links

• "α_2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2181. 
• Human ADRA2A genome location and ADRA2A gene details page in the UCSC Genome Browser.
• Human ZNF32 genome location and ZNF32 gene details page in the UCSC Genome Browser.

Further reading

• "Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues". Brain Research. Molecular Brain Research 16 (1–2): 57–63. Nov 1992. doi:10.1016/0169-328X(92)90193-F. PMID 1334200. 
• "A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents". Science 257 (5072): 977–80. Aug 1992. doi:10.1126/science.1354394. PMID 1354394. Bibcode: 1992Sci...257..977S. 
• "Promoter region of the human alpha 2A adrenergic receptor gene". The Journal of Biological Chemistry 267 (33): 24017–22. Nov 1992. doi:10.1016/S0021-9258(18)35938-6. PMID 1385431. 
• "A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists". The Journal of Biological Chemistry 266 (23): 15488–92. Aug 1991. doi:10.1016/S0021-9258(18)98642-4. PMID 1678390. 
• "Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists". Molecular Pharmacology 40 (2): 168–79. Aug 1991. PMID 1678850. 
• "Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR". FEBS Letters 280 (2): 241–4. Mar 1991. doi:10.1016/0014-5793(91)80301-I. PMID 1849485. 
• "Cloning, sequencing, and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride analogs". The Journal of Biological Chemistry 265 (28): 17307–17. Oct 1990. doi:10.1016/S0021-9258(17)44904-0. PMID 2170371. 
• "Cloning, sequence analysis, and permanent expression of a human alpha 2-adrenergic receptor in Chinese hamster ovary cells. Evidence for independent pathways of receptor coupling to adenylate cyclase attenuation and activation". The Journal of Biological Chemistry 264 (20): 11754–61. Jul 1989. doi:10.1016/S0021-9258(18)80130-2. PMID 2568356. 
• "Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor". Science 238 (4827): 650–6. Oct 1987. doi:10.1126/science.2823383. PMID 2823383. Bibcode: 1987Sci...238..650K. 
• "Evidence for high and low affinity alpha 2-receptors. Comparison of [3H]norepinephrine and [3H]phentolamine binding to human platelet membranes". The Journal of Biological Chemistry 256 (7): 3298–303. Apr 1981. doi:10.1016/S0021-9258(19)69606-7. PMID 6259160. 
• "Four consecutive serines in the third intracellular loop are the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor". The Journal of Biological Chemistry 270 (9): 4681–8. Mar 1995. doi:10.1074/jbc.270.9.4681. PMID 7876239. 
• "Analysis of the relative interactions between the alpha 2C10 adrenoceptor and the guanine-nucleotide-binding proteins G(o)1 alpha and Gi 2 alpha following co-expression of these polypeptides in rat 1 fibroblasts". The Biochemical Journal 306 (Pt 2): 525–30. Mar 1995. doi:10.1042/bj3060525. PMID 7887906. 
• "Enhanced transcription of the human alpha 2A-adrenergic receptor gene by cAMP: evidence for multiple cAMP responsive sequences in the promoter region of this gene". Cellular Signalling 6 (1): 73–82. Jan 1994. doi:10.1016/0898-6568(94)90062-0. PMID 8011430. 
• "Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa". The Journal of Clinical Investigation 91 (5): 2049–57. May 1993. doi:10.1172/JCI116427. PMID 8098045. 
• "Gi-mediated activation of the p21ras-mitogen-activated protein kinase pathway by alpha 2-adrenergic receptors expressed in fibroblasts". The Journal of Biological Chemistry 268 (30): 22235–8. Oct 1993. doi:10.1016/S0021-9258(18)41514-1. PMID 8226727. 
• "A novel interaction between adrenergic receptors and the alpha-subunit of eukaryotic initiation factor 2B". The Journal of Biological Chemistry 272 (31): 19099–102. Aug 1997. doi:10.1074/jbc.272.31.19099. PMID 9235896. 
• "Gbeta gamma-independent coupling of alpha2-adrenergic receptor to p21(rhoA) in preadipocytes". The Journal of Biological Chemistry 273 (25): 15804–10. Jun 1998. doi:10.1074/jbc.273.25.15804. PMID 9624180. http://www.hal.inserm.fr/inserm-00110175/document. 
• "The zeta isoform of 14-3-3 proteins interacts with the third intracellular loop of different alpha2-adrenergic receptor subtypes". The Journal of Biological Chemistry 274 (19): 13462–9. May 1999. doi:10.1074/jbc.274.19.13462. PMID 10224112. 
• "Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission". Nature 402 (6758): 181–4. Nov 1999. doi:10.1038/46040. PMID 10647009. Bibcode: 1999Natur.402..181H. 
• "Alpha(2) adrenoceptors regulate proliferation of human intestinal epithelial cells". Gut 47 (2): 242–50. Aug 2000. doi:10.1136/gut.47.2.242. PMID 10896916.