Alpha-2A adrenergic receptor

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Adrenoceptor alpha 2A

PDB rendering based on 1hll.
Available structures
PDB Ortholog search: PDBe, RCSB
Identifiers
Symbols ADRA2A ; ADRA2; ADRA2R; ADRAR; ALPHA2AAR; ZNF32
External IDs OMIM104210 MGI87934 HomoloGene47944 IUPHAR: α2A-adrenoceptor ChEMBL: 1867 GeneCards: ADRA2A Gene
RNA expression pattern
PBB GE ADRA2A 209869 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 150 11551
Ensembl ENSG00000150594 ENSMUSG00000033717
UniProt P08913 Q01338
RefSeq (mRNA) NM_000681 NM_007417
RefSeq (protein) NP_000672 NP_031443
Location (UCSC) Chr 10:
112.84 – 112.84 Mb
Chr 19:
54.05 – 54.05 Mb
PubMed search [1] [2]

The alpha-2A adrenergic receptor2A adrenoceptor), also known as ADRA2A, is an α2 adrenergic receptor, and also denotes the human gene encoding it.[1]

Receptor

α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. 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 α2A and α2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the α2A subtype inhibited transmitter release at high stimulation frequencies, whereas the α2C subtype modulated neurotransmission at lower levels of nerve activity.

Gene

This gene encodes α2A subtype and it contains no introns in either its coding or untranslated sequences.[1]

Role in Central Nervous System[edit]

Although the pre-synaptic functions of α2A receptors have been a major focus (see above), the majority of α2 receptors in the brain are actually localized post-synapticly to noradrenergic terminals[citation needed], and therefore aid in the function of norepinephrine. Many post-synaptic α2A receptors have important effects on brain function; for example, α2A receptors are localized on prefrontal cortical neurons where they regulate higher cognitive function.

Ligands[edit]

Agonists[edit]

Antagonists[edit]

See also[edit]

References[edit]

External links[edit]

  • 2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

Further reading[edit]

  • Perälä M, Hirvonen H, Kalimo H et al. (1993). "Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues". Brain Res. Mol. Brain Res. 16 (1–2): 57–63. doi:10.1016/0169-328X(92)90193-F. PMID 1334200. 
  • Surprenant A, Horstman DA, Akbarali H, Limbird LE (1992). "A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents". Science 257 (5072): 977–80. doi:10.1126/science.1354394. PMID 1354394. 
  • Handy DE, Gavras H (1992). "Promoter region of the human alpha 2A adrenergic receptor gene". J. Biol. Chem. 267 (33): 24017–22. PMID 1385431. 
  • Suryanarayana S, Daunt DA, Von Zastrow M, Kobilka BK (1991). "A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists". J. Biol. Chem. 266 (23): 15488–92. PMID 1678390. 
  • Wang CD, Buck MA, Fraser CM (1991). "Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists". Mol. Pharmacol. 40 (2): 168–79. PMID 1678850. 
  • Chhajlani V, Rangel N, Uhlén S, Wikberg JE (1991). "Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR". FEBS Lett. 280 (2): 241–4. doi:10.1016/0014-5793(91)80301-I. PMID 1849485. 
  • Guyer CA, Horstman DA, Wilson AL et al. (1990). "Cloning, sequencing, and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride analogs". J. Biol. Chem. 265 (28): 17307–17. PMID 2170371. 
  • Fraser CM, Arakawa S, McCombie WR, Venter JC (1989). "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". J. Biol. Chem. 264 (20): 11754–61. PMID 2568356. 
  • Kobilka BK, Matsui H, Kobilka TS et al. (1987). "Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor". Science 238 (4827): 650–6. doi:10.1126/science.2823383. PMID 2823383. 
  • Lynch CJ, Steer ML (1981). "Evidence for high and low affinity alpha 2-receptors. Comparison of [3H]norepinephrine and [3H]phentolamine binding to human platelet membranes". J. Biol. Chem. 256 (7): 3298–303. PMID 6259160. 
  • Eason MG, Moreira SP, Liggett SB (1995). "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". J. Biol. Chem. 270 (9): 4681–8. doi:10.1074/jbc.270.9.4681. PMID 7876239. 
  • Grassie MA, Milligan G (1995). "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". Biochem. J. 306 ( Pt 2) (Pt 2): 525–30. PMC 1136549. PMID 7887906. 
  • Shilo L, Sakaue M, Thomas JM et al. (1994). "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". Cell. Signal. 6 (1): 73–82. doi:10.1016/0898-6568(94)90062-0. PMID 8011430. 
  • Valet P, Senard JM, Devedjian JC et al. (1993). "Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa". J. Clin. Invest. 91 (5): 2049–57. doi:10.1172/JCI116427. PMC 288203. PMID 8098045. 
  • Alblas J, van Corven EJ, Hordijk PL et al. (1993). "Gi-mediated activation of the p21ras-mitogen-activated protein kinase pathway by alpha 2-adrenergic receptors expressed in fibroblasts". J. Biol. Chem. 268 (30): 22235–8. PMID 8226727. 
  • Klein U, Ramirez MT, Kobilka BK, von Zastrow M (1997). "A novel interaction between adrenergic receptors and the alpha-subunit of eukaryotic initiation factor 2B". J. Biol. Chem. 272 (31): 19099–102. doi:10.1074/jbc.272.31.19099. PMID 9235896. 
  • Bétuing S, Daviaud D, Pagès C et al. (1998). "Gbeta gamma-independent coupling of alpha2-adrenergic receptor to p21(rhoA) in preadipocytes". J. Biol. Chem. 273 (25): 15804–10. doi:10.1074/jbc.273.25.15804. PMID 9624180. 
  • Prezeau L, Richman JG, Edwards SW, Limbird LE (1999). "The zeta isoform of 14-3-3 proteins interacts with the third intracellular loop of different alpha2-adrenergic receptor subtypes". J. Biol. Chem. 274 (19): 13462–9. doi:10.1074/jbc.274.19.13462. PMID 10224112. 
  • Hein L, Altman JD, Kobilka BK (2000). "Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission". Nature 402 (6758): 181–4. doi:10.1038/46040. PMID 10647009. 
  • Schaak S, Cussac D, Cayla C et al. (2000). "Alpha2 adrenoceptors regulate proliferation of human intestinal epithelial cells". Gut 47 (2): 242–50. doi:10.1136/gut.47.2.242. PMC 1728001. PMID 10896916.