Alpha-2A adrenergic receptor
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| Location (UCSC) | Chr 10: 111.08 – 111.08 Mb | Chr 19: 54.03 – 54.04 Mb | |||||||
| PubMed search | [3] | [4] | |||||||
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The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an
human gene encoding it.[5]
Receptor
α2 adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating
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[6]
Gene
This gene encodes α2A subtype and it contains no
untranslated sequences.[5]
Ligands
Agonists
- 4-NEMD
- Brimonidine
- Clonidine
- Dexmedetomidine
- Guanfacine
- Lofexidine
- Myrcene
- Medetomidine
- PS75[7]
- Tizanidine
- Xylazine
Antagonists
- Idazoxan
- )
- Asenapine
- BRL-44408
- Clozapine
- Lurasidone
- Mianserin
- Mirtazapine
- Paliperidone
- Risperidone
- Yohimbine
See also
References
- ^ a b c GRCh38: Ensembl release 89: ENSG00000150594 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000033717 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ a b "Entrez Gene: ADRA2A adrenergic, alpha-2A-, receptor".
- S2CID 205047992.
- PMID 36173843.
External links
- "α2A-adrenoceptor". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2015-04-02. Retrieved 2008-11-25.
- 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
- Perälä M, Hirvonen H, Kalimo H, Ala-Uotila S, Regan JW, Akerman KE, Scheinin M (Nov 1992). "Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues". Brain Research. Molecular Brain Research. 16 (1–2): 57–63. PMID 1334200.
- Surprenant A, Horstman DA, Akbarali H, Limbird LE (Aug 1992). "A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents". Science. 257 (5072): 977–80. PMID 1354394.
- Handy DE, Gavras H (Nov 1992). "Promoter region of the human alpha 2A adrenergic receptor gene". The Journal of Biological Chemistry. 267 (33): 24017–22. PMID 1385431.
- Suryanarayana S, Daunt DA, Von Zastrow M, Kobilka BK (Aug 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". The Journal of Biological Chemistry. 266 (23): 15488–92. PMID 1678390.
- Wang CD, Buck MA, Fraser CM (Aug 1991). "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. PMID 1678850.
- Chhajlani V, Rangel N, Uhlén S, Wikberg JE (Mar 1991). "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. S2CID 26642747.
- Guyer CA, Horstman DA, Wilson AL, Clark JD, Cragoe EJ, Limbird LE (Oct 1990). "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. PMID 2170371.
- Fraser CM, Arakawa S, McCombie WR, Venter JC (Jul 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". The Journal of Biological Chemistry. 264 (20): 11754–61. PMID 2568356.
- Kobilka BK, Matsui H, Kobilka TS, Yang-Feng TL, Francke U, Caron MG, Lefkowitz RJ, Regan JW (Oct 1987). "Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor". Science. 238 (4827): 650–6. PMID 2823383.
- Lynch CJ, Steer ML (Apr 1981). "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. PMID 6259160.
- Eason MG, Moreira SP, Liggett SB (Mar 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". The Journal of Biological Chemistry. 270 (9): 4681–8. PMID 7876239.
- Grassie MA, Milligan G (Mar 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". The Biochemical Journal. 306 (Pt 2): 525–30. PMID 7887906.
- Shilo L, Sakaue M, Thomas JM, Philip M, Hoffman BB (Jan 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". Cellular Signalling. 6 (1): 73–82. PMID 8011430.
- Valet P, Senard JM, Devedjian JC, Planat V, Salomon R, Voisin T, Drean G, Couvineau A, Daviaud D, Denis C (May 1993). "Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa". The Journal of Clinical Investigation. 91 (5): 2049–57. PMID 8098045.
- Alblas J, van Corven EJ, Hordijk PL, Milligan G, Moolenaar WH (Oct 1993). "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. PMID 8226727.
- Klein U, Ramirez MT, Kobilka BK, von Zastrow M (Aug 1997). "A novel interaction between adrenergic receptors and the alpha-subunit of eukaryotic initiation factor 2B". The Journal of Biological Chemistry. 272 (31): 19099–102. PMID 9235896.
- Bétuing S, Daviaud D, Pagès C, Bonnard E, Valet P, Lafontan M, Saulnier-Blache JS (Jun 1998). "Gbeta gamma-independent coupling of alpha2-adrenergic receptor to p21(rhoA) in preadipocytes". The Journal of Biological Chemistry. 273 (25): 15804–10. PMID 9624180.
- Prezeau L, Richman JG, Edwards SW, Limbird LE (May 1999). "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. PMID 10224112.
- Hein L, Altman JD, Kobilka BK (Nov 1999). "Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission". Nature. 402 (6758): 181–4. S2CID 205047992.
- Schaak S, Cussac D, Cayla C, Devedjian JC, Guyot R, Paris H, Denis C (Aug 2000). "Alpha(2) adrenoceptors regulate proliferation of human intestinal epithelial cells". Gut. 47 (2): 242–50. PMID 10896916.
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