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词条 Alpha-2A adrenergic receptor
释义

  1. Receptor

  2. Gene

  3. Role in central nervous system

  4. Ligands

     Agonists  Antagonists 

  5. See also

  6. References

  7. External links

  8. Further reading

{{Infobox_gene}}

The alpha-2A adrenergic receptor (α2A 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 [1]

Gene

This gene encodes α2A subtype and it contains no introns in either its coding or untranslated sequences.[2]

Role in central nervous system

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-synaptically to noradrenergic terminals{{Citation needed|date=September 2011}}, 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

Agonists

  • Clonidine
  • Lofexidine
  • Dexmedetomidine
  • Guanfacine
  • Myrcene

Antagonists

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

See also

  • Adrenergic receptor

References

1. ^{{Cite journal | doi=10.1038/46040|pmid = 10647009| title=Two functionally distinct α2-adrenergic receptors regulate sympathetic neurotransmission| journal=Nature| volume=402| issue=6758| pages=181–184| year=1999| last1=Hein| first1=Lutz| last2=Altman| first2=John D.| last3=Kobilka| first3=Brian K.}}
2. ^1 {{cite web | title = Entrez Gene: ADRA2A adrenergic, alpha-2A-, receptor| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=150| accessdate = }}

External links

  • {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2181 | title = α2A-adrenoceptor | accessdate = | author = | authorlink = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }}
  • {{UCSC gene info|ADRA2A}}
  • {{UCSC gene info|ZNF32}}

Further reading

{{refbegin | 2}}
  • {{cite journal | vauthors = Perälä M, Hirvonen H, Kalimo H, Ala-Uotila S, Regan JW, Akerman KE, Scheinin M | title = Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues | journal = Brain Research. Molecular Brain Research | volume = 16 | issue = 1–2 | pages = 57–63 | date = Nov 1992 | pmid = 1334200 | doi = 10.1016/0169-328X(92)90193-F }}
  • {{cite journal | vauthors = Surprenant A, Horstman DA, Akbarali H, Limbird LE | title = A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents | journal = Science | volume = 257 | issue = 5072 | pages = 977–80 | date = Aug 1992 | pmid = 1354394 | doi = 10.1126/science.1354394 }}
  • {{cite journal | vauthors = Handy DE, Gavras H | title = Promoter region of the human alpha 2A adrenergic receptor gene | journal = The Journal of Biological Chemistry | volume = 267 | issue = 33 | pages = 24017–22 | date = Nov 1992 | pmid = 1385431 | doi = }}
  • {{cite journal | vauthors = Suryanarayana S, Daunt DA, Von Zastrow M, Kobilka BK | title = A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists | journal = The Journal of Biological Chemistry | volume = 266 | issue = 23 | pages = 15488–92 | date = Aug 1991 | pmid = 1678390 | doi = }}
  • {{cite journal | vauthors = Wang CD, Buck MA, Fraser CM | title = Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists | journal = Molecular Pharmacology | volume = 40 | issue = 2 | pages = 168–79 | date = Aug 1991 | pmid = 1678850 | doi = }}
  • {{cite journal | vauthors = Chhajlani V, Rangel N, Uhlén S, Wikberg JE | title = Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR | journal = FEBS Letters | volume = 280 | issue = 2 | pages = 241–4 | date = Mar 1991 | pmid = 1849485 | doi = 10.1016/0014-5793(91)80301-I }}
  • {{cite journal | vauthors = Guyer CA, Horstman DA, Wilson AL, Clark JD, Cragoe EJ, Limbird LE | title = Cloning, sequencing, and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride analogs | journal = The Journal of Biological Chemistry | volume = 265 | issue = 28 | pages = 17307–17 | date = Oct 1990 | pmid = 2170371 | doi = }}
  • {{cite journal | vauthors = Fraser CM, Arakawa S, McCombie WR, Venter JC | title = 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 | journal = The Journal of Biological Chemistry | volume = 264 | issue = 20 | pages = 11754–61 | date = Jul 1989 | pmid = 2568356 | doi = }}
  • {{cite journal | vauthors = Kobilka BK, Matsui H, Kobilka TS, Yang-Feng TL, Francke U, Caron MG, Lefkowitz RJ, Regan JW | title = Cloning, sequencing, and expression of the gene coding for the human platelet alpha 2-adrenergic receptor | journal = Science | volume = 238 | issue = 4827 | pages = 650–6 | date = Oct 1987 | pmid = 2823383 | doi = 10.1126/science.2823383 }}
  • {{cite journal | vauthors = Lynch CJ, Steer ML | title = Evidence for high and low affinity alpha 2-receptors. Comparison of [3H]norepinephrine and [3H]phentolamine binding to human platelet membranes | journal = The Journal of Biological Chemistry | volume = 256 | issue = 7 | pages = 3298–303 | date = Apr 1981 | pmid = 6259160 | doi = }}
  • {{cite journal | vauthors = Eason MG, Moreira SP, Liggett SB | title = 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 | journal = The Journal of Biological Chemistry | volume = 270 | issue = 9 | pages = 4681–8 | date = Mar 1995 | pmid = 7876239 | doi = 10.1074/jbc.270.9.4681 }}
  • {{cite journal | vauthors = Grassie MA, Milligan G | title = 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 | journal = The Biochemical Journal | volume = 306 | issue = Pt 2 | pages = 525–30 | date = Mar 1995 | pmid = 7887906 | pmc = 1136549 | doi = 10.1042/bj3060525}}
  • {{cite journal | vauthors = Shilo L, Sakaue M, Thomas JM, Philip M, Hoffman BB | title = 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 | journal = Cellular Signalling | volume = 6 | issue = 1 | pages = 73–82 | date = Jan 1994 | pmid = 8011430 | doi = 10.1016/0898-6568(94)90062-0 }}
  • {{cite journal | vauthors = Valet P, Senard JM, Devedjian JC, Planat V, Salomon R, Voisin T, Drean G, Couvineau A, Daviaud D, Denis C | title = Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa | journal = The Journal of Clinical Investigation | volume = 91 | issue = 5 | pages = 2049–57 | date = May 1993 | pmid = 8098045 | pmc = 288203 | doi = 10.1172/JCI116427 }}
  • {{cite journal | vauthors = Alblas J, van Corven EJ, Hordijk PL, Milligan G, Moolenaar WH | title = Gi-mediated activation of the p21ras-mitogen-activated protein kinase pathway by alpha 2-adrenergic receptors expressed in fibroblasts | journal = The Journal of Biological Chemistry | volume = 268 | issue = 30 | pages = 22235–8 | date = Oct 1993 | pmid = 8226727 | doi = }}
  • {{cite journal | vauthors = Klein U, Ramirez MT, Kobilka BK, von Zastrow M | title = A novel interaction between adrenergic receptors and the alpha-subunit of eukaryotic initiation factor 2B | journal = The Journal of Biological Chemistry | volume = 272 | issue = 31 | pages = 19099–102 | date = Aug 1997 | pmid = 9235896 | doi = 10.1074/jbc.272.31.19099 }}
  • {{cite journal | vauthors = Bétuing S, Daviaud D, Pagès C, Bonnard E, Valet P, Lafontan M, Saulnier-Blache JS | title = Gbeta gamma-independent coupling of alpha2-adrenergic receptor to p21(rhoA) in preadipocytes | journal = The Journal of Biological Chemistry | volume = 273 | issue = 25 | pages = 15804–10 | date = Jun 1998 | pmid = 9624180 | doi = 10.1074/jbc.273.25.15804 | url = http://www.hal.inserm.fr/inserm-00110175/document }}
  • {{cite journal | vauthors = Prezeau L, Richman JG, Edwards SW, Limbird LE | title = The zeta isoform of 14-3-3 proteins interacts with the third intracellular loop of different alpha2-adrenergic receptor subtypes | journal = The Journal of Biological Chemistry | volume = 274 | issue = 19 | pages = 13462–9 | date = May 1999 | pmid = 10224112 | doi = 10.1074/jbc.274.19.13462 }}
  • {{cite journal | vauthors = Hein L, Altman JD, Kobilka BK | title = Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission | journal = Nature | volume = 402 | issue = 6758 | pages = 181–4 | date = Nov 1999 | pmid = 10647009 | doi = 10.1038/46040 }}
  • {{cite journal | vauthors = Schaak S, Cussac D, Cayla C, Devedjian JC, Guyot R, Paris H, Denis C | title = Alpha(2) adrenoceptors regulate proliferation of human intestinal epithelial cells | journal = Gut | volume = 47 | issue = 2 | pages = 242–50 | date = Aug 2000 | pmid = 10896916 | pmc = 1728001 | doi = 10.1136/gut.47.2.242 }}
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2 : Adrenergic receptors|Biology of attention deficit hyperactivity disorder
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