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Dopamine receptor D2

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Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the DRD2 gene.

Function Edit

This gene encodes the D2 subtype of the dopamine receptor. This G protein-coupled receptor inhibits adenylyl cyclase activity. A missense mutation in this gene causes myoclonus dystonia; other mutations have been associated with schizophrenia.[1]

Alternative splicing of this gene results in two transcript variants encoding different isoforms. A third variant has been described, but it has not been determined whether this form is normal or due to aberrant splicing.[2]

Genetics Edit

Allelic variants:

Some researchers have previously associated the polymorphism Taq 1A (rs1800497) to the DRD2 gene. However, the polymorphism sits in exon 8 of the ANKK1 gene.[6]

Ligands Edit

Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D2 receptor, but are, in general, very unselective, at best selective only for the "D2-like family" receptors and so binding to D2, D3 and D4, and often also to many other receptors such as those for serotonin and histamine, resulting in a range of side-effects and making them poor agents for scientific research. In similar manner, older dopamine agonists used for Parkinson's disease such as bromocriptine and cabergoline are poorly selective for one dopamine receptor over another, and, although most of these agents do act as D2 agonists, they affect other subtypes as well. Several selective D2 ligands are, however, now available, and this number is likely to increase as further research progresses.

AgonistsEdit

AntagonistsEdit

D2Sh selective (presynaptic autoreceptors)

InteractionsEdit

Dopamine receptor D2 has been shown to interact with Adenosine A2A receptor,[12] EPB41L1[13] and PPP1R9B.[14]

See alsoEdit

ReferencesEdit

  1. Gene Overview of All Published Schizophrenia-Association Studies for DRD2. Schizophrenia Research Forum. URL accessed on 2009-06-09.
  2. Entrez Gene: DRD2 dopamine receptor D2.
  3. Duan J, Wainwright MS, Comeron JM, Saitou N, Sanders AR, Gelernter J, Gejman PV (February 2003). Synonymous mutations in the human dopamine receptor D2 (DRD2) affect mRNA stability and synthesis of the receptor. Hum. Mol. Genet. 12 (3): 205–16.
  4. Arinami T, Gao M, Hamaguchi H, Toru M (April 1997). A functional polymorphism in the promoter region of the dopamine D2 receptor gene is associated with schizophrenia. Hum. Mol. Genet. 6 (4): 577–82.
  5. Glatt SJ, Faraone SV, Tsuang MT (July 2004). DRD2 -141C insertion/deletion polymorphism is not associated with schizophrenia: results of a meta-analysis. Am. J. Med. Genet. B Neuropsychiatr. Genet. 128B (1): 21–3.
  6. Lucht M, Rosskopf D (July 2008). Comment on "Genetically determined differences in learning from errors". Science 321 (5886): 200; author reply 200.
  7. Clinical Pharmacology for Abilify. RxList.com. URL accessed on 2010-01-21.
  8. Holmes IP, Blunt RJ, Lorthioir OE, Blowers SM, Gribble A, Payne AH, Stansfield IG, Wood M, Woollard PM, Reavill C, Howes CM, Micheli F, Di Fabio R, Donati D, Terreni S, Hamprecht D, Arista L, Worby A, Watson SP (March 2010). The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure. Bioorganic & Medicinal Chemistry Letters 20 (6): 2013–6.
  9. Giacomelli S, Palmery M, Romanelli L, Cheng CY, Silvestrini B (1998). Lysergic acid diethylamide (LSD) is a partial agonist of D2 dopaminergic receptors and it potentiates dopamine-mediated prolactin secretion in lactotrophs in vitro. Life Sci. 63 (3): 215–22.
  10. Wang GJ, Volkow ND, Thanos PK, Fowler JS (2004). Similarity between obesity and drug addiction as assessed by neurofunctional imaging: a concept review. J Addict Dis 23 (3): 39–53.
  11. http://ajp.psychiatryonline.org/cgi/content/abstract/156/6/876
  12. Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). Oligomerization of adenosine A2A and dopamine D2 receptors in living cells. Biochem. Biophys. Res. Commun. 306 (2): 544–9.
  13. Binda AV, Kabbani N, Lin R, Levenson R (September 2002). D2 and D3 dopamine receptor cell surface localization mediated by interaction with protein 4.1N. Mol. Pharmacol. 62 (3): 507–13.
  14. Smith FD, Oxford GS, Milgram SL (July 1999). Association of the D2 dopamine receptor third cytoplasmic loop with spinophilin, a protein phosphatase-1-interacting protein. J. Biol. Chem. 274 (28): 19894–900.

Further readingEdit


  • Missale C, Nash SR, Robinson SW, et al. (1998). Dopamine receptors: from structure to function. Physiol. Rev. 78 (1): 189–225.
  • Sidhu A, Niznik HB (2000). Coupling of dopamine receptor subtypes to multiple and diverse G proteins. Int. J. Dev. Neurosci. 18 (7): 669–77.
  • Araki K, Kuwano R, Morii K, et al. (1993). Structure and expression of human and rat D2 dopamine receptor genes. Neurochem. Int. 21 (1): 91–8.
  • Eubanks JH, Djabali M, Selleri L, et al. (1993). Structure and linkage of the D2 dopamine receptor and neural cell adhesion molecule genes on human chromosome 11q23. Genomics 14 (4): 1010–8.
  • Dearry A, Falardeau P, Shores C, Caron MG (1992). D2 dopamine receptors in the human retina: cloning of cDNA and localization of mRNA. Cell. Mol. Neurobiol. 11 (5): 437–53.
  • Sarkar G, Kapelner S, Grandy DK, et al. (1992). Direct sequencing of the dopamine D2 receptor (DRD2) in schizophrenics reveals three polymorphisms but no structural change in the receptor. Genomics 11 (1): 8–14.
  • Stormann TM, Gdula DC, Weiner DM, Brann MR (1990). Molecular cloning and expression of a dopamine D2 receptor from human retina. Mol. Pharmacol. 37 (1): 1–6.
  • Robakis NK, Mohamadi M, Fu DY, et al. (1990). Human retina D2 receptor cDNAs have multiple polyadenylation sites and differ from a pituitary clone at the 5' non-coding region. Nucleic Acids Res. 18 (5): 1299.
  • Selbie LA, Hayes G, Shine J (1990). DNA homology screening: isolation and characterization of the human D2A dopamine receptor subtype. Adv. Second Messenger Phosphoprotein Res. 24: 9–14.
  • Monsma FJ, McVittie LD, Gerfen CR, et al. (1990). Multiple D2 dopamine receptors produced by alternative RNA splicing. Nature 342 (6252): 926–9.
  • Dal Toso R, Sommer B, Ewert M, et al. (1990). The dopamine D2 receptor: two molecular forms generated by alternative splicing. EMBO J. 8 (13): 4025–34.
  • Grandy DK, Marchionni MA, Makam H, et al. (1990). Cloning of the cDNA and gene for a human D2 dopamine receptor. Proc. Natl. Acad. Sci. U.S.A. 86 (24): 9762–6.
  • Selbie LA, Hayes G, Shine J (1990). The major dopamine D2 receptor: molecular analysis of the human D2A subtype. DNA 8 (9): 683–9.
  • Leysen JE, Gommeren W, Mertens J, et al. (1995). Comparison of in vitro binding properties of a series of dopamine antagonists and agonists for cloned human dopamine D2S and D2L receptors and for D2 receptors in rat striatal and mesolimbic tissues, using [125I] 2'-iodospiperone. Psychopharmacology (Berl.) 110 (1–2): 27–36.
  • Itokawa M, Arinami T, Futamura N, et al. (1994). A structural polymorphism of human dopamine D2 receptor, D2(Ser311-->Cys). Biochem. Biophys. Res. Commun. 196 (3): 1369–75.
  • Malmberg A, Jackson DM, Eriksson A, Mohell N (1993). Unique binding characteristics of antipsychotic agents interacting with human dopamine D2A, D2B, and D3 receptors. Mol. Pharmacol. 43 (5): 749–54.
  • Seeman P, Ohara K, Ulpian C, et al. (1993). Schizophrenia: normal sequence in the dopamine D2 receptor region that couples to G-proteins. DNA polymorphisms in D2. Neuropsychopharmacology 8 (2): 137–42.
  • Cravchik A, Sibley DR, Gejman PV (1996). Functional analysis of the human D2 dopamine receptor missense variants. J. Biol. Chem. 271 (42): 26013–7.
  • Ho MK, Wong YH (1997). Functional role of amino-terminal serine16 and serine27 of G alphaZ in receptor and effector coupling. J. Neurochem. 68 (6): 2514–22.



  • Centonze D, Gubellini P, "et al." (2004). Differential contribution of dopamine D2S and D2L receptors in the modulation of glutamate and GABA transmission in the striatum. Neuroscience 129 (1): 157–66.


External links Edit

Template:Transmembranereceptor-stub This article incorporates text from the United States National Library of Medicine, which is in the public domain.


[Category:Dopamine]]

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