D2 receptor

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The correct title of this article is Dopamine receptor D2. It appears incorrectly here because of technical restrictions.
Dopamine receptor D2
Identifiers
Symbols DRD2; D2DR; D2R
External IDs OMIM: 126450 MGI: 94924 HomoloGene: 22561
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 1813 13489
Ensembl ENSG00000149295 ENSMUSG00000032259
Uniprot P14416 Q0VGH9
Refseq NM_000795 (mRNA)
NP_000786 (protein)		 NM_010077 (mRNA)
NP_034207 (protein)
Location Chr 11: 112.79 - 112.85 Mb Chr 9: 49.09 - 49.16 Mb
Pubmed search [1] [2]

Dopamine receptor D2, also known as DRD2, is a protein that is a receptor. The human protein is coded by the DRD2 gene.

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]

Contents

Genetics

Allelic variants:

The polymorphisms has been investigated with respect to association with schizophrenia.[3]

Ligands

Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D2 receptor, but are generally 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. Similarly 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 also affect other subtypes as well. Several selective D2 ligands are however now available, and this number is likely to increase as further research progresses.

Agonists

  • BHT-920 (5,6,7,8-Tetrahydro-6-(2-propen-1-yl)-4H-thiazolo[4,5-d]azepin-2-amine) - selective for D2 over other dopamine receptors, but also acts as α2-adrenoceptor agonist and 5HT3 antagonist.

Antagonists

  • L-741,626 (3-[4-(4-Chlorophenyl)-4-hydroxypiperidin-l-yl]methyl-1H-indole) - highly selective D2 antagonist
  • Melperone - D2 antagonist but also 5HT2A antagonist
  • Risperidone - D2 antagonist but also 5HT2A antagonist
  • Ziprasidone - D2 antagonist but also 5HT2A antagonist

See also

References

  1. ^ Gene Overview of All Published Schizophrenia-Association Studies for DRD2 - Schizophrenia Research Forum SZGene database.
  2. ^ "Entrez Gene: DRD2 dopamine receptor D2".
  3. ^ Stephen J. Glatt, Stephen V. Faraone, Ming T. Tsuang. "DRD2 -141C insertion/deletion polymorphism is not associated with schizophrenia: Results of a meta-analysis". American Journal of Medical Genetics Part B: Neuropsychiatric Genetics 128B (1): 21–23. doi:10.1002/ajmg.b.30007. 

Further reading

  • Missale C, Nash SR, Robinson SW, et al. (1998). "Dopamine receptors: from structure to function.". Physiol. Rev. 78 (1): 189–225. PMID 9457173. 
  • Sidhu A, Niznik HB (2000). "Coupling of dopamine receptor subtypes to multiple and diverse G proteins.". Int. J. Dev. Neurosci. 18 (7): 669–77. PMID 10978845. 
  • 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. PMID 1363862. 
  • 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. PMID 1478642. 
  • 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. PMID 1835903. 
  • 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. PMID 1837284. 
  • 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. PMID 2137193. 
  • 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. PMID 2138729. 
  • 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. PMID 2144985. 
  • Monsma FJ, McVittie LD, Gerfen CR, et al. (1990). "Multiple D2 dopamine receptors produced by alternative RNA splicing.". Nature 342 (6252): 926–9. doi:10.1038/342926a0. PMID 2480527. 
  • 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. PMID 2531656. 
  • 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. PMID 2532362. 
  • Selbie LA, Hayes G, Shine J (1990). "The major dopamine D2 receptor: molecular analysis of the human D2A subtype.". DNA 8 (9): 683–9. PMID 2533064. 
  • 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. PMID 7870895. 
  • 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. doi:10.1006/bbrc.1993.2404. PMID 7902708. 
  • 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. PMID 8099194. 
  • 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. PMID 8471125. 
  • Cravchik A, Sibley DR, Gejman PV (1996). "Functional analysis of the human D2 dopamine receptor missense variants.". J. Biol. Chem. 271 (42): 26013–7. PMID 8824240. 
  • 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. PMID 9166747. 

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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
α1 (A, B, D), α2 (A, B, C), β1, β2, β3
CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin (DP, EP (1, 2, 3, 4), PGF), Prostacyclin, Thromboxane
B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182)
Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - neuromedin (B, U (1, 2)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like
Class C: Metabotropic
glutamate / pheromone
Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened

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