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Dopamine receptors C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Overview
Receptors
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D1 receptor
C
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D2 receptor
C
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D3 receptor
C
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D4 receptor
C
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D5 receptor
C
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Further reading
* Key recommended reading is highlighted with an asterisk
* Beaulieu JM, Espinoza S, Gainetdinov RR. (2015) Dopamine receptors - IUPHAR Review 13. Br J Pharmacol, 172 (1): 1-23. [PMID:25671228]
* Beaulieu JM, Gainetdinov RR. (2011) The physiology, signaling, and pharmacology of dopamine receptors. Pharmacol Rev, 63 (1): 182-217. [PMID:21303898]
Björklund A, Dunnett SB. (2007) Dopamine neuron systems in the brain: an update. Trends Neurosci, 30 (5): 194-202. [PMID:17408759]
Björklund A, Dunnett SB. (2007) Fifty years of dopamine research. Trends Neurosci, 30 (5): 185-7. [PMID:17397938]
Carlsson A, Carlsson ML. (2008) Adaptive properties and heterogeneity of dopamine D(2) receptors - pharmacological implications. Brain Res Rev, 58 (2): 374-8. [PMID:18511124]
* Cumming P. (2011) Absolute abundances and affinity states of dopamine receptors in mammalian brain: A review. Synapse, 65 (9): 892-909. [PMID:21308799]
De Mei C, Ramos M, Iitaka C, Borrelli E. (2009) Getting specialized: presynaptic and postsynaptic dopamine D2 receptors. Curr Opin Pharmacol, 9 (1): 53-8. [PMID:19138563]
Giorgioni G, Piergentili A, Ruggieri S, Quaglia W. (2008) Dopamine D5 receptors: a challenge to medicinal chemists. Mini Rev Med Chem, 8 (10): 976-95. [PMID:18782049]
Hasbi A, O'Dowd BF, George SR. (2010) Heteromerization of dopamine D2 receptors with dopamine D1 or D5 receptors generates intracellular calcium signaling by different mechanisms. Curr Opin Pharmacol, 10 (1): 93-9. [PMID:19897420]
Hoebel BG, Avena NM, Rada P. (2007) Accumbens dopamine-acetylcholine balance in approach and avoidance. Curr Opin Pharmacol, 7 (6): 617-27. [PMID:18023617]
Horowski R. (2007) A history of dopamine agonists. From the physiology and pharmacology of dopamine to therapies for prolactinomas and Parkinson's disease - a subjective view. J Neural Transm, 114 (1): 127-34. [PMID:16897593]
Iversen SD, Iversen LL. (2007) Dopamine: 50 years in perspective. Trends Neurosci, 30 (5): 188-93. [PMID:17368565]
Joyce JN, Millan MJ. (2007) Dopamine D3 receptor agonists for protection and repair in Parkinson's disease. Curr Opin Pharmacol, 7 (1): 100-5. [PMID:17174156]
Le Foll B, Gallo A, Le Strat Y, Lu L, Gorwood P. (2009) Genetics of dopamine receptors and drug addiction: a comprehensive review. Behav Pharmacol, 20 (1): 1-17. [PMID:19179847]
Maggio R, Millan MJ. (2010) Dopamine D2-D3 receptor heteromers: pharmacological properties and therapeutic significance. Curr Opin Pharmacol, 10 (1): 100-7. [PMID:19896900]
* Moritz AE, Free RB, Sibley DR. (2018) Advances and challenges in the search for D2 and D3 dopamine receptor-selective compounds. Cell Signal, 41: 75-81. [PMID:28716664]
Ohara K. (2007) The n-3 polyunsaturated fatty acid/dopamine hypothesis of schizophrenia. Prog Neuropsychopharmacol Biol Psychiatry, 31 (2): 469-74. [PMID:17184889]
Ptácek R, Kuzelová H, Stefano GB. (2011) Dopamine D4 receptor gene DRD4 and its association with psychiatric disorders. Med Sci Monit, 17 (9): RA215-20. [PMID:21873960]
Reiner-Link D, Madsen JS, Gloriam DE, Bräuner-Osborne H, Hauser AS. (2024) Differential G protein activation by the long and short isoforms of the dopamine D2 receptor. Br J Pharmacol, [Epub ahead of print]. [PMID:38725357]
Rollo CD. (2009) Dopamine and aging: intersecting facets. Neurochem Res, 34 (4): 601-29. [PMID:18841466]
Rolls ET, Loh M, Deco G, Winterer G. (2008) Computational models of schizophrenia and dopamine modulation in the prefrontal cortex. Nat Rev Neurosci, 9 (9): 696-709. [PMID:18714326]
Rondou P, Haegeman G, Van Craenenbroeck K. (2010) The dopamine D4 receptor: biochemical and signalling properties. Cell Mol Life Sci, 67 (12): 1971-86. [PMID:20165900]
Schwartz J-C et al.. (1998) Dopamine Receptors. In The IUPHAR Compendium of Receptor Characterization and Classification Edited by Girdlestone D (IUPHAR Media) 141-151.
Scott L, Aperia A. (2009) Interaction between N-methyl-D-aspartic acid receptors and D1 dopamine receptors: an important mechanism for brain plasticity. Neuroscience, 158 (1): 62-6. [PMID:19000746]
Stanwood GD. (2008) Protein-protein interactions and dopamine D2 receptor signaling: a calcium connection. Mol Pharmacol, 74 (2): 317-9. [PMID:18511653]
Thomas MJ, Kalivas PW, Shaham Y. (2008) Neuroplasticity in the mesolimbic dopamine system and cocaine addiction. Br J Pharmacol, 154 (2): 327-42. [PMID:18345022]
Undieh AS. (2010) Pharmacology of signaling induced by dopamine D(1)-like receptor activation. Pharmacol Ther, 128 (1): 37-60. [PMID:20547182]
* Urs NM, Peterson SM, Caron MG. (2017) New Concepts in Dopamine D2 Receptor Biased Signaling and Implications for Schizophrenia Therapy. Biol Psychiatry, 81 (1): 78-85. [PMID:27832841]
Wood MD, Wren PB. (2008) Serotonin-dopamine interactions: implications for the design of novel therapeutic agents for psychiatric disorders. Prog Brain Res, 172: 213-30. [PMID:18772035]
* Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP et al.. (2021) Structural insights into the human D1 and D2 dopamine receptor signaling complexes. Cell, 184 (4): 931-942.e18. [PMID:33571431]
References
1. Akunne HC, Towers P, Ellis GJ, Dijkstra D, Wikström H, Heffner TG, Wise LD, Pugsley TA. (1995) Characterization of binding of [3H]PD 128907, a selective dopamine D3 receptor agonist ligand, to CHO-K1 cells. Life Sci, 57 (15): 1401-10. [PMID:7674830]
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4. Auerbach SS, DrugMatrix® and ToxFX® Coordinator National Toxicology Program. National Toxicology Program: Dept of Health and Human Services. Accessed on 02/05/2014. Modified on 02/05/2014. DrugMatrix, https://ntp.niehs.nih.gov/drugmatrix/index.html
5. Berry CB, Bubser M, Jones CK, Hayes JP, Wepy JA, Locuson CW, Daniels JS, Lindsley CW, Hopkins CR. (2014) Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity. ACS Med Chem Lett, 5 (9): 1060-4. [PMID:25221667]
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9. Conroy JL, Free RB, Sibley DR. (2015) Identification of G protein-biased agonists that fail to recruit β-arrestin or promote internalization of the D1 dopamine receptor. ACS Chem Neurosci, 6 (4): 681-92. [PMID:25660762]
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11. Dijkstra D, Rodenhuis N, Vermeulen ES, Pugsley TA, Wise LD, Wikström HV. (2002) Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety. J Med Chem, 45 (14): 3022-31. [PMID:12086487]
12. Free RB, Chun LS, Moritz AE, Miller BN, Doyle TB, Conroy JL, Padron A, Meade JA, Xiao J, Hu X et al.. (2014) Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol, 86 (1): 96-105. [PMID:24755247]
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28. McCall RB, Lookingland KJ, Bédard PJ, Huff RM. (2005) Sumanirole, a highly dopamine D2-selective receptor agonist: in vitro and in vivo pharmacological characterization and efficacy in animal models of Parkinson's disease. J Pharmacol Exp Ther, 314 (3): 1248-56. [PMID:15980060]
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NC-IUPHAR subcommittee and family contributors
Subcommittee members:
Raul R. Gainetdinov (Chairperson)
Jean-Martin Beaulieu
Emiliana Borrelli
Marc G. Caron
Gilberto Fisone
David K. Grandy
Maria Cristina Missale
Kim A. Neve (Past chairperson)
David R. Sibley
Pierre Sokoloff
Arvid Carlsson (Past contributor)
Olivier Civelli (Past contributor)
John W. Kebabian (Past contributor)
Saloman Z. Langer (Past contributor)
Bernard Scatton (Past contributor)
Jean-Charles Schwartz (Past chairperson)
Goran Sedvall (Past contributor)
Philip Seeman (Past contributor)
Pierre F. Spano (Past contributor)
Hubert H. M. Van Tol (Past contributor) |
Other contributors:
Stefano Espinoza |
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Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.
The selectivity of many of these agents is less than two orders of magnitude. [3H]Raclopride exhibits similar high affinity for D2 and D3 receptors (low affinity for D4), but has been used to label D2 receptors in the presence of a D3-selective antagonist. [3H]7-OH-DPAT has similar affinity for D2 and D3 receptors, but labels only D3 receptors in the absence of divalent cations. The pharmacological profile of the D5 receptor is similar to, yet distinct from, that of the D1 receptor. The splice variants of the D2 receptor are commonly termed D2S and D2L (short and long). The DRD4 gene encoding the D4 receptor is highly polymorphic in humans, with allelic variations of the protein from amino acid 387 to 515.