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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]
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]
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]
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]
References
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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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31. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A. (2002) Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther, 303: 791-804. [PMID:12388666]
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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 |
How to cite this family page
Database page citation:
Raul R. Gainetdinov, Jean-Martin Beaulieu, Emiliana Borrelli, Arvid Carlsson, Marc G. Caron, Olivier Civelli, Stefano Espinoza, Gilberto Fisone, David K. Grandy, John W. Kebabian, Saloman Z. Langer, Maria Cristina Missale, Kim A. Neve, Bernard Scatton, Jean-Charles Schwartz, Goran Sedvall, Philip Seeman, David R. Sibley, Pierre Sokoloff, Pierre F. Spano, Hubert H. M. Van Tol. Dopamine receptors. Accessed on 18/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=20.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: G protein-coupled receptors. Br J Pharmacol. 174 Suppl 1: S17-S129.
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.