- Home
- Targets
- G protein-coupled receptors
- Dopamine receptors
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
|
D1 receptor
C
Show summary »« Hide summary
More detailed page
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
D2 receptor
C
Show summary »« Hide summary
More detailed page
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
D3 receptor
C
Show summary »« Hide summary
More detailed page
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
D4 receptor
C
Show summary »« Hide summary
More detailed page
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
D5 receptor
C
Show summary »« Hide summary
More detailed page
|
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]
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]
2. Andersen PH, Jansen JA. (1990) Dopamine receptor agonists: selectivity and dopamine D1 receptor efficacy. Eur J Pharmacol, 188 (6): 335-47. [PMID:1973652]
3. Arnt J, Skarsfeldt T. (1998) Do novel antipsychotics have similar pharmacological characteristics? A review of the evidence. Neuropsychopharmacology, 18 (2): 63-101. [PMID:9430133]
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]
6. Bunzow JR, Van Tol HH, Grandy DK, Albert P, Salon J, Christie M, Machida CA, Neve KA, Civelli O. (1988) Cloning and expression of a rat D2 dopamine receptor cDNA. Nature, 336 (6201): 783-7. [PMID:2974511]
7. Burris KD, Pacheco MA, Filtz TM, Kung MP, Kung HF, Molinoff PB. (1995) Lack of discrimination by agonists for D2 and D3 dopamine receptors. Neuropsychopharmacology, 12 (4): 335-45. [PMID:7576010]
8. Burstein ES, Ma J, Wong S, Gao Y, Pham E, Knapp AE, Nash NR, Olsson R, Davis RE, Hacksell U et al.. (2005) Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist. J Pharmacol Exp Ther, 315 (3): 1278-87. [PMID:16135699]
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]
10. Dearry A, Gingrich JA, Falardeau P, Fremeau Jr RT, Bates MD, Caron MG. (1990) Molecular cloning and expression of the gene for a human D1 dopamine receptor. Nature, 347 (6288): 72-6. [PMID:2144334]
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]
13. Freedman SB, Patel S, Marwood R, Emms F, Seabrook GR, Knowles MR, McAllister G. (1994) Expression and pharmacological characterization of the human D3 dopamine receptor. J Pharmacol Exp Ther, 268 (1): 417-26. [PMID:8301582]
14. Furman CA, Roof RA, Moritz AE, Miller BN, Doyle TB, Free RB, Banala AK, Paul NM, Kumar V, Sibley CD et al.. (2015) Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists. Eur Neuropsychopharmacol, 25 (9): 1448-61. [PMID:25583363]
15. Gregori-Puigjané E, Setola V, Hert J, Crews BA, Irwin JJ, Lounkine E, Marnett L, Roth BL, Shoichet BK. (2012) Identifying mechanism-of-action targets for drugs and probes. Proc Natl Acad Sci USA, 109 (28): 11178-83. [PMID:22711801]
16. Grundt P, Husband SL, Luedtke RR, Taylor M, Newman AH. (2007) Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR. Bioorg Med Chem Lett, 17 (3): 745-9. [PMID:17095222]
17. Grundt P, Prevatt KM, Cao J, Taylor M, Floresca CZ, Choi JK, Jenkins BG, Luedtke RR, Newman AH. (2007) Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents. J Med Chem, 50 (17): 4135-46. [PMID:17672446]
18. Heier RF, Dolak LA, Duncan JN, Hyslop DK, Lipton MF, Martin IJ, Mauragis MA, Piercey MF, Nichols NF, Schreur PJ et al.. (1997) Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites. J Med Chem, 40 (5): 639-46. [PMID:9057850]
19. Hidaka K, Matsumoto M, Tada S, Tasaki Y, Yamaguchi T. (1995) Differential effects of [3H]nemonapride and [3H]spiperone binding on human dopamine D4 receptors. Neurosci Lett, 186 (2-3): 145-8. [PMID:7777184]
20. Hoare SR, Coldwell MC, Armstrong D, Strange PG. (2000) Regulation of human D(1), d(2(long)), d(2(short)), D(3) and D(4) dopamine receptors by amiloride and amiloride analogues. Br J Pharmacol, 130 (5): 1045-59. [PMID:10882389]
21. Kiss B, Horváth A, Némethy Z, Schmidt E, Laszlovszky I, Bugovics G, Fazekas K, Hornok K, Orosz S, Gyertyán I et al.. (2010) Cariprazine (RGH-188), a dopamine D(3) receptor-preferring, D(3)/D(2) dopamine receptor antagonist-partial agonist antipsychotic candidate: in vitro and neurochemical profile. J Pharmacol Exp Ther, 333 (1): 328-40. [PMID:20093397]
22. Kortagere S, Gmeiner P, Weinstein H, Schetz JA. (2004) Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain. Mol Pharmacol, 66 (6): 1491-9. [PMID:15448188]
23. Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL. (2003) H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs. Neuropsychopharmacology, 28 (3): 519-26. [PMID:12629531]
24. Kulagowski JJ, Broughton HB, Curtis NR, Mawer IM, Ridgill MP, Baker R, Emms F, Freedman SB, Marwood R, Patel S et al.. (1996) 3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor. J Med Chem, 39 (10): 1941-2. [PMID:8642550]
25. Köhler C, Hall H, Ogren SO, Gawell L. (1985) Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain. Biochem Pharmacol, 34 (13): 2251-9. [PMID:4015674]
26. Lahti RA, Evans DL, Stratman NC, Figur LM. (1993) Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. Eur J Pharmacol, 236 (3): 483-6. [PMID:8102973]
27. MacKenzie RG, VanLeeuwen D, Pugsley TA, Shih YH, Demattos S, Tang L, Todd RD, O'Malley KL. (1994) Characterization of the human dopamine D3 receptor expressed in transfected cell lines. Eur J Pharmacol, 266 (1): 79-85. [PMID:7907989]
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]
29. Mierau J, Schneider FJ, Ensinger HA, Chio CL, Lajiness ME, Huff RM. (1995) Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. Eur J Pharmacol, 290 (1): 29-36. [PMID:7664822]
30. Millan MJ, Audinot V, Rivet JM, Gobert A, Vian J, Prost JF, Spedding M, Peglion JL. (1994) S 14297, a novel selective ligand at cloned human dopamine D3 receptors, blocks 7-OH-DPAT-induced hypothermia in rats. Eur J Pharmacol, 260 (2-3): R3-5. [PMID:7988633]
31. Millan MJ, Gobert A, Newman-Tancredi A, Lejeune F, Cussac D, Rivet JM, Audinot V, Dubuffet T, Lavielle G. (2000) S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. J Pharmacol Exp Ther, 293 (3): 1048-62. [PMID:10869410]
32. 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 (2): 791-804. [PMID:12388666]
33. Millan MJ, Peglion JL, Vian J, Rivet JM, Brocco M, Gobert A, Newman-Tancredi A, Dacquet C, Bervoets K, Girardon S. (1995) Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: 1. Activation of postsynaptic D3 receptors mediates hypothermia, whereas blockade of D2 receptors elicits prolactin secretion and catalepsy. J Pharmacol Exp Ther, 275: 885-898. [PMID:7473180]
34. Moreland RB, Patel M, Hsieh GC, Wetter JM, Marsh K, Brioni JD. (2005) A-412997 is a selective dopamine D4 receptor agonist in rats. Pharmacol Biochem Behav, 82 (1): 140-7. [PMID:16153699]
35. Nakane M, Cowart MD, Hsieh GC, Miller L, Uchic ME, Chang R, Terranova MA, Donnelly-Roberts DL, Namovic MT, Miller TR et al.. (2005) 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology, 49 (1): 112-21. [PMID:15992586]
36. Nergårdh R, Oerther S, Fredholm BB. (2005) Differences between A 68930 and SKF 82958 could suggest synergistic roles of D1 and D5 receptors. Pharmacol Biochem Behav, 82 (3): 495-505. [PMID:16318870]
37. Ochi T, Sakamoto M, Minamida A, Suzuki K, Ueda T, Une T, Toda H, Matsumoto K, Terauchi Y. (2005) Syntheses and properties of the major hydroxy metabolites in humans of blonanserin AD-5423, a novel antipsychotic agent. Bioorg Med Chem Lett, 15 (4): 1055-9. [PMID:15686911]
38. Patel S, Patel S, Marwood R, Emms F, Marston D, Leeson PD, Curtis NR, Kulagowski JJ, Freedman SB. (1996) Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor. Mol Pharmacol, 50 (6): 1658-64. [PMID:8967990]
39. Primus RJ, Thurkauf A, Xu J, Yevich E, McInerney S, Shaw K, Tallman JF, Gallagher DW. (1997) II. Localization and characterization of dopamine D4 binding sites in rat and human brain by use of the novel, D4 receptor-selective ligand [3H]NGD 94-1. J Pharmacol Exp Ther, 282 (2): 1020-7. [PMID:9262371]
40. Pugsley TA, Davis MD, Akunne HC, MacKenzie RG, Shih YH, Damsma G, Wikstrom H, Whetzel SZ, Georgic LM, Cooke LW et al.. (1995) Neurochemical and functional characterization of the preferentially selective dopamine D3 agonist PD 128907. J Pharmacol Exp Ther, 275 (3): 1355-66. [PMID:8531103]
41. Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J, Coldwell MC et al.. (2000) Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A. J Pharmacol Exp Ther, 294 (3): 1154-65. [PMID:10945872]
42. Ricci A, Amenta F. (1994) Dopamine D5 receptors in human peripheral blood lymphocytes: a radioligand binding study. J Neuroimmunol, 53 (1): 1-7. [PMID:8051291]
43. Ricci A, Veglio F, Amenta F. (1995) Radioligand binding characterization of putative dopamine D3 receptor in human peripheral blood lymphocytes with [3H]7-OH-DPAT. J Neuroimmunol, 58 (2): 139-44. [PMID:7759603]
44. Rowley M, Broughton HB, Collins I, Baker R, Emms F, Marwood R, Patel S, Patel S, Ragan CI, Freedman SB et al.. (1996) 5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors. J Med Chem, 39 (10): 1943-5. [PMID:8642551]
45. Ryman-Rasmussen JP, Griffith A, Oloff S, Vaidehi N, Brown JT, Goddard 3rd WA, Mailman RB. (2007) Functional selectivity of dopamine D1 receptor agonists in regulating the fate of internalized receptors. Neuropharmacology, 52 (2): 562-75. [PMID:17067639]
46. Sautel F, Griffon N, Lévesque D, Pilon C, Schwartz JC, Sokoloff P. (1995) A functional test identifies dopamine agonists selective for D3versus D2receptors. Neuroreport, 6: 329-332. [PMID:7756621]
47. Sautel F, Griffon N, Sokoloff P, Schwartz JC, Launay C, Simon P, Costentin J, Schoenfelder A, Garrido F, Mann A et al.. (1995) Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents. J Pharmacol Exp Ther, 275 (3): 1239-46. [PMID:8531087]
48. Schlachter SK, Poel TJ, Lawson CF, Dinh DM, Lajiness ME, Romero AG, Rees SA, Duncan JN, Smith MW. (1997) Substituted 4-aminopiperidines having high in vitro affinity and selectivity for the cloned human dopamine D4 receptor. Eur J Pharmacol, 322 (2-3): 283-6. [PMID:9098699]
49. Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE. (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl.), 124 (1-2): 57-73. [PMID:8935801]
50. Schwartz JC Carlsson A Caron M Scatton B Civelli O Kebabian JW Langer SZ Sedvall G Seeman P Spano PF Sokoloff P Van Tol H. (1998) Dopamine receptors. In The IUPHAR Compendium of Receptor Characterization and Classification Edited by Girdlestone D (IUPHAR media) 141-151.
51. Seeman P. (2001) Antipsychotic drugs, dopamine receptors, and schizophrenia. Clinical Neuroscience Research, 1 (1-2): 53-60. DOI: 10.1016/S1566-2772(00)00007-4
52. Seeman P, Chau-Wong M, Tedesco J, Wong K. (1975) Brain receptors for antipsychotic drugs and dopamine: direct binding assays. Proc Natl Acad Sci USA, 72 (11): 4376-80. [PMID:1060115]
53. Seeman P, Corbett R, Van Tol HH. (1997) Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Neuropsychopharmacology, 16 (2): 93-110; discussion 111-35. [PMID:9015795]
54. Seeman P, Tallerico T. (1998) Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol Psychiatry, 3 (2): 123-34. [PMID:9577836]
55. Shahid M, Walker GB, Zorn SH, Wong EH. (2009) Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol (Oxford), 23 (1): 65-73. [PMID:18308814]
56. Sokoloff P, Andrieux M, Besançon R, Pilon C, Martres MP, Giros B, Schwartz JC. (1992) Pharmacology of human dopamine D3 receptor expressed in a mammalian cell line: comparison with D2 receptor. Eur J Pharmacol, 225 (4): 331-7. [PMID:1354163]
57. Sokoloff P, Giros B, Martres MP, Andrieux M, Besancon R, Pilon C, Bouthenet ML, Souil E, Schwartz JC. (1992) Localization and function of the D3 dopamine receptor. Arzneimittelforschung, 42 (2A): 224-30. [PMID:1586393]
58. Sokoloff P, Giros B, Martres MP, Bouthenet ML, Schwartz JC. (1990) Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature, 347 (6289): 146-51. [PMID:1975644]
59. Sunahara RK, Guan HC, O'Dowd BF, Seeman P, Laurier LG, Ng G, George SR, Torchia J, Van Tol HH, Niznik HB. (1991) Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. Nature, 350 (6319): 614-9. [PMID:1826762]
60. Tang L, Todd RD, Heller A, O'Malley KL. (1994) Pharmacological and functional characterization of D2, D3 and D4 dopamine receptors in fibroblast and dopaminergic cell lines. J Pharmacol Exp Ther, 268 (1): 495-502. [PMID:8301592]
61. Tiberi M, Caron MG. (1994) High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype. J Biol Chem, 269 (45): 27925-31. [PMID:7525564]
62. Tice MA, Hashemi T, Taylor LA, Duffy RA, McQuade RD. (1994) Characterization of the binding of SCH 39166 to the five cloned dopamine receptor subtypes. Pharmacol Biochem Behav, 49 (3): 567-71. [PMID:7862709]
63. Van Tol HH, Bunzow JR, Guan HC, Sunahara RK, Seeman P, Niznik HB, Civelli O. (1991) Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature, 350 (6319): 610-4. [PMID:1840645]
64. Xi ZX, Gardner EL. (2007) Pharmacological actions of NGB 2904, a selective dopamine D3 receptor antagonist, in animal models of drug addiction. CNS Drug Rev, 13 (2): 240-59. [PMID:17627675]
65. Xiao J, Free RB, Barnaeva E, Conroy J, Doyle T, Bryant-Genevier M, Taylor MK, Southall N, Hu X, Ferrer M et al.. (2010) Discovery, optimization, and characterization of a novel series of dopamine D2 versus D3 receptor selective antagonists. Probe Reports from the NIH Molecular Libraries Program,. [PMID:24260782]
66. Xiao J, Free RB, Barnaeva E, Conroy JL, Doyle T, Miller B, Bryant-Genevier M, Taylor MK, Hu X, Dulcey AE et al.. (2014) Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists. J Med Chem, 57 (8): 3450-63. [PMID:24666157]
67. Zajdel P, Marciniec K, Maślankiewicz A, Grychowska K, Satała G, Duszyńska B, Lenda T, Siwek A, Nowak G, Partyka A et al.. (2013) Antidepressant and antipsychotic activity of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole targeting serotonin 5-HT₁A/5-HT₂A/5-HT₇ and dopamine D₂/D₃ receptors. Eur J Med Chem, 60: 42-50. [PMID:23279866]
68. Zhen J, Antonio T, Dutta AK, Reith ME. (2010) Concentration of receptor and ligand revisited in a modified receptor binding protocol for high-affinity radioligands: [3H]Spiperone binding to D2 and D3 dopamine receptors. J Neurosci Methods, 188 (1): 32-8. [PMID:20122961]
69. Zhou QY, Grandy DK, Thambi L, Kushner JA, Van Tol HH, Cone R, Pribnow D, Salon J, Bunzow JR, Civelli O. (1990) Cloning and expression of human and rat D1 dopamine receptors. Nature, 347 (6288): 76-80. [PMID:2168520]
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 (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License
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.