Target Information
Target General Infomation | |||||
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Target ID |
T02551
|
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Former ID |
TTDS00013
|
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Target Name |
D(3) dopamine receptor
|
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Gene Name |
DRD3
|
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Synonyms |
Dopamine receptor 3; DRD3
|
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Target Type |
Successful
|
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Disease | Bipolar disorder [ICD9: 296.0, 296.1, 296.4, 296.5, 296.6, 296.7, 296.8, 300; ICD10: F31, F40-F42] | ||||
Cocaine addiction [ICD9: 304.2; ICD10: F14.2] | |||||
Drug abuse [ICD9: 303-304; ICD10: F10-F19] | |||||
Emesis [ICD9: 787; ICD10: R11] | |||||
Emesis; Gastric motility disorder [ICD9: 294.1, 307.23, 314.00, 314.01, 320-322, 323, 331.0, 332, 333.4, 340, 344.1, 344.81, 348.0, 536.8, 787; ICD10: F02.2, F02.3, F90, F95.2, G00-G37, G83.5, G93.0] | |||||
Female sexual dysfunction [ICD9: 302.7; ICD10: F52] | |||||
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | |||||
Male sexual disorders [ICD10: F52] | |||||
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29] | |||||
Parkinson's disease [ICD9: 332; ICD10: G20] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
Substance dependence [ICD10: F10-F19] | |||||
Unspecified [ICD code not available] | |||||
Function |
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
|
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BioChemical Class |
GPCR rhodopsin
|
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Target Validation |
T02551
|
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UniProt ID | |||||
Sequence |
MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC |
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Drugs and Mode of Action | |||||
Drug(s) | Cariprazine | Drug Info | Approved | Bipolar disorder | [1], [2] |
Pramipexole | Drug Info | Approved | Parkinson's disease | [3], [4] | |
Ropinirole | Drug Info | Approved | Parkinson's disease | [5], [6] | |
CM-2395 | Drug Info | Phase 3 | Schizophrenia | [7] | |
P2B-001 | Drug Info | Phase 2/3 | Parkinson's disease | [8] | |
GSK598809 | Drug Info | Phase 2 | Drug abuse | [9] | |
GSK618334 | Drug Info | Phase 1 | Drug abuse | [10] | |
Pfizer 10 | Drug Info | Phase 1 | Female sexual dysfunction | [11] | |
F-15063 | Drug Info | Preclinical | Schizophrenia | [12] | |
PD-157533 | Drug Info | Preclinical | Schizophrenia | [13] | |
PD-157695 | Drug Info | Preclinical | Schizophrenia | [13] | |
PD-158771 | Drug Info | Preclinical | Schizophrenia | [13] | |
S-33084 | Drug Info | Preclinical | Psychotic disorders | [14], [15] | |
S32504 | Drug Info | Preclinical | Parkinson's disease | [16] | |
U-99194A | Drug Info | Preclinical | Schizophrenia | [13] | |
Quinelorane | Drug Info | Discontinued in Phase 3 | Male sexual disorders | [17], [18] | |
A-437203 | Drug Info | Discontinued in Phase 2 | Psychotic disorders | [19] | |
BP-897 | Drug Info | Discontinued in Phase 2 | Cocaine addiction | [20], [21] | |
MAZAPERTINE | Drug Info | Discontinued in Phase 2 | Discovery agent | [22] | |
AVE-5997 | Drug Info | Discontinued in Phase 1 | Psychotic disorders | [23] | |
S-33138 | Drug Info | Discontinued in Phase 1 | Psychotic disorders | [24] | |
AS-8112 | Drug Info | Terminated | Emesis | [25] | |
AVE-5997EF | Drug Info | Terminated | Schizophrenia | [13] | |
BP4.879a | Drug Info | Terminated | Schizophrenia | [13] | |
BTS-79018 | Drug Info | Terminated | Schizophrenia | [13] | |
E-2040 | Drug Info | Terminated | Schizophrenia | [26] | |
GR-218231 | Drug Info | Terminated | Discovery agent | [27], [28] | |
PNU-177864 | Drug Info | Terminated | Schizophrenia | [13] | |
PNU-96391A | Drug Info | Terminated | Substance dependence | [29] | |
RGH-1756 | Drug Info | Terminated | Schizophrenia | [13] | |
S32504 | Drug Info | Terminated | Major depressive disorder | [30] | |
SB-277011 | Drug Info | Terminated | Schizophrenia | [13], [31] | |
YM-43611 | Drug Info | Terminated | Psychotic disorders | [32] | |
Inhibitor | (+)-3-(1-Propyl-piperidin-3-yl)-phenol | Drug Info | [33] | ||
(+)-BUTACLAMOL | Drug Info | [34] | |||
(+/-)-7-hydroxy-2-(N,N-di-n-propylamino)tetralin | Drug Info | [35] | |||
(+/-)-nantenine | Drug Info | [36] | |||
(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile | Drug Info | [33] | |||
(-)-5-hydroxy-2-(dipropylamino)tetralin | Drug Info | [37] | |||
(2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine | Drug Info | [38] | |||
(4-Dipropylamino-cyclohexylidene)-acetonitrile | Drug Info | [39] | |||
(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine | Drug Info | [40] | |||
(4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine | Drug Info | [39] | |||
(R)-(-)-2-Methyl-apomorphine hydrochloride | Drug Info | [41] | |||
(R)-(-)-2-Phenyl-apomorphine hydrochloride | Drug Info | [41] | |||
(R)-2-(Benzylamino-methyl)-chroman-7-ol | Drug Info | [42] | |||
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine | Drug Info | [43] | |||
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one | Drug Info | [44] | |||
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine | Drug Info | [45] | |||
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine | Drug Info | [45] | |||
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine | Drug Info | [45] | |||
1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine | Drug Info | [45] | |||
1-Benzyl-4-pyrrol-1-yl-piperidine | Drug Info | [45] | |||
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine | Drug Info | [46] | |||
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine | Drug Info | [47] | |||
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine | Drug Info | [38] | |||
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine | Drug Info | [38] | |||
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine | Drug Info | [38] | |||
2-(4-Dipropylamino-cyclohexylidene)-malononitrile | Drug Info | [39] | |||
3-(1-Propyl-pyrrolidin-3-yl)-phenol | Drug Info | [47] | |||
3-(2-Benzylamino-ethoxy)-phenol | Drug Info | [48] | |||
3-(4-Benzyl-piperazin-1-yl)-phenol | Drug Info | [49] | |||
3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole | Drug Info | [50] | |||
3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole | Drug Info | [50] | |||
3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole | Drug Info | [50] | |||
4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one | Drug Info | [48] | |||
4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole | Drug Info | [49] | |||
4-(4-Benzyl-piperazin-1-yl)-1H-indole | Drug Info | [49] | |||
4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole | Drug Info | [49] | |||
4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole | Drug Info | [49] | |||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [51] | |||
4-Dipropylamino-cyclohex-1-enecarbonitrile | Drug Info | [39] | |||
A-690344 | Drug Info | [52] | |||
A-706149 | Drug Info | [53] | |||
A-987306 | Drug Info | [34] | |||
Azaperone | Drug Info | [54] | |||
Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine | Drug Info | [48] | |||
Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine | Drug Info | [48] | |||
D-189 | Drug Info | [55] | |||
D-190 | Drug Info | [55] | |||
D-192 | Drug Info | [55] | |||
D-193 | Drug Info | [55] | |||
D-203 | Drug Info | [55] | |||
D-210 | Drug Info | [55] | |||
D-218 | Drug Info | [55] | |||
D-219 | Drug Info | [55] | |||
D-220 | Drug Info | [55] | |||
D-237 | Drug Info | [35] | |||
D-264 | Drug Info | [56] | |||
D-315 | Drug Info | [57] | |||
D-366 | Drug Info | [37] | |||
Etoloxamine | Drug Info | [38] | |||
FLUMEZAPINE | Drug Info | [58] | |||
FLUTROLINE | Drug Info | [59] | |||
GR-218231 | Drug Info | [60] | |||
ISOCLOZAPINE | Drug Info | [46] | |||
ISOLOXAPINE | Drug Info | [61] | |||
L-741626 | Drug Info | [62] | |||
L-741742 | Drug Info | [63] | |||
MAZAPERTINE | Drug Info | [64] | |||
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide | Drug Info | [40] | |||
N-(4-Propylaminobutyl)-4-biphenylcarboxamide | Drug Info | [40] | |||
P2B-001 | Drug Info | [65] | |||
PG-01037 | Drug Info | [66] | |||
QUINPIROLE | Drug Info | [67] | |||
R-226161 | Drug Info | [68] | |||
SB-271046 | Drug Info | [69] | |||
SPIPERONE | Drug Info | [70] | |||
STEPHOLIDINE | Drug Info | [71] | |||
UH-232 | Drug Info | [72] | |||
[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine | Drug Info | [48] | |||
Antagonist | (+)-AJ76 | Drug Info | [73] | ||
(+)-S-14297 | Drug Info | [74] | |||
AS-8112 | Drug Info | [75] | |||
AS-9705 | Drug Info | [75] | |||
AVE-5997 | Drug Info | [76] | |||
AVE-5997EF | Drug Info | [13] | |||
BP4.879a | Drug Info | [13] | |||
GSK598809 | Drug Info | [77] | |||
GSK618334 | Drug Info | [77] | |||
nafadotride | Drug Info | [78] | |||
NGB 2904 | Drug Info | [79] | |||
PD-157533 | Drug Info | [13] | |||
PD-157695 | Drug Info | [13] | |||
PD-158771 | Drug Info | [13] | |||
PNU-177864 | Drug Info | [13] | |||
RGH-1756 | Drug Info | [13] | |||
S-33138 | Drug Info | [80], [81] | |||
SB-277011 | Drug Info | [13] | |||
[3H]nemonapride | Drug Info | [82] | |||
[3H]spiperone | Drug Info | [83] | |||
Agonist | (-)-N-porphynorapomorphine | Drug Info | [84] | ||
7-trans-OH-PIPAT | Drug Info | [85] | |||
CM-2395 | Drug Info | [86] | |||
PD 128907 | Drug Info | [87] | |||
PF-592379 | Drug Info | [88] | |||
Pfizer 10 | Drug Info | [11] | |||
piribedil | Drug Info | [89] | |||
[3H]7-OH-DPAT | Drug Info | [90] | |||
[3H]PD128907 | Drug Info | [91] | |||
Modulator | 7-OH-DPAT | Drug Info | |||
A-437203 | Drug Info | ||||
BP-897 | Drug Info | ||||
Cariprazine | Drug Info | [1] | |||
E-2040 | Drug Info | [92] | |||
F-15063 | Drug Info | ||||
PD-152255 | Drug Info | ||||
PNU-96391A | Drug Info | [29] | |||
Pramipexole | Drug Info | [93] | |||
Quinelorane | Drug Info | ||||
Ropinirole | Drug Info | [93] | |||
S-33084 | Drug Info | [94] | |||
S32504 | Drug Info | [16] | |||
YM-43611 | Drug Info | ||||
Binder | BTS-79018 | Drug Info | [13] | ||
U-99194A | Drug Info | [13] | |||
Modulator (allosteric modulator) | SB269652 | Drug Info | [95] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Dopaminergic synapse | |||||
Reactome | Dopamine receptors | ||||
G alpha (i) signalling events | |||||
WikiPathways | Monoamine GPCRs | ||||
GPCRs, Class A Rhodopsin-like | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
Nicotine Activity on Dopaminergic Neurons | |||||
GPCRs, Other | |||||
References | |||||
REF 1 | 2013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9. | ||||
REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7671). | ||||
REF 3 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
REF 4 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 953). | ||||
REF 5 | Update on ropinirole in the treatment of Parkinson's disease. Neuropsychiatr Dis Treat. 2009;5:33-6. Epub 2009 Apr 8. | ||||
REF 6 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7295). | ||||
REF 7 | Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010. | ||||
REF 8 | ClinicalTrials.gov (NCT01968460) Safety, Tolerability and Efficacy of Two Doses of Once Daily P2B001 in Subjects With Early Parkinson's Disease. U.S. National Institutes of Health. | ||||
REF 9 | ClinicalTrials.gov (NCT01188967) Effectiveness of GSK598809, a Selective D3 Antagonist, Added to Cognitive Behavioral Therapy and Nicotine Replacement Therapy for Smoking Cessation and Prevention of Very Early Relapse to Smoking. U.S. National Institutes of Health. | ||||
REF 10 | ClinicalTrials.gov (NCT00513279) To Investigate If Single Doses Of GSK618334 Are Safe And To Investigate Blood Levels Of GSK618334. U.S. National Institutes of Health. | ||||
REF 11 | Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27. | ||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026348) | ||||
REF 13 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
REF 14 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 129). | ||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013394) | ||||
REF 16 | S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: II. Actions in rodent, primate, and cellular models of antiparkinsonian activity in comparison to ropinirole. J Pharmacol Exp Ther. 2004 Jun;309(3):921-35. Epub 2004 Feb 20. | ||||
REF 17 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 954). | ||||
REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001472) | ||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012940) | ||||
REF 20 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7625). | ||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012397) | ||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662) | ||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018413) | ||||
REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014544) | ||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009088) | ||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126) | ||||
REF 27 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 70). | ||||
REF 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008161) | ||||
REF 29 | The dopamine stabilizer (-)-OSU6162 occupies a subpopulation of striatal dopamine D2/D3 receptors: an [(11)C]raclopride PET study in healthy human subjects. Neuropsychopharmacology. 2015 Jan;40(2):472-9. | ||||
REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012906) | ||||
REF 31 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 143). | ||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005975) | ||||
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REF 53 | Bioorg Med Chem Lett. 2006 Feb;16(3):658-62. Epub 2005 Nov 2.Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com. | ||||
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