Target Information

Target General Infomation
Target ID
T02551
Former ID
TTDS00013
Target Name
D(3) dopamine receptor
Gene Name
DRD3
Synonyms
Dopamine receptor 3; DRD3
Target Type
Successful
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]
Parkinson's disease [ICD9: 332; ICD10: G20]
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29]
Substance dependence [ICD10: F10-F19]
Schizophrenia [ICD9: 295; ICD10: F20]
Unspecified [ICD code not available]
Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
BioChemical Class
GPCR rhodopsin
Target Validation
T02551
UniProt ID
P35462
Sequence
MASLSQLSSHLNYTCGAENSTGASQARPHAYYALSYCALILAIVFGNGLVCMAVLKERAL
QTTTNYLVVSLAVADLLVATLVMPWVVYLEVTGGVWNFSRICCDVFVTLDVMMCTASILN
LCAISIDRYTAVVMPVHYQHGTGQSSCRRVALMITAVWVLAFAVSCPLLFGFNTTGDPTV
CSISNPDFVIYSSVVSFYLPFGVTVLVYARIYVVLKQRRRKRILTRQNSQCNSVRPGFPQ
QTLSPDPAHLELKRYYSICQDTALGGPGFQERGGELKREEKTRNSLSPTIAPKLSLEVRK
LSNGRLSTSLKLGPLQPRGVPLREKKATQMVAIVLGAFIVCWLPFFLTHVLNTHCQTCHV
SPELYSATTWLGYVNSALNPVIYTTFNIEFRKAFLKILSC
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
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REF 3Novel 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 5Update 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 7Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010.
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REF 9ClinicalTrials.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 10ClinicalTrials.gov (NCT00513279) To Investigate If Single Doses Of GSK618334 Are Safe And To Investigate Blood Levels Of GSK618334. U.S. National Institutes of Health.
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REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013394)
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REF 18Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001472)
REF 19Trusted, 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 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012397)
REF 22Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662)
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018413)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014544)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009088)
REF 26Trusted, 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 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008161)
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REF 32Trusted, 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 77Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
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