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]
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.
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 [532651], [542650]
Pramipexole Drug Info Approved Parkinson's disease [536580], [543322]
Ropinirole Drug Info Approved Parkinson's disease [537532], [542315]
CM-2395 Drug Info Phase 3 Schizophrenia [551513]
P2B-001 Drug Info Phase 2/3 Parkinson's disease [524487]
GSK598809 Drug Info Phase 2 Drug abuse [523147]
GSK618334 Drug Info Phase 1 Drug abuse [522083]
Pfizer 10 Drug Info Phase 1 Female sexual dysfunction [536493]
F-15063 Drug Info Preclinical Schizophrenia [548528]
PD-157533 Drug Info Preclinical Schizophrenia [536463]
PD-157695 Drug Info Preclinical Schizophrenia [536463]
PD-158771 Drug Info Preclinical Schizophrenia [536463]
S-33084 Drug Info Preclinical Psychotic disorders [538794], [547145]
S32504 Drug Info Preclinical Parkinson's disease [526972]
U-99194A Drug Info Preclinical Schizophrenia [536463]
Quinelorane Drug Info Discontinued in Phase 3 Male sexual disorders [543323], [544908]
A-437203 Drug Info Discontinued in Phase 2 Psychotic disorders [547085]
BP-897 Drug Info Discontinued in Phase 2 Cocaine addiction [542612], [547037]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [545274]
AVE-5997 Drug Info Discontinued in Phase 1 Psychotic disorders [547685]
S-33138 Drug Info Discontinued in Phase 1 Psychotic disorders [547260]
AS-8112 Drug Info Terminated Emesis [546591]
AVE-5997EF Drug Info Terminated Schizophrenia [536463]
BP4.879a Drug Info Terminated Schizophrenia [536463]
BTS-79018 Drug Info Terminated Schizophrenia [536463]
E-2040 Drug Info Terminated Schizophrenia [546598]
GR-218231 Drug Info Terminated Discovery agent [542030], [546446]
PNU-177864 Drug Info Terminated Schizophrenia [536463]
PNU-96391A Drug Info Terminated Substance dependence [532971]
RGH-1756 Drug Info Terminated Schizophrenia [536463]
S32504 Drug Info Terminated Major depressive disorder [547082]
SB-277011 Drug Info Terminated Schizophrenia [536463], [538907]
YM-43611 Drug Info Terminated Psychotic disorders [546030]
Inhibitor (+)-3-(1-Propyl-piperidin-3-yl)-phenol Drug Info [533938]
(+)-BUTACLAMOL Drug Info [529789]
(+/-)-7-hydroxy-2-(N,N-di-n-propylamino)tetralin Drug Info [529836]
(+/-)-nantenine Drug Info [530558]
(-)-3-(1-Propyl-piperidin-3-yl)-benzonitrile Drug Info [533938]
(-)-5-hydroxy-2-(dipropylamino)tetralin Drug Info [530606]
(2-Benzyl-phenyl)-(2-pyrrolidin-1-yl-ethyl)-amine Drug Info [527160]
(4-Dipropylamino-cyclohexylidene)-acetonitrile Drug Info [525701]
(4-Ethynyl-cyclohex-3-enyl)-dipropyl-amine Drug Info [529734]
(4-Phenylethynyl-cyclohex-3-enyl)-dipropyl-amine Drug Info [525701]
(R)-(-)-2-Methyl-apomorphine hydrochloride Drug Info [529328]
(R)-(-)-2-Phenyl-apomorphine hydrochloride Drug Info [529328]
(R)-2-(Benzylamino-methyl)-chroman-7-ol Drug Info [526840]
1-(4-(1H-pyrazol-1-yl)benzyl)-4-phenylpiperazine Drug Info [528099]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one Drug Info [528904]
1-Benzyl-4-(2-ethynyl-pyrrol-1-yl)-piperidine Drug Info [525629]
1-Benzyl-4-(2-iodo-pyrrol-1-yl)-piperidine Drug Info [525629]
1-Benzyl-4-(2-oxazol-5-yl-pyrrol-1-yl)-piperidine Drug Info [525629]
1-Benzyl-4-(3-oxazol-5-yl-pyrrol-1-yl)-piperidine Drug Info [525629]
1-Benzyl-4-pyrrol-1-yl-piperidine Drug Info [525629]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine Drug Info [533570]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info [551334]
1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine Drug Info [527160]
1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine Drug Info [527160]
1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine Drug Info [527160]
2-(4-Dipropylamino-cyclohexylidene)-malononitrile Drug Info [525701]
3-(1-Propyl-pyrrolidin-3-yl)-phenol Drug Info [551334]
3-(2-Benzylamino-ethoxy)-phenol Drug Info [525599]
3-(4-Benzyl-piperazin-1-yl)-phenol Drug Info [534802]
3-(4-Methyl-piperidin-1-ylmethyl)-1H-indole Drug Info [534131]
3-(4-Phenyl-piperazin-1-ylmethyl)-1H-indole Drug Info [534131]
3-(4-Phenyl-piperidin-1-ylmethyl)-1H-indole Drug Info [534131]
4-(2-Benzylamino-ethoxy)-1,3-dihydro-indol-2-one Drug Info [525599]
4-(4-Benzyl-piperazin-1-yl)-1H-benzoimidazole Drug Info [534802]
4-(4-Benzyl-piperazin-1-yl)-1H-indole Drug Info [534802]
4-(4-Benzyl-piperazin-1-yl)-5-chloro-1H-indole Drug Info [534802]
4-(4-Benzyl-piperazin-1-yl)-7-bromo-1H-indole Drug Info [534802]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-Dipropylamino-cyclohex-1-enecarbonitrile Drug Info [525701]
A-690344 Drug Info [527867]
A-706149 Drug Info [527843]
A-987306 Drug Info [529789]
Azaperone Drug Info [533796]
Benzyl-[2-(1H-indazol-4-yloxy)-ethyl]-amine Drug Info [525599]
Benzyl-[2-(1H-indol-4-yloxy)-ethyl]-amine Drug Info [525599]
D-189 Drug Info [529420]
D-190 Drug Info [529420]
D-192 Drug Info [529420]
D-193 Drug Info [529420]
D-203 Drug Info [529420]
D-210 Drug Info [529420]
D-218 Drug Info [529420]
D-219 Drug Info [529420]
D-220 Drug Info [529420]
D-237 Drug Info [529836]
D-264 Drug Info [530117]
D-315 Drug Info [531014]
D-366 Drug Info [530606]
Etoloxamine Drug Info [527160]
FLUMEZAPINE Drug Info [533515]
FLUTROLINE Drug Info [533512]
GR-218231 Drug Info [529862]
ISOCLOZAPINE Drug Info [533570]
ISOLOXAPINE Drug Info [533577]
L-741626 Drug Info [551224]
L-741742 Drug Info [534132]
MAZAPERTINE Drug Info [533800]
N-(4-Dipropylaminobutyl)-4-biphenylcarboxamide Drug Info [529734]
N-(4-Propylaminobutyl)-4-biphenylcarboxamide Drug Info [529734]
P2B-001 Drug Info [534641]
PG-01037 Drug Info [528974]
QUINPIROLE Drug Info [530429]
R-226161 Drug Info [528772]
SB-271046 Drug Info [529191]
SPIPERONE Drug Info [527420]
STEPHOLIDINE Drug Info [530374]
UH-232 Drug Info [551330]
[2-(1H-Benzoimidazol-4-yloxy)-ethyl]-benzyl-amine Drug Info [525599]
Antagonist (+)-AJ76 Drug Info [530381]
(+)-S-14297 Drug Info [533834]
AS-8112 Drug Info [536188]
AS-9705 Drug Info [536188]
AVE-5997 Drug Info [527957]
AVE-5997EF Drug Info [536463]
BP4.879a Drug Info [536463]
GSK598809 Drug Info [550963]
GSK618334 Drug Info [550963]
nafadotride Drug Info [534073]
NGB 2904 Drug Info [528948]
PD-157533 Drug Info [536463]
PD-157695 Drug Info [536463]
PD-158771 Drug Info [536463]
PNU-177864 Drug Info [536463]
RGH-1756 Drug Info [536463]
S-33138 Drug Info [531061], [551871]
SB-277011 Drug Info [536463]
[3H]nemonapride Drug Info [526842]
[3H]spiperone Drug Info [525818]
Agonist (-)-N-porphynorapomorphine Drug Info [533725]
7-trans-OH-PIPAT Drug Info [533838]
CM-2395 Drug Info [548980]
PD 128907 Drug Info [534074]
PF-592379 Drug Info [531866]
Pfizer 10 Drug Info [536493]
piribedil Drug Info [526443]
[3H]7-OH-DPAT Drug Info [533726]
[3H]PD128907 Drug Info [533687]
Modulator 7-OH-DPAT Drug Info
A-437203 Drug Info
BP-897 Drug Info
Cariprazine Drug Info [532651]
E-2040 Drug Info [546599]
F-15063 Drug Info
PD-152255 Drug Info
PNU-96391A Drug Info [532971]
Pramipexole Drug Info [556264]
Quinelorane Drug Info
Ropinirole Drug Info [556264]
S-33084 Drug Info [525807]
S32504 Drug Info [526972]
YM-43611 Drug Info
Binder BTS-79018 Drug Info [536463]
U-99194A Drug Info [536463]
Modulator (allosteric modulator) SB269652 Drug Info [533107]
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 522083ClinicalTrials.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 523147ClinicalTrials.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 524487ClinicalTrials.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 526972S32504, 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 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 532971The 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 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536493Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 537532Update on ropinirole in the treatment of Parkinson's disease. Neuropsychiatr Dis Treat. 2009;5:33-6. Epub 2009 Apr 8.
Ref 538794(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 538907(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 542030(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 542315(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 542612(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 542650(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 543322(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 543323(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).
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Ref 546446Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008161)
Ref 546591Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009088)
Ref 546598Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009126)
Ref 547037Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012397)
Ref 547082Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012906)
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Ref 547145Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013394)
Ref 547260Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014544)
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Ref 525701J Med Chem. 2000 Feb 24;43(4):756-62.Conjugated enynes as nonaromatic catechol bioisosteres: synthesis, binding experiments, and computational studies of novel dopamine receptor agonists recognizing preferentially the D(3) subtype.
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Ref 525818Regulation 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. 2000 Jul;130(5):1045-59.
Ref 526443Differential 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. 2002 Nov;303(2):791-804.
Ref 526840J Med Chem. 2003 Oct 9;46(21):4377-92.Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybrid pharmacophore- and structure-based database searching approach.
Ref 526842Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole. J Neurochem. 2003 Nov;87(3):631-41.
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Ref 527843Bioorg 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.
Ref 527867Bioorg Med Chem Lett. 2006 Feb;16(3):490-4. Epub 2005 Nov 11.Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: 1H-pyrimidin-2-one derivatives.
Ref 527957Effect of dopamine D3 antagonists on PPI in DBA/2J mice or PPI deficit induced by neonatal ventral hippocampal lesions in rats. Neuropsychopharmacology. 2006 Jul;31(7):1382-92. Epub 2005 Dec 14.
Ref 528099Bioorg Med Chem Lett. 2006 Jun 1;16(11):2955-9. Epub 2006 Mar 24.Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.
Ref 528772Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Ref 528904Bioorg Med Chem. 2007 Sep 1;15(17):5811-8. Epub 2007 Jun 7.Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand.
Ref 528948Pharmacological actions of NGB 2904, a selective dopamine D3 receptor antagonist, in animal models of drug addiction. CNS Drug Rev. 2007 Summer;13(2):240-59.
Ref 528974J Med Chem. 2007 Aug 23;50(17):4135-46. Epub 2007 Aug 2.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.
Ref 529191Bioorg Med Chem Lett. 2008 Jan 15;18(2):738-43. Epub 2007 Nov 17.Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
Ref 529328Bioorg Med Chem. 2008 Apr 1;16(7):3773-9. Epub 2008 Feb 5.Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines.
Ref 529420J Med Chem. 2008 May 22;51(10):3005-19. Epub 2008 Apr 12.Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Ref 529734J Med Chem. 2008 Nov 13;51(21):6829-38. Epub 2008 Oct 4.Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Ref 529836J Med Chem. 2008 Dec 25;51(24):7806-19.Structurally constrained hybrid derivatives containing octahydrobenzo[g or f]quinoline moieties for dopamine D2 and D3 receptors: binding characterization at D2/D3 receptors and elucidation of a pharmacophore model.
Ref 529862Bioorg Med Chem. 2009 Jan 15;17(2):758-66. Epub 2008 Nov 24.Design, synthesis, and binding affinities of potential positron emission tomography (PET) ligands with optimal lipophilicity for brain imaging of the dopamine D3 receptor. Part II.
Ref 530117Bioorg Med Chem. 2009 Jun 1;17(11):3923-33. Epub 2009 Apr 19.Investigation of various N-heterocyclic substituted piperazine versions of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol: effect on affinity and selectivity for dopamine D3 receptor.
Ref 530374Bioorg Med Chem. 2009 Oct 1;17(19):6898-907. Epub 2009 Aug 20.Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?.
Ref 530381Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. 1990 Sep 13;347(6289):146-51.
Ref 530429J Med Chem. 2009 Nov 12;52(21):6860-70.1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 530606J Med Chem. 2010 Feb 11;53(3):1023-37.Development of (S)-N6-(2-(4-(isoquinolin-1-yl)piperazin-1-yl)ethyl)-N6-propyl-4,5,6,7-tetrahydrobenzo[d]-thiazole-2,6-diamine and its analogue as a D3 receptor preferring agonist: potent in vivo activity in Parkinson's disease animal models.
Ref 531014Bioorg Med Chem. 2010 Aug 1;18(15):5661-74. Epub 2010 Jun 12.Further delineation of hydrophobic binding sites in dopamine D(2)/D(3) receptors for N-4 substituents on the piperazine ring of the hybrid template 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro-naphthalen-2-ol.
Ref 531061The dopamine D3 receptor antagonist, S33138, counters cognitive impairment in a range of rodent and primate procedures. Int J Neuropsychopharmacol. 2010 Sep;13(8):1035-51.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531866Lack of abuse potential in a highly selective dopamine D3 agonist, PF-592,379, in drug self-administration and drug discrimination in rats. Behav Pharmacol. 2012 Jun;23(3):280-91.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 532971The 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 533107Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists. Eur Neuropsychopharmacol. 2015 Sep;25(9):1448-61.
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