Target Information

Target General Infomation
Target ID
T46828
Former ID
TTDS00015
Target Name
D(1B) dopamine receptor
Gene Name
DRD5
Synonyms
D(5) dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D1beta dopamine receptor; Dopamine receptor 5; DRD5
Target Type
Successful
Disease Allergy [ICD9: 995.3; ICD10: T78.4]
Schizophrenia [ICD9: 295; ICD10: F20]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
BioChemical Class
GPCR rhodopsin
Target Validation
T46828
UniProt ID
P21918
Sequence
MLPPGSNGTAYPGQFALYQQLAQGNAVGGSAGAPPLGPSQVVTACLLTLLIIWTLLGNVL
VCAAIVRSRHLRANMTNVFIVSLAVSDLFVALLVMPWKAVAEVAGYWPFGAFCDVWVAFD
IMCSTASILNLCVISVDRYWAISRPFRYKRKMTQRMALVMVGLAWTLSILISFIPVQLNW
HRDQAASWGGLDLPNNLANWTPWEEDFWEPDVNAENCDSSLNRTYAISSSLISFYIPVAI
MIVTYTRIYRIAQVQIRRISSLERAAEHAQSCRSSAACAPDTSLRASIKKETKVLKTLSV
IMGVFVCCWLPFFILNCMVPFCSGHPEGPPAGFPCVSETTFDVFVWFGWANSSLNPVIYA
FNADFQKVFAQLLGCSHFCSRTPVETVNISNELISYNQDIVFHKEIAAAYIHMMPNAVTP
GNREVDNDEEEGPFDRMFQIYQTSPDGDPVAESVWELDCEGEISLDKITPFTPNGFH
Drugs and Mode of Action
Drug(s) Phenyltoloxamine Drug Info Approved Allergy [551871]
DS-8273 Drug Info Phase 1 Solid tumours [524661]
LE-300 Drug Info Preclinical Schizophrenia [536463]
GMC-283 Drug Info Terminated Schizophrenia [536463]
ZD-3638 Drug Info Terminated Schizophrenia [536463]
Agonist (+)-ADTN Drug Info [529311]
beta-ergocriptine Drug Info [529311]
N-propylnorapomorphine Drug Info [529311]
Inhibitor (+/-)-nantenine Drug Info [530558]
1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one Drug Info [528904]
1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine Drug Info [533570]
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]
4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine Drug Info [527160]
FLUMEZAPINE Drug Info [533515]
FLUTROLINE Drug Info [533512]
ISOCLOZAPINE Drug Info [533570]
ISOLOXAPINE Drug Info [533577]
Phenyltoloxamine Drug Info [527160]
STEPHOLIDINE Drug Info [530374]
Antagonist GMC-283 Drug Info [536463]
LE-300 Drug Info [536463]
SKF-83556 Drug Info [529311]
[125I]SCH23982 Drug Info [543568]
[3H]SCH-23390 Drug Info [533868]
Binder ZD-3638 Drug Info [536463]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Dopaminergic synapse
PANTHER Pathway Dopamine receptor mediated signaling pathway
Reactome Dopamine receptors
G alpha (s) signalling events
WikiPathways Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 524661ClinicalTrials.gov (NCT02076451) Open-label Study of DS-8273a to Assess Its Safety and Tolerability, and Assess Its Pharmacokinetic and Pharmacodynamic Properties in Subjects With Advanced Solid Tumors or Lymphomas. U.S. National Institutes of Health.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 527160J Med Chem. 2004 Aug 12;47(17):4155-8.Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
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 529311Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. Nature. 1991 Apr 18;350(6319):614-9.
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 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 533512J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines.
Ref 533515J Med Chem. 1982 Oct;25(10):1133-40.Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems.
Ref 533570J Med Chem. 1982 Jul;25(7):855-8.Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain.
Ref 533577J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.
Ref 533868Dopamine D5 receptors in human peripheral blood lymphocytes: a radioligand binding study. J Neuroimmunol. 1994 Aug;53(1):1-7.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 543568(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. (Target id: 218).
Ref 550586Clinical pipeline report, company report or official report of Daiichi Sankyo.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.