Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T46828
|
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| Former ID |
TTDS00015
|
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| Target Name |
D(1B) dopamine receptor
|
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| Gene Name |
DRD5
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| Synonyms |
D(5) dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D1beta dopamine receptor; Dopamine receptor 5; DRD5
|
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| Target Type |
Successful
|
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| 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.
|
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| BioChemical Class |
GPCR rhodopsin
|
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| Target Validation |
T46828
|
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| UniProt ID | |||||
| Sequence |
MLPPGSNGTAYPGQFALYQQLAQGNAVGGSAGAPPLGPSQVVTACLLTLLIIWTLLGNVL
VCAAIVRSRHLRANMTNVFIVSLAVSDLFVALLVMPWKAVAEVAGYWPFGAFCDVWVAFD IMCSTASILNLCVISVDRYWAISRPFRYKRKMTQRMALVMVGLAWTLSILISFIPVQLNW HRDQAASWGGLDLPNNLANWTPWEEDFWEPDVNAENCDSSLNRTYAISSSLISFYIPVAI MIVTYTRIYRIAQVQIRRISSLERAAEHAQSCRSSAACAPDTSLRASIKKETKVLKTLSV IMGVFVCCWLPFFILNCMVPFCSGHPEGPPAGFPCVSETTFDVFVWFGWANSSLNPVIYA FNADFQKVFAQLLGCSHFCSRTPVETVNISNELISYNQDIVFHKEIAAAYIHMMPNAVTP GNREVDNDEEEGPFDRMFQIYQTSPDGDPVAESVWELDCEGEISLDKITPFTPNGFH |
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| Drugs and Mode of Action | |||||
| Drug(s) | Phenyltoloxamine | Drug Info | Approved | Allergy | [1] |
| DS-8273 | Drug Info | Phase 1 | Solid tumours | [2] | |
| LE-300 | Drug Info | Preclinical | Schizophrenia | [3] | |
| GMC-283 | Drug Info | Terminated | Schizophrenia | [3] | |
| ZD-3638 | Drug Info | Terminated | Schizophrenia | [3] | |
| Agonist | (+)-ADTN | Drug Info | [4] | ||
| beta-ergocriptine | Drug Info | [4] | |||
| N-propylnorapomorphine | Drug Info | [4] | |||
| Inhibitor | (+/-)-nantenine | Drug Info | [5] | ||
| 1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one | Drug Info | [6] | |||
| 1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine | Drug Info | [7] | |||
| 1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine | Drug Info | [8] | |||
| 1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine | Drug Info | [8] | |||
| 1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine | Drug Info | [8] | |||
| 4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine | Drug Info | [8] | |||
| FLUMEZAPINE | Drug Info | [9] | |||
| FLUTROLINE | Drug Info | [10] | |||
| ISOCLOZAPINE | Drug Info | [7] | |||
| ISOLOXAPINE | Drug Info | [11] | |||
| Phenyltoloxamine | Drug Info | [8] | |||
| STEPHOLIDINE | Drug Info | [12] | |||
| Antagonist | GMC-283 | Drug Info | [3] | ||
| LE-300 | Drug Info | [3] | |||
| SKF-83556 | Drug Info | [4] | |||
| [125I]SCH23982 | Drug Info | [13] | |||
| [3H]SCH-23390 | Drug Info | [14] | |||
| Binder | ZD-3638 | Drug Info | [3] | ||
| 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 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 2 | ClinicalTrials.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 3 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
| REF 4 | Cloning 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 5 | Bioorg 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 6 | Bioorg 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 7 | J 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 8 | J 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 9 | J Med Chem. 1982 Oct;25(10):1133-40.Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. | ||||
| REF 10 | J Med Chem. 1980 Jun;23(6):635-43.Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. | ||||
| REF 11 | J 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 12 | Bioorg 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 13 | (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 14 | Dopamine D5 receptors in human peripheral blood lymphocytes: a radioligand binding study. J Neuroimmunol. 1994 Aug;53(1):1-7. | ||||
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