Target Information
Target General Infomation | |||||
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Target ID |
T29683
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Former ID |
TTDC00117
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Target Name |
Nigral tachykinin NK(3) receptor
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Gene Name |
TACR3
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Synonyms |
NK-3 receptor; NK-3R; NKR; Neurokinin B receptor; Neurokinin-3 receptor; Neuromedin K receptor; Tachykinin receptor 3; TACR3
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Target Type |
Clinical Trial
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Disease | Asthma [ICD10: J45] | ||||
Central nervous system disease [ICD10: G00-G99] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Depression [ICD9: 311; ICD10: F30-F39] | |||||
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1] | |||||
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29] | |||||
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99] | |||||
Schizophrenia; Schizoaffective disorders [ICD9: 295, 295.70; ICD10: F20, F25] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
Function |
This is a receptor for the tachykinin neuropeptide neuromedin-K (neurokinin B). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: neuromedin-K > substance K > substance P.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T29683
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UniProt ID | |||||
Sequence |
MATLPAAETWIDGGGGVGADAVNLTASLAAGAATGAVETGWLQLLDQAGNLSSSPSALGL
PVASPAPSQPWANLTNQFVQPSWRIALWSLAYGVVVAVAVLGNLIVIWIILAHKRMRTVT NYFLVNLAFSDASMAAFNTLVNFIYALHSEWYFGANYCRFQNFFPITAVFASIYSMTAIA VDRYMAIIDPLKPRLSATATKIVIGSIWILAFLLAFPQCLYSKTKVMPGRTLCFVQWPEG PKQHFTYHIIVIILVYCFPLLIMGITYTIVGITLWGGEIPGDTCDKYHEQLKAKRKVVKM MIIVVMTFAICWLPYHIYFILTAIYQQLNRWKYIQQVYLASFWLAMSSTMYNPIIYCCLN KRFRAGFKRAFRWCPFIKVSSYDELELKTTRFHPNRQSSMYTVTRMESMTVVFDPNDADT TRSSRKKRATPRDPSFNGCSRRNSKSASATSSFISSPYTSVDEYS |
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Drugs and Mode of Action | |||||
Drug(s) | SB222200 | Drug Info | Preclinical | Schizophrenia; Schizoaffective disorders | [525871], [539352] |
Osanetant | Drug Info | Discontinued in Phase 2b | Schizophrenia; Schizoaffective disorders | [536463], [539337] | |
AZD2624 | Drug Info | Discontinued in Phase 2 | Schizophrenia | [522334], [541098] | |
CS-003 | Drug Info | Discontinued in Phase 2 | Chronic obstructive pulmonary disease | [536223] | |
Talnetant | Drug Info | Discontinued in Phase 2 | Schizophrenia; Schizoaffective disorders | [536224], [539353] | |
Talnetant | Drug Info | Discontinued in Phase 2 | Irritable bowel syndrome | [536224], [539353] | |
GSK1144814 | Drug Info | Discontinued in Phase 1 | Schizophrenia | [522978] | |
SSR-146977 | Drug Info | Discontinued in Phase 1 | Psychotic disorders | [539354], [547239] | |
Osanetant | Drug Info | Terminated | Depression | [536463], [539337] | |
Inhibitor | 2-phenyl-N-(1-phenylethyl)quinoline-4-carboxamide | Drug Info | [531249] | ||
3-methoxy-N',2-diphenylquinoline-4-carbohydrazide | Drug Info | [528420] | |||
N-phenethyl-2-phenylquinoline-4-carboxamide | Drug Info | [531249] | |||
NEUROKININ B | Drug Info | [551267] | |||
PD-157672 | Drug Info | [551267] | |||
PD-160946 | Drug Info | [551281] | |||
PD-161182 | Drug Info | [551281] | |||
Modulator | AZD2624 | Drug Info | |||
GSK1144814 | Drug Info | ||||
Antagonist | CS-003 | Drug Info | [536223] | ||
GR138676 | Drug Info | [533624] | |||
GSK-172981 | Drug Info | [543793] | |||
N',2-diphenylquinoline-4-carbohydrazide | Drug Info | [528420] | |||
N',2-diphenylquinoline-4-carbohydrazide 8m | Drug Info | [528419] | |||
NK-3 antagonists | Drug Info | [543793] | |||
NK3 antagonist PET ligand | Drug Info | [543793] | |||
Osanetant | Drug Info | [536865], [536894], [537495] | |||
PD 154740 | Drug Info | [533591] | |||
R-820 | Drug Info | [535700] | |||
SB222200 | Drug Info | [536641], [536693], [536987] | |||
SCH 206272 | Drug Info | [526412] | |||
SSR-146977 | Drug Info | [526353] | |||
Talnetant | Drug Info | [536865], [536894], [537495] | |||
[3H]osanetant | Drug Info | [543793] | |||
Agonist | eledoisin | Drug Info | [526727] | ||
kassinin | Drug Info | [534153] | |||
neurokinin A | Drug Info | [525988] | |||
Senktide | Drug Info | [535700], [537952] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 522334 | ClinicalTrials.gov (NCT00686998) Phase IIA Study in Patients With Schizophrenia. U.S. National Institutes of Health. | ||||
Ref 522978 | ClinicalTrials.gov (NCT01090440) Pharmacokinetics, Effect of Food, Safety and Tolerability of a New Tablet Formulation of GSK1144814 in Healthy Subjects. U.S. National Institutes of Health. | ||||
Ref 525871 | Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):373-81. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536224 | Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. | ||||
Ref 536463 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
Ref 539337 | (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: 2110). | ||||
Ref 539352 | (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: 2131). | ||||
Ref 539353 | (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: 2132). | ||||
Ref 539354 | (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: 2133). | ||||
Ref 525988 | Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor. Eur J Pharmacol. 2001 Feb 16;413(2-3):143-50. | ||||
Ref 526353 | Biochemical and pharmacological activities of SSR 146977, a new potent nonpeptide tachykinin NK3 receptor antagonist. Can J Physiol Pharmacol. 2002 May;80(5):482-8. | ||||
Ref 526412 | SCH 206272: a potent, orally active tachykinin NK(1), NK(2), and NK(3) receptor antagonist. Eur J Pharmacol. 2002 Aug 23;450(2):191-202. | ||||
Ref 526727 | Molecular characterisation, expression and localisation of human neurokinin-3 receptor. FEBS Lett. 1992 Mar 24;299(1):90-5. | ||||
Ref 528419 | N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5752-6. Epub 2006 Sep 6. | ||||
Ref 528420 | Bioorg Med Chem Lett. 2006 Nov 15;16(22):5748-51. Epub 2006 Sep 6.N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists. | ||||
Ref 531249 | J Med Chem. 2010 Nov 25;53(22):8080-8. Epub 2010 Nov 3.Virtual screening to identify novel antagonists for the G protein-coupled NK3 receptor. | ||||
Ref 533591 | Two classes of structurally different antagonists display similar species preference for the human tachykinin neurokinin3 receptor. Mol Pharmacol. 1995 Oct;48(4):711-6. | ||||
Ref 533624 | GR138676, a novel peptidic tachykinin antagonist which is potent at NK3 receptors. Neuropeptides. 1994 Dec;27(6):333-41. | ||||
Ref 534153 | The unpredicted high affinities of a large number of naturally occurring tachykinins for chimeric NK1/NK3 receptors suggest a role for an inhibitory domain in determining receptor specificity. J BiolChem. 1996 Aug 23;271(34):20250-7. | ||||
Ref 535700 | Implication of nigral tachykinin NK3 receptors in the maintenance of hypertension in spontaneously hypertensive rats: a pharmacologic and autoradiographic study. Br J Pharmacol. 2003 Feb;138(4):554-63. | ||||
Ref 536223 | Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91. | ||||
Ref 536641 | Substance P depolarizes striatal projection neurons and facilitates their glutamatergic inputs. J Physiol. 2008 Apr 15;586(8):2143-55. Epub 2008 Feb 28. | ||||
Ref 536693 | Neurokinin B/NK3 receptors exert feedback inhibition on L-DOPA actions in the 6-OHDA lesion rat model of Parkinson's disease. Neuropharmacology. 2008 Jun;54(7):1143-52. Epub 2008 Mar 18. | ||||
Ref 536865 | Augmentation of antipsychotic-induced neurochemical changes by the NK3 receptor antagonist talnetant (SB-223412). Neuropharmacology. 2009 Feb;56(2):342-9. Epub 2008 Sep 18. | ||||
Ref 536894 | The tachykinin NK3 receptor agonist senktide induces locomotor activity in male Mongolian gerbils. Eur J Pharmacol. 2008 Dec 14;600(1-3):87-92. Epub 2008 Oct 10. | ||||
Ref 536987 | Evidence for mediation of nociception by injection of the NK-3 receptor agonist, senktide, into the dorsal periaqueductal gray of rats. Psychopharmacology (Berl). 2009 May;204(1):13-24. Epub 2008 Dec 18. | ||||
Ref 537495 | Pharmacological characterization of senktide-induced tail whips. Neuropharmacology. 2009 Jun 21. | ||||
Ref 537952 | Neurokinin-3 receptors modulate dopamine cell function and alter the effects of 6-hydroxydopamine. Brain Res. 1995 Oct 9;695(1):19-24. | ||||
Ref 543793 | (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: 362). |
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