Target Information
Target General Infomation | |||||
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Target ID |
T59881
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Former ID |
TTDC00298
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Target Name |
Vasopressin V1b receptor
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Gene Name |
AVPR1B
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Synonyms |
AVPR V1b; AVPR V3; Antidiuretic hormone receptor 1b; V1bR; Vasopressin V(1b) Receptor; Vasopressin V3 receptor; AVPR1B
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Target Type |
Successful
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Disease | Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | ||||
Hyponatraemia [ICD10: E87.1] | |||||
Major depressive disorder; Anxiety [ICD9: 300; ICD10: F40-F42] | |||||
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | |||||
Function |
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl- inositol-calcium second messenger system.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T59881
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UniProt ID | |||||
Sequence |
MDSGPLWDANPTPRGTLSAPNATTPWLGRDEELAKVEIGVLATVLVLATGGNLAVLLTLG
QLGRKRSRMHLFVLHLALTDLAVALFQVLPQLLWDITYRFQGPDLLCRAVKYLQVLSMFA STYMLLAMTLDRYLAVCHPLRSLQQPGQSTYLLIAAPWLLAAIFSLPQVFIFSLREVIQG SGVLDCWADFGFPWGPRAYLTWTTLAIFVLPVTMLTACYSLICHEICKNLKVKTQAWRVG GGGWRTWDRPSPSTLAATTRGLPSRVSSINTISRAKIRTVKMTFVIVLAYIACWAPFFSV QMWSVWDKNAPDEDSTNVAFTISMLLGNLNSCCNPWIYMGFNSHLLPRPLRHLACCGGPQ PRMRRRLSDGSLSSRHTTLLTRSSCPATLSLSLSLTLSGRPRPEESPRDLELADGEGTAE TIIF |
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Drugs and Mode of Action | |||||
Modulator | ABT-436 | Drug Info | [544158] | ||
Inhibitor | ARGENINE VASOPRESSIN | Drug Info | [528674] | ||
ATOSIBAN | Drug Info | [529164] | |||
D[Arg4,Dab8]VP | Drug Info | [528674] | |||
D[Arg4,Lys8]VP | Drug Info | [528674] | |||
D[Arg4,Orn8]VP | Drug Info | [528674] | |||
D[Arg4]AVP | Drug Info | [528674] | |||
D[Cha4,Dab8]VP | Drug Info | [528674] | |||
D[Cha4,Dap8]VP | Drug Info | [528674] | |||
D[Cha4,Lys8]VP | Drug Info | [528674] | |||
D[Cha4,Orn8]VP | Drug Info | [528674] | |||
D[Cha4]AVP | Drug Info | [528674] | |||
D[D-3-Pal2]AVP | Drug Info | [528674] | |||
D[Leu4,Dab8]VP | Drug Info | [528674] | |||
D[Leu4,Dap8]VP | Drug Info | [528674] | |||
D[Leu4,Lys8]VP | Drug Info | [528674] | |||
D[Leu4,Orn8]VP | Drug Info | [528674] | |||
D[Leu4]AVP | Drug Info | [528674] | |||
D[Lys8(5/6-Flu)]VT | Drug Info | [526347] | |||
D[Orn4,Lys8]VP | Drug Info | [528674] | |||
D[Orn4,Orn8]VP | Drug Info | [528674] | |||
D[Orn4]AVP | Drug Info | [528674] | |||
D[Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Thr4,Lys8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
D[Val4]AVP | Drug Info | [528674] | |||
Mozavaptan | Drug Info | [533576] | |||
SR-149415 | Drug Info | [530420] | |||
[HO1][Lys8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[HO1][Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[HO1][Thr4,Lys8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[HO1][Thr4,Orn8(5/6C-Flu)]VT | Drug Info | [526347] | |||
[Lys8(Alexa 488) ]PVA | Drug Info | [529036] | |||
Antagonist | d(CH2)5[Tyr(Me)2]AVP | Drug Info | [534447] | ||
d[Pen1,Tyr(Me)2]AVP | Drug Info | [534813] | |||
Small molecule 2a | Drug Info | [543797] | |||
SSR149415 | Drug Info | [536580] | |||
YM 218 | Drug Info | [527388] | |||
YM 471 | Drug Info | [526095] | |||
[3H]nelivaptan | Drug Info | [543797] | |||
Agonist | dAVP | Drug Info | [527042] | ||
[3H]OT (human, mouse, rat) | Drug Info | [534481] | |||
[Val4]AVP | Drug Info | [526466] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Vascular smooth muscle contraction | |||||
Reactome | Vasopressin-like receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 524034 | ClinicalTrials.gov (NCT01673399) Oxytocin Antagonist in Patients With Repeated Failure of Implantation. U.S. National Institutes of Health. | ||||
Ref 524149 | ClinicalTrials.gov (NCT01741142) Efficacy and Safety Study of ABT-436 in Major Depressive Disorder. U.S. National Institutes of Health. | ||||
Ref 535432 | Anxiolytic- and antidepressant-like effects of the non-peptide vasopressin V1b receptor antagonist, SSR149415, suggest an innovative approach for the treatment of stress-related disorders. Proc Natl Acad Sci U S A. 2002 Apr 30;99(9):6370-5. Epub 2002 Apr 16. | ||||
Ref 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
Ref 539396 | (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: 2197). | ||||
Ref 539402 | (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: 2202). | ||||
Ref 539407 | (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: 2213). | ||||
Ref 526095 | Effects of YM471, a nonpeptide AVP V(1A) and V(2) receptor antagonist, on human AVP receptor subtypes expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells. Br J Pharmacol. 2001 Jul;133(5):746-54. | ||||
Ref 526347 | J Med Chem. 2002 Jun 6;45(12):2579-88.Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. | ||||
Ref 526466 | [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology. 2002 Dec;143(12):4655-64. | ||||
Ref 527042 | Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem. 2004 Apr 22;47(9):2375-88. | ||||
Ref 527388 | Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res. 2005 Mar;51(3):275-81. | ||||
Ref 528674 | J Med Chem. 2007 Feb 22;50(4):835-47.Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8. | ||||
Ref 529036 | J Med Chem. 2007 Oct 4;50(20):4976-85. Epub 2007 Sep 12.Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. | ||||
Ref 529164 | Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. Epub 2007 Nov 6.The discovery of GSK221149A: a potent and selective oxytocin antagonist. | ||||
Ref 530420 | Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. | ||||
Ref 534447 | 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor. Biochem Pharmacol. 1997 Jun 1;53(11):1711-7. | ||||
Ref 534481 | The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways. Endocrinology. 1997 Oct;138(10):4109-22. | ||||
Ref 534813 | Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 1998 Dec;125(7):1463-70. | ||||
Ref 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. |
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