Target Information

Target General Infomation
Target ID
T59881
Former ID
TTDC00298
Target Name
Vasopressin V1b receptor
Gene Name
AVPR1B
Synonyms
AVPR V1b; AVPR V3; Antidiuretic hormone receptor 1b; V1bR; Vasopressin V(1b) Receptor; Vasopressin V3 receptor; AVPR1B
Target Type
Successful
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T59881
UniProt ID
P47901
Sequence
MDSGPLWDANPTPRGTLSAPNATTPWLGRDEELAKVEIGVLATVLVLATGGNLAVLLTLG
QLGRKRSRMHLFVLHLALTDLAVALFQVLPQLLWDITYRFQGPDLLCRAVKYLQVLSMFA
STYMLLAMTLDRYLAVCHPLRSLQQPGQSTYLLIAAPWLLAAIFSLPQVFIFSLREVIQG
SGVLDCWADFGFPWGPRAYLTWTTLAIFVLPVTMLTACYSLICHEICKNLKVKTQAWRVG
GGGWRTWDRPSPSTLAATTRGLPSRVSSINTISRAKIRTVKMTFVIVLAYIACWAPFFSV
QMWSVWDKNAPDEDSTNVAFTISMLLGNLNSCCNPWIYMGFNSHLLPRPLRHLACCGGPQ
PRMRRRLSDGSLSSRHTTLLTRSSCPATLSLSLSLTLSGRPRPEESPRDLELADGEGTAE
TIIF
Drugs and Mode of Action
Drug(s) Mozavaptan Drug Info Approved Hyponatraemia [539396], [544970], [551871]
ATOSIBAN Drug Info Phase 4 Discovery agent [524034], [539407]
ABT-436 Drug Info Phase 2 Anxiety disorder [524149]
SSR149415 Drug Info Phase 2 Major depressive disorder; Anxiety [535432], [536580], [539402]
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 524034ClinicalTrials.gov (NCT01673399) Oxytocin Antagonist in Patients With Repeated Failure of Implantation. U.S. National Institutes of Health.
Ref 524149ClinicalTrials.gov (NCT01741142) Efficacy and Safety Study of ABT-436 in Major Depressive Disorder. U.S. National Institutes of Health.
Ref 535432Anxiolytic- 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 536580Novel 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 544970Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001739)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526095Effects 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 526347J 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 527042Design 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 527388Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res. 2005 Mar;51(3):275-81.
Ref 528674J 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 529036J 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 529164Bioorg 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 530420Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Ref 533576J Med Chem. 1981 May;24(5):496-9.New analgesic drugs derived from phencyclidine.
Ref 5344471-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor. Biochem Pharmacol. 1997 Jun 1;53(11):1711-7.
Ref 534481The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways. Endocrinology. 1997 Oct;138(10):4109-22.
Ref 534813Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 1998 Dec;125(7):1463-70.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 543797(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: 367).
Ref 544158The vasopressin Avprlb receptor: Molecular and pharmacological studies. Stress. 2011 January; 14(1): 98-115.

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