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 [1], [2], [3]
ATOSIBAN Drug Info Phase 4 Discovery agent [4], [5]
ABT-436 Drug Info Phase 2 Anxiety disorder [6]
SSR149415 Drug Info Phase 2 Major depressive disorder; Anxiety [7], [8], [9]
Modulator ABT-436 Drug Info [10]
Inhibitor ARGENINE VASOPRESSIN Drug Info [11]
ATOSIBAN Drug Info [12]
D[Arg4,Dab8]VP Drug Info [11]
D[Arg4,Lys8]VP Drug Info [11]
D[Arg4,Orn8]VP Drug Info [11]
D[Arg4]AVP Drug Info [11]
D[Cha4,Dab8]VP Drug Info [11]
D[Cha4,Dap8]VP Drug Info [11]
D[Cha4,Lys8]VP Drug Info [11]
D[Cha4,Orn8]VP Drug Info [11]
D[Cha4]AVP Drug Info [11]
D[D-3-Pal2]AVP Drug Info [11]
D[Leu4,Dab8]VP Drug Info [11]
D[Leu4,Dap8]VP Drug Info [11]
D[Leu4,Lys8]VP Drug Info [11]
D[Leu4,Orn8]VP Drug Info [11]
D[Leu4]AVP Drug Info [11]
D[Lys8(5/6-Flu)]VT Drug Info [13]
D[Orn4,Lys8]VP Drug Info [11]
D[Orn4,Orn8]VP Drug Info [11]
D[Orn4]AVP Drug Info [11]
D[Orn8(5/6C-Flu)]VT Drug Info [13]
D[Thr4,Lys8(5/6C-Flu)]VT Drug Info [13]
D[Thr4,Orn8(5/6C-Flu)]VT Drug Info [13]
D[Val4]AVP Drug Info [11]
Mozavaptan Drug Info [14]
SR-149415 Drug Info [15]
[HO1][Lys8(5/6C-Flu)]VT Drug Info [13]
[HO1][Orn8(5/6C-Flu)]VT Drug Info [13]
[HO1][Thr4,Lys8(5/6C-Flu)]VT Drug Info [13]
[HO1][Thr4,Orn8(5/6C-Flu)]VT Drug Info [13]
[Lys8(Alexa 488) ]PVA Drug Info [16]
Antagonist d(CH2)5[Tyr(Me)2]AVP Drug Info [17]
d[Pen1,Tyr(Me)2]AVP Drug Info [18]
Small molecule 2a Drug Info [19]
SSR149415 Drug Info [8]
YM 218 Drug Info [20]
YM 471 Drug Info [21]
[3H]nelivaptan Drug Info [19]
Agonist dAVP Drug Info [22]
[3H]OT (human, mouse, rat) Drug Info [23]
[Val4]AVP Drug Info [24]
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 1(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 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001739)
REF 3Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 4ClinicalTrials.gov (NCT01673399) Oxytocin Antagonist in Patients With Repeated Failure of Implantation. U.S. National Institutes of Health.
REF 5(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 6ClinicalTrials.gov (NCT01741142) Efficacy and Safety Study of ABT-436 in Major Depressive Disorder. U.S. National Institutes of Health.
REF 7Anxiolytic- 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 8Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
REF 9(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 10The vasopressin Avprlb receptor: Molecular and pharmacological studies. Stress. 2011 January; 14(1): 98-115.
REF 11J 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 12Bioorg 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 13J 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 14J Med Chem. 1981 May;24(5):496-9.New analgesic drugs derived from phencyclidine.
REF 15Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
REF 16J 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 171-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor. Biochem Pharmacol. 1997 Jun 1;53(11):1711-7.
REF 18Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 1998 Dec;125(7):1463-70.
REF 19(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 20Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res. 2005 Mar;51(3):275-81.
REF 21Effects 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 22Design 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 23The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways. Endocrinology. 1997 Oct;138(10):4109-22.
REF 24[1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology. 2002 Dec;143(12):4655-64.

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