Target Information
Target General Infomation | |||||
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Target ID |
T66237
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Former ID |
TTDS00111
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Target Name |
Vasopressin V2 receptor
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Gene Name |
AVPR2
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Synonyms |
AVPR V2; Antidiuretic hormone receptor; Renal-type arginine vasopressin receptor; AVPR2
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Target Type |
Successful
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Disease | Acute and chronic heart failure [ICD9: 428; ICD10: I50] | ||||
Congestive heart failure [ICD9: 428; ICD10: I50] | |||||
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6] | |||||
Enuresis; Polyuria; Diabetes insipidus [ICD9: 250, 253.5, 307.6, 588.1, 788.30, 788.42; ICD10: E08-E13, E23.2, F98.0, N25.1] | |||||
Euvolemic hyponatremia; Hypervolemic hyponatremia [ICD9: 276.1; ICD10: E87.1] | |||||
Euvolemic hyponatremia [ICD9: 276.1; ICD10: E87.1] | |||||
Hypervolaemic hyponatraemia; Euvolaemic hyponatraemia [ICD9: 276.1; ICD10: E87.1] | |||||
Heart failure [ICD9: 428; ICD10: I50] | |||||
Hyponatraemia [ICD10: E87.1] | |||||
Nocturia [ICD10: R35] | |||||
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32] | |||||
Function |
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Involved in renal water reabsorption.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T66237
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UniProt ID | |||||
Sequence |
MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLA
ALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQM VGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQ RNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGP SERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEA PLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTT ASSSLAKDTSS |
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Drugs and Mode of Action | |||||
Drug(s) | Conivaptan | Drug Info | Approved | Euvolemic hyponatremia | [537060], [539403] |
DDAVP | Drug Info | Approved | Diabetes | [522431] | |
Mozavaptan | Drug Info | Approved | Hyponatraemia | [539396], [544970], [551871] | |
OPC-31260 | Drug Info | Approved | Hyponatraemia | [544970], [551871] | |
Tolvaptan | Drug Info | Approved | Hypervolaemic hyponatraemia; Euvolaemic hyponatraemia | [530677], [539410] | |
Vasopressin | Drug Info | Approved | Enuresis; Polyuria; Diabetes insipidus | [537024], [539373] | |
ATOSIBAN | Drug Info | Phase 4 | Discovery agent | [524034], [539407] | |
Lixivaptan | Drug Info | Phase 3 | Euvolemic hyponatremia; Hypervolemic hyponatremia | [537063], [539415] | |
Satavaptan | Drug Info | Phase 3 | Acute and chronic heart failure | [537062], [539398] | |
SR121463B | Drug Info | Phase 3 | Discovery agent | [521775] | |
Tolvaptan | Drug Info | Phase 3 | Heart failure | [530677], [539410] | |
ASP-7035 | Drug Info | Phase 2 | Nocturia | [548915] | |
Lixivaptan | Drug Info | Phase 2 | Congestive heart failure | [537063], [539415] | |
SPD-556 | Drug Info | Phase 2 | Heart failure | [523132] | |
VA-106483 | Drug Info | Phase 2 | Nocturia | [522905] | |
OPC-51803 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [539376], [546847] | |
OX 19 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [548005] | |
VNA-932 | Drug Info | Discontinued in Phase 1 | Urinary incontinence | [540469], [547176] | |
JTV-605 | Drug Info | Terminated | Dysmenorrhea | [546818] | |
Inhibitor | ARGENINE VASOPRESSIN | Drug Info | [528674] | ||
ATOSIBAN | Drug Info | [529164] | |||
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT | Drug Info | [526347] | |||
DVDAVP | Drug Info | [528674] | |||
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[Orn4,Lys8]VP | Drug Info | [528674] | |||
D[Orn4,Orn8]VP | Drug Info | [528674] | |||
D[Orn4]AVP | Drug Info | [528674] | |||
D[Val4]AVP | Drug Info | [528674] | |||
L-372662 | Drug Info | [530975] | |||
Mozavaptan | Drug Info | [533576] | |||
SR-149415 | Drug Info | [530420] | |||
VA-106483 | Drug Info | [529841] | |||
YM-35278 | Drug Info | [529738] | |||
Agonist | ASP-7035 | Drug Info | [548916] | ||
dAVP | Drug Info | [527042] | |||
DDAVP | Drug Info | [535006], [536397], [537856], [537914] | |||
OPC-51803 | Drug Info | [526938] | |||
OX 19 | Drug Info | [527914] | |||
Vasopressin | Drug Info | [536236] | |||
VNA-932 | Drug Info | [544100], [551871] | |||
[3H]OT (human, mouse, rat) | Drug Info | [543798] | |||
[Phe3]OT | Drug Info | [533733] | |||
[Val4]AVP | Drug Info | [526466] | |||
Antagonist | CL-385004 | Drug Info | [535608] | ||
d(CH2)5[D-Ile2,Ile4]AVP | Drug Info | [525878] | |||
d(CH2)5[Tyr(Me)2]AVP | Drug Info | [525878] | |||
d[Pen1,Tyr(Me)2]AVP | Drug Info | [525878] | |||
FR161282 | Drug Info | [535608] | |||
JTV-605 | Drug Info | [535608] | |||
Lixivaptan | Drug Info | [536372] | |||
OPC-31260 | Drug Info | [534873], [535116], [535608] | |||
Satavaptan | Drug Info | [537062] | |||
SPD-556 | Drug Info | [543798] | |||
SR 121463 A | Drug Info | [534873] | |||
SR121463B | Drug Info | [535006] | |||
Tolvaptan | Drug Info | [530677], [537061] | |||
VP-343 | Drug Info | [535608] | |||
YM 218 | Drug Info | [527388] | |||
YM 471 | Drug Info | [526095] | |||
[3H]SR 121463A | Drug Info | [534299] | |||
Modulator | Conivaptan | Drug Info | [526189], [529082] | ||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Vasopressin-regulated water reabsorption | |||||
Pathway Interaction Database | Arf6 trafficking events | ||||
PathWhiz Pathway | Vasopressin Regulation of Water Homeostasis | ||||
Reactome | Vasopressin-like receptors | ||||
G alpha (s) signalling events | |||||
Vasopressin regulates renal water homeostasis via Aquaporins | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Regulation of Water Balance by Renal Aquaporins | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 521775 | ClinicalTrials.gov (NCT00264914) Safety and Efficacy of SR121463B in Patients With Syndrome of Inappropriate Antidiuretic Hormone Secretion. U.S. National Institutes of Health. | ||||
Ref 522431 | ClinicalTrials.gov (NCT00748072) 1-deamino 8-d-arginine Vasopressin (DDAVP) in Percutaneous Ultrasound-guided Renal Biopsy. U.S. National Institutes of Health. | ||||
Ref 522905 | ClinicalTrials.gov (NCT01038843) Efficacy Study of VA106483 in Males With Nocturia.. U.S. National Institutes of Health. | ||||
Ref 523132 | ClinicalTrials.gov (NCT01179607) Study of Efficacy of a Vasopressin 2 Receptor Antagonist M0002 for Treatment of Ascites in Cirrhotic Subjects With Hypo- or Normonatraemia. U.S. National Institutes of Health. | ||||
Ref 524034 | ClinicalTrials.gov (NCT01673399) Oxytocin Antagonist in Patients With Repeated Failure of Implantation. U.S. National Institutes of Health. | ||||
Ref 537024 | New topics in vasopressin receptors and approach to novel drugs: research and development of conivaptan hydrochloride (YM087), a drug for the treatment of hyponatremia. J Pharmacol Sci. 2009 Jan;109(1):53-9. | ||||
Ref 537060 | Emerging diuretics for the treatment of heart failure. Expert Opin Emerg Drugs. 2009 Mar;14(1):195-204. | ||||
Ref 537062 | Post-translational import of protein into the endoplasmic reticulum of a trypanosome: an in vitro system for discovery of anti-trypanosomal chemical entities. Biochem J. 2009 Apr 15;419(2):507-17. | ||||
Ref 537063 | Physical state of kappa-carrageenan modulates the mode of action of kappa-carrageenase from Pseudoalteromonas carrageenovora. Biochem J. 2009 May 1;419(3):545-53. | ||||
Ref 539373 | (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: 2168). | ||||
Ref 539376 | (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: 2173). | ||||
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 539398 | (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: 2199). | ||||
Ref 539403 | (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: 2203). | ||||
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 539410 | (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: 2226). | ||||
Ref 539415 | (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: 2238). | ||||
Ref 540469 | (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: 3537). | ||||
Ref 544970 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001739) | ||||
Ref 546818 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010443) | ||||
Ref 546847 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010599) | ||||
Ref 547176 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013621) | ||||
Ref 548005 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021110) | ||||
Ref 525878 | Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463. Kidney Int. 2000 Oct;58(4):1613-22. | ||||
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 526189 | Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation. 2001 Nov 13;104(20):2417-23. | ||||
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 526938 | Effects of OPC-51803, a novel, nonpeptide vasopressin V2-receptor agonist, on micturition frequency in Brattleboro and aged rats. J Pharmacol Sci. 2003 Dec;93(4):484-8. | ||||
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 527914 | Investigation of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors: molecular dynamics simulation of the agonist-bound state in the membrane-aqueous system. Biopolymers. 2006 Apr 5;81(5):321-38. | ||||
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 529082 | Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79. | ||||
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 529738 | Bioorg Med Chem. 2008 Nov 1;16(21):9524-35. Epub 2008 Sep 17.Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists. | ||||
Ref 529841 | J Med Chem. 2008 Dec 25;51(24):8124-34.New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. | ||||
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 533733 | Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J. 1995 May 15;14(10):2176-82. | ||||
Ref 534299 | Characterization of SR 121463A, a highly potent and selective, orally active vasopressin V2 receptor antagonist. J Clin Invest. 1996 Dec 15;98(12):2729-38. | ||||
Ref 534873 | Nonpeptide vasopressin antagonists: a new group of hormone blockers entering the scene. Exp Clin Endocrinol Diabetes. 1999;107(3):157-65. | ||||
Ref 535006 | Vasopressin-induced von Willebrand factor secretion from endothelial cells involves V2 receptors and cAMP. J Clin Invest. 2000 Jul;106(1):107-16. | ||||
Ref 535116 | Effects of an oral vasopressin receptor antagonist (OPC-31260) in a dog with syndrome of inappropriate secretion of antidiuretic hormone. Aust Vet J. 2000 Dec;78(12):825-30. | ||||
Ref 535608 | Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Prog Brain Res. 2002;139:197-210. | ||||
Ref 536236 | Vasopressin receptors: structure/function relationships and signal transduction in target cells. J Soc Biol. 2005;199(4):351-9. | ||||
Ref 536372 | Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. | ||||
Ref 536397 | Hydronephrosis: prevention by restoration of urinary concentrating ability using desamino-8D-arginine vasopressin (DDAVP) in Brattleboro rats. Int J Exp Pathol. 1991 Oct;72(5):581-7. | ||||
Ref 537061 | Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor. Biochem J. 2009 May 1;419(3):577-84. | ||||
Ref 537062 | Post-translational import of protein into the endoplasmic reticulum of a trypanosome: an in vitro system for discovery of anti-trypanosomal chemical entities. Biochem J. 2009 Apr 15;419(2):507-17. | ||||
Ref 537856 | An extracellular residue determines the agonist specificity of V2 vasopressin receptors. FEBS Lett. 1995 Mar 27;362(1):19-23. | ||||
Ref 537914 | The abnormal quinine drinking aversion in the Brattleboro rat with diabetes insipidus is reversed by the vasopressin agonist DDAVP: a possible role for vasopressin in the motivation to drink. PhysiolBehav. 1994 Mar;55(3):407-12. | ||||
Ref 543798 | (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: 368). | ||||
Ref 544100 | Biased Agonist Pharmacochaperones of the AVP V2 Receptor May Treat Congenital Nephrogenic Diabetes Insipidus. J Am Soc Nephrol. 2009 October; 20(10): 2190-2203. |
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