Therapeutic Targets Database
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TTD Target ID: TTDS00111

Target Information
NameVasopressin V2 receptor    
Type of targetSuccessful target    
SynonymsAVPR V2    
Antidiuretic hormone receptor    
Renal-type arginine vasopressin receptor    
DiseaseCerebral edema
[ICD9: 348.5   ICD10: G93.6]
[1]
Congestive heart failure
[ICD9: 428.0   ICD10: I50]
[2][3]
Diabetes insipidus
[ICD9: 253.5, 588.1   ICD10: E23.2, N25.1]
[4][5]
Glaucoma
[ICD9: 365   ICD10: H40-H42]
[6]
Hydronephrosis
[ICD9: 591   ICD10: N13.0-N13.3]
[7]
Hyponatremia
[ICD9: 276.1   ICD10: E87.1]
[8]
Liver cirrhosis[9]
Nephrogenic diabetes insipidus
[ICD9: 250, 253.5, 588.1   ICD10: E08-E13, E23.2, N25.1]
[10]
Ocular hypertension
[ICD9: 365.04   ICD10: H40.0]
[6]
Renal colic
[ICD9: 788.0   ICD10: N23]
[11]
Renal diseases
[ICD9: 580-599   ICD10: N00-N39]
[12]
Syndrome of inappropriate secretion of antidiuretic hormone[2][13]
Von Willebrand's disease
[ICD9: 286.4   ICD10: D68.0]
[14]
Water-retaining diseases[12]
Drug(s)ConivaptanApprovedEuvolemic hyponatremia[15][16]
DesmopressinApprovedPrimary nocturnal enuresis[17]
TolvaptanApprovedHypervolaemic and euvolaemic hyponatraemia[18][19]
VasopressinApprovedEnuresis, polyuria and diabetes insipidus[20]
SatavaptanPhase III completedAcute and chronic heart failure[21]
LixivaptanPhase IIIEuvolemic Hyponatremia; Hypervolemic Hyponatremia[22]
TolvaptanPhase IIIHeart failure[18][19]
LixivaptanPhase IICongestive Heart Failure[22]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP30518
FunctionReceptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.    
SequenceMLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLA ALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQM VGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQ RNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGP SERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEA PLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTT ASSSLAKDTSS
Related US Patent6,235,900
6,268,360
6,297,234
6,344,451
6,620,807
6,627,649
6,664,249
Target ValidationClick to Find Target Validation Information.    
InhibitorARGENINE VASOPRESSIN[23]
ATOSIBAN[24]
GSK-221149A[24]
L-368899,   NCGC00094029-01[25]
L-372662[26]
Mozavaptan[27]
SR-149415[28]
VA-106483[29]
VNA-932,   WAY-VNA-932[30]
YM-35278[31]
d (CH2)5[Tyr[32]
dVDAVP[23]
d[Arg4,Dab8]VP[23]
d[Arg4,Lys8]VP[23]
d[Arg4,Orn8]VP[23]
d[Arg4]AVP[23]
d[Cha4,Dab8]VP[23]
d[Cha4,Dap8]VP[23]
d[Cha4,Lys8]VP[23]
d[Cha4,Orn8]VP[23]
d[Cha4]AVP[23]
d[D-3-Pal2]AVP[23]
d[Leu4,Dab8]VP[23]
d[Leu4,Dap8]VP[23]
d[Leu4,Lys8]VP[23]
d[Leu4,Orn8]VP[23]
d[Leu4]AVP[23]
d[Orn4,Lys8]VP[23]
d[Orn4,Orn8]VP[23]
d[Orn4]AVP[23]
d[Val4]AVP[23]
AgonistDDAVP[14][4][7][5]
Vasopressin[20]
AntagonistCL-385004[2]
Conivaptan[15][16]
FR161282[2]
JTV-605[2]
Lixivaptan[22]
OPC-31260[2][13][3]
SR 121463 A[3]
SR121463[6]
SR121463B[14]
Satavaptan[21]
Satavaptan Lixivaptan[33]
Tolvaptan[18][19]
VP-343[2]
YM 087[3][12]
StimulatorDesmopressin[17]
MultitargetConivaptan[15][16]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Vasopressin receptor antagonist OPC-31260 prevents cerebral oedema after subarachnoid haemorrhage. Eur J Pharmacol. 1999 Jan 8;364(2-3):115-22. To Reference
Ref 2Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Prog Brain Res. 2002;139:197-210. To Reference
Ref 3Nonpeptide vasopressin antagonists: a new group of hormone blockers entering the scene. Exp Clin Endocrinol Diabetes. 1999;107(3):157-65. To Reference
Ref 4The 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. Physiol Behav. 1994 Mar;55(3):407-12. To Reference
Ref 5An extracellular residue determines the agonist specificity of V2 vasopressin receptors. FEBS Lett. 1995 Mar 27;362(1):19-23. To Reference
Ref 6Effect of SR121463, a selective non-peptide vasopressin V2 receptor antagonist, in a rabbit model of ocular hypertension. J Ocul Pharmacol Ther. 2000 Jun;16(3):203-16. To Reference
Ref 7Hydronephrosis: 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. To Reference
Ref 8Correction of hyponatremia. Semin Nephrol. 2001 May;21(3):269-72. To Reference
Ref 9Therapeutic role of vasopressin receptor antagonism in patients with liver cirrhosis. Clin Sci (Lond). 2003 Jul;105(1):1-8. To Reference
Ref 10Nephrogenic diabetes insipidus: clinical symptoms, pathogenesis, genetics and treatment. Pediatr Nephrol. 1992 Sep;6(5):476-82. To Reference
Ref 11Effects of [1-desamino-8-D-arginine]vasopressin and papaverine on rabbit renal pelvis. Eur J Pharmacol. 1990 Jan 17;175(3):359-62. To Reference
Ref 12Pharmacological profile of YM087, a novel nonpeptide dual vasopressin V1A and V2 receptor antagonist, in dogs. Eur J Pharmacol. 1997 Feb 26;321(2):225-30. To Reference
Ref 13Effects 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. To Reference
Ref 14Vasopressin-induced von Willebrand factor secretion from endothelial cells involves V2 receptors and cAMP. J Clin Invest. 2000 Jul;106(1):107-16. To Reference
Ref 15Conivaptan: promise of treatment in heart failure. Expert Opin Pharmacother. 2009 Sep;10(13):2161-9. To Reference
Ref 16Conivaptan: a step forward in the treatment of hyponatremia? Ther Clin Risk Manag. 2008 Apr;4(2):315-26. To Reference
Ref 17Investigational vasopressin receptor modulators in the pipeline. Expert Opin Investig Drugs. 2009 Aug;18(8):1119-31. To Reference
Ref 18Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor. Biochem J. 2009 May 1;419(3):577-84. To Reference
Ref 19Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. To Reference
Ref 20Vasopressin receptors: structure/function relationships and signal transduction in target cells. J Soc Biol. 2005;199(4):351-9. To Reference
Ref 21Post-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. To Reference
Ref 22Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95. To Reference
Ref 23J 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. To Reference
Ref 24Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4. Epub 2007 Nov 6.The discovery of GSK221149A: a potent and selective oxytocin antagonist. To Reference
Ref 25J Med Chem. 1994 Mar 4;37(5):565-71.1-((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo [2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperaz ine (L-368,899): an orally bioavailable, non-peptide oxytocin antagonist with potential utility for managing preterm labor. To Reference
Ref 26J Med Chem. 2010 Sep 23;53(18):6525-38.Oral oxytocin antagonists. To Reference
Ref 27J Med Chem. 1981 May;24(5):496-9.New analgesic drugs derived from phencyclidine. To Reference
Ref 28Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. To Reference
Ref 29J Med Chem. 2008 Dec 25;51(24):8124-34.New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. To Reference
Ref 30J Med Chem. 2010 Feb 25;53(4):1546-62.Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist. To Reference
Ref 31Bioorg 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. To Reference
Ref 32J 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. To Reference
Ref 33Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74. To Reference



 

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