Target Validation Information
Target ID T59881
Target Name Vasopressin V1b receptor
Target Type
Successful
Drug Potency against Target SR-149415 Drug Info Ki = 1 nM [530420]
SSR149415 Drug Info Ki = 0.457 nM [552546]
D[Orn4]AVP Drug Info Ki = 0.45 nM [528674]
D[Leu4,Dap8]VP Drug Info Ki = 0.38 nM [528674]
D[Orn4,Orn8]VP Drug Info Ki = 0.91 nM [528674]
D[Orn4,Lys8]VP Drug Info Ki = 0.45 nM [528674]
D[Cha4,Orn8]VP Drug Info Ki = 3 nM [528674]
D[Arg4,Dab8]VP Drug Info Ki = 0.19 nM [528674]
D[Val4]AVP Drug Info Ki = 0.25 nM [528674]
D[Cha4,Lys8]VP Drug Info Ki = 1.9 nM [528674]
D[Arg4,Orn8]VP Drug Info Ki = 0.6 nM [528674]
[Lys8(Alexa 488) ]PVA Drug Info Ki = 100 nM [529036]
D[Orn8(5/6C-Flu)]VT Drug Info Ki = 393 nM [526347]
[HO1][Orn8(5/6C-Flu)]VT Drug Info Ki = 126 nM [526347]
D[Lys8(5/6-Flu)]VT Drug Info Ki = 124 nM [526347]
[HO1][Lys8(5/6C-Flu)]VT Drug Info Ki = 66 nM [526347]
D[Arg4]AVP Drug Info Ki = 0.13 nM [528674]
D[Cha4,Dab8]VP Drug Info Ki = 0.8 nM [528674]
D[Leu4,Orn8]VP Drug Info Ki = 0.26 nM [528674]
D[Leu4,Lys8]VP Drug Info Ki = 0.16 nM [528674]
D[Arg4,Lys8]VP Drug Info Ki = 0.6 nM [528674]
D[Cha4]AVP Drug Info Ki = 1.4 nM [528674]
Mozavaptan Drug Info IC50 = 5000 nM [533576]
D[Cha4,Dap8]VP Drug Info Ki = 10 nM [528674]
D[D-3-Pal2]AVP Drug Info Ki = 112 nM [528674]
ARGENINE VASOPRESSIN Drug Info Ki = 0.29 nM [528674]
D[Leu4,Dab8]VP Drug Info Ki = 0.25 nM [528674]
D[Thr4,Lys8(5/6C-Flu)]VT Drug Info Ki = 150 nM [526347]
D[Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 282 nM [526347]
[HO1][Thr4,Orn8(5/6C-Flu)]VT Drug Info Ki = 87 nM [526347]
[HO1][Thr4,Lys8(5/6C-Flu)]VT Drug Info Ki = 53 nM [526347]
ATOSIBAN Drug Info Ki = 44 nM [529164]
Action against Disease Model SSR149415 An arginine vasopressin V1b antagonist, SSR149415 elicits antidepressant-like effects in an olfactory bulbectomy model.oral chronic treatment with SSR149415 (10 and 30 mg/kg) orCP-154,526 (10 mg/kg) significantly reduced hyperemotionality. [552667] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations V1a and V1b receptor transcripts were absent in the islets from V1a-KO and V1b-KO, respectively.Arginine vasopressin-induced acc uMulation of insulin release from cultured isletcells was similar for the V1a-KO and wild-type control mouse. However, AVP-stimulated insulin release from the islet cells was completely lost in V1b-KO mice. V1b receptor subtype is fully operative in mouse pancreatic islet cells and that AVP-mediated insulin release seems to occur solely via the V1b receptor [552667]
References
Ref 552667An arginine vasopressin V1b antagonist, SSR149415 elicits antidepressant-like effects in an olfactory bulbectomy model. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Apr 13;31(3):622-7. Epub 2006 Dec 15.
Ref 530420Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.
Ref 552546Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. Br J Pharmacol. 2005 Nov;146(5):744-51.
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 533576J Med Chem. 1981 May;24(5):496-9.New analgesic drugs derived from phencyclidine.
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 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 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 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 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 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 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 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 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.

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