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 552667 | An 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 530420 | Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. Epub 2009 Sep 17.Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. | ||||
Ref 552546 | Selectivity 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 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 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 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 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 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 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 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 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 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 529036 | J 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 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 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 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 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 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 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 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 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 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 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 533576 | J Med Chem. 1981 May;24(5):496-9.New analgesic drugs derived from phencyclidine. | ||||
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 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 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 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 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 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 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 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 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. |
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