Target Validation Information
TTD ID	T59881
Target Name	Vasopressin V1b receptor (V1BR)
Type of Target	Successful
Drug Potency against Target	SSR149415	Drug Info	Ki = 0.457 nM	[7]
	ARGENINE VASOPRESSIN	Drug Info	Ki = 0.29 nM	[2]
	ATOSIBAN	Drug Info	Ki = 44 nM	[4]
	D[Arg4,Dab8]VP	Drug Info	Ki = 0.19 nM	[2]
	D[Arg4,Lys8]VP	Drug Info	Ki = 0.6 nM	[2]
	D[Arg4,Orn8]VP	Drug Info	Ki = 0.6 nM	[2]
	D[Arg4]AVP	Drug Info	Ki = 0.13 nM	[2]
	D[Cha4,Dab8]VP	Drug Info	Ki = 0.8 nM	[2]
	D[Cha4,Dap8]VP	Drug Info	Ki = 10 nM	[2]
	D[Cha4,Lys8]VP	Drug Info	Ki = 1.9 nM	[2]
	D[Cha4,Orn8]VP	Drug Info	Ki = 3 nM	[2]
	D[Cha4]AVP	Drug Info	Ki = 1.4 nM	[2]
	D[D-3-Pal2]AVP	Drug Info	Ki = 112 nM	[2]
	D[Leu4,Dab8]VP	Drug Info	Ki = 0.25 nM	[2]
	D[Leu4,Dap8]VP	Drug Info	Ki = 0.38 nM	[2]
	D[Leu4,Lys8]VP	Drug Info	Ki = 0.16 nM	[2]
	D[Leu4,Orn8]VP	Drug Info	Ki = 0.26 nM	[2]
	D[Lys8(5/6-Flu)]VT	Drug Info	Ki = 124 nM	[1]
	D[Orn4,Lys8]VP	Drug Info	Ki = 0.45 nM	[2]
	D[Orn4,Orn8]VP	Drug Info	Ki = 0.91 nM	[2]
	D[Orn4]AVP	Drug Info	Ki = 0.45 nM	[2]
	D[Orn8(5/6C-Flu)]VT	Drug Info	Ki = 393 nM	[1]
	D[Thr4,Lys8(5/6C-Flu)]VT	Drug Info	Ki = 150 nM	[1]
	D[Thr4,Orn8(5/6C-Flu)]VT	Drug Info	Ki = 282 nM	[1]
	D[Val4]AVP	Drug Info	Ki = 0.25 nM	[2]
	Mozavaptan	Drug Info	IC50 = 5000 nM	[6]
	SSR149415	Drug Info	Ki = 1 nM	[5]
	[HO1][Lys8(5/6C-Flu)]VT	Drug Info	Ki = 66 nM	[1]
	[HO1][Orn8(5/6C-Flu)]VT	Drug Info	Ki = 126 nM	[1]
	[HO1][Thr4,Lys8(5/6C-Flu)]VT	Drug Info	Ki = 53 nM	[1]
	[HO1][Thr4,Orn8(5/6C-Flu)]VT	Drug Info	Ki = 87 nM	[1]
	[Lys8(Alexa 488) ]PVA	Drug Info	Ki = 100 nM	[3]
Action against Disease Model	SSR149415	Drug Info	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.	[8]
References
REF 1	Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors. J Med Chem. 2002 Jun 6;45(12):2579-88.
REF 2	Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasop... J Med Chem. 2007 Feb 22;50(4):835-47.
REF 3	Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands. J Med Chem. 2007 Oct 4;50(20):4976-85.
REF 4	The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
REF 5	Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
REF 6	New analgesic drugs derived from phencyclidine. J Med Chem. 1981 May;24(5):496-9.
REF 7	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 8	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.

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