Details of the Drug-Related molecule(s) Interaction Atlas

General Information of DTT (ID: TTK8R02)

• DTT Name: Vasopressin V2 receptor (V2R) DTT Info
• Gene Name: AVPR2

Molecule-Related Drug & Molecule List

7 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Conivaptan	DM1V329	Euvolemic hyponatremia	5C72	Approved	[1]
Desmopressin	DMS3GVE	Diabetic complication	5A2Y	Approved	[2]
Mozavaptan	DMZ905C	Hyponatraemia	5C72	Approved	[3]
Oxytocin	DMDL27I	Autism spectrum disorder	6A02	Approved	[4]
Tolvaptan	DMIWFRL	Autosomal dominant polycystic kidney disease	GB81	Approved	[5]
Vasopressin	DMQ2FPC	Diabetes insipidus	5A61.5	Approved	[6]
ATOSIBAN	DMB7WYM	N. A.	N. A.	Phase 4	[7]

6 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lixivaptan	DMDN4ZP	Hyponatraemia	5C72	Phase 3	[8]
Satavaptan	DME5PN3	Acute and chronic heart failure	BD1Z	Phase 3	[9]
ASP-7035	DMTF24A	Nocturia	MF55	Phase 2	[10]
SPD-556	DM9OPK3	Heart failure	BD10-BD13	Phase 2	[4]
SSR149415	DMCMD93	Anxiety disorder	6B00-6B0Z	Phase 2	[11]
VA-106483	DM1ODP6	Nocturia	MF55	Phase 2	[12]

4 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OPC-51803	DMDCOSP	Urinary incontinence	MF50.2	Discontinued in Phase 1	[13]
OX 19	DM5UYI7	Urinary incontinence	MF50.2	Discontinued in Phase 1	[14]
VNA-932	DMKRG0I	Urinary incontinence	MF50.2	Discontinued in Phase 1	[15]
JTV-605	DM89TXB	Dysmenorrhea	GA34.3	Terminated	[3]

34 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ARGENINE VASOPRESSIN	DM8KN0Q	Discovery agent	N.A.	Investigative	[16]
CL-385004	DMLQZGJ	Discovery agent	N.A.	Investigative	[3]
d(CH2)5[D-Ile2,Ile4]AVP	DMAX7LW	Discovery agent	N.A.	Investigative	[17]
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT	DM1BMT7	Discovery agent	N.A.	Investigative	[18]
d(CH2)5[Tyr(Me)2]AVP	DMHTSAX	Discovery agent	N.A.	Investigative	[17]
DVDAVP	DM53079	Discovery agent	N.A.	Investigative	[16]
D[Arg4,Dab8]VP	DMCU8HK	Discovery agent	N.A.	Investigative	[16]
D[Arg4,Lys8]VP	DM69OVM	Discovery agent	N.A.	Investigative	[16]
D[Arg4,Orn8]VP	DM8D4QT	Discovery agent	N.A.	Investigative	[16]
D[Arg4]AVP	DM76Q2B	Discovery agent	N.A.	Investigative	[16]
D[Cha4,Dab8]VP	DMCLUXI	Discovery agent	N.A.	Investigative	[16]
D[Cha4,Dap8]VP	DMAPZKB	Discovery agent	N.A.	Investigative	[16]
D[Cha4,Lys8]VP	DM0GO7U	Discovery agent	N.A.	Investigative	[16]
D[Cha4,Orn8]VP	DMZWTJK	Discovery agent	N.A.	Investigative	[16]
D[Cha4]AVP	DM8FCX5	Discovery agent	N.A.	Investigative	[16]
D[D-3-Pal2]AVP	DMD4V6U	Discovery agent	N.A.	Investigative	[16]
D[Leu4,Dab8]VP	DMNSXG9	Discovery agent	N.A.	Investigative	[16]
D[Leu4,Dap8]VP	DME3HK8	Discovery agent	N.A.	Investigative	[16]
D[Leu4,Lys8]VP	DMDBU7Q	Discovery agent	N.A.	Investigative	[16]
D[Leu4,Orn8]VP	DMJCW8Y	Discovery agent	N.A.	Investigative	[16]
D[Leu4]AVP	DMREZT7	Discovery agent	N.A.	Investigative	[16]
D[Orn4,Lys8]VP	DMNQTBU	Discovery agent	N.A.	Investigative	[16]
D[Orn4,Orn8]VP	DMONV0M	Discovery agent	N.A.	Investigative	[16]
D[Orn4]AVP	DMJNT95	Discovery agent	N.A.	Investigative	[16]
d[Pen1,Tyr(Me)2]AVP	DMT8KI6	Discovery agent	N.A.	Investigative	[17]
D[Val4]AVP	DM3GM8E	Discovery agent	N.A.	Investigative	[16]
FR161282	DMZSFEP	Discovery agent	N.A.	Investigative	[3]
L-372662	DMQV974	Discovery agent	N.A.	Investigative	[19]
VP-343	DMT03VB	Discovery agent	N.A.	Investigative	[3]
YM 218	DMPYM3J	Discovery agent	N.A.	Investigative	[20]
YM 471	DM5BFL4	Discovery agent	N.A.	Investigative	[21]
YM-35278	DMXRZ6N	Discovery agent	N.A.	Investigative	[22]
[Phe3]OT	DMK18CS	Discovery agent	N.A.	Investigative	[23]
[Val4]AVP	DMW82ZT	Discovery agent	N.A.	Investigative	[24]

References

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• [2] 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.
• [3] Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Prog Brain Res. 2002;139:197-210.
• [4] URL: 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).
• [5] Antibody-mediated disruption of the interaction between PCSK9 and the low-density lipoprotein receptor. Biochem J. 2009 May 1;419(3):577-84.
• [6] Vasopressin receptors: structure/function relationships and signal transduction in target cells. J Soc Biol. 2005;199(4):351-9.
• [7] The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
• [8] Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.
• [9] 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.
• [10] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030285)
• [11] Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
• [12] New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. J Med Chem. 2008 Dec 25;51(24):8124-34.
• [13] 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.
• [14] 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.
• [15] Biased Agonist Pharmacochaperones of the AVP V2 Receptor May Treat Congenital Nephrogenic Diabetes Insipidus. J Am Soc Nephrol. 2009 October; 20(10): 2190-2203.
• [16] 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.
• [17] Binding properties of a selective tritiated vasopressin V2 receptor antagonist, [H]-SR 121463. Kidney Int. 2000 Oct;58(4):1613-22.
• [18] 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.
• [19] Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38.
• [20] Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res. 2005 Mar;51(3):275-81.
• [21] 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.
• [22] 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. Bioorg Med Chem. 2008 Nov 1;16(21):9524-35.
• [23] Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J. 1995 May 15;14(10):2176-82.
• [24] [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology. 2002 Dec;143(12):4655-64.