Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTK8R02)

• DTT Name: Vasopressin V2 receptor (V2R)
• Synonyms: Renal-type arginine vasopressin receptor; DIR3; DIR; Antidiuretic hormone receptor; AVPR V2; ADHR
• Gene Name: AVPR2
• DTT Type: Successful target; [1]
• Related Disease:
  Acute diabete complication [ICD-11: 5A2Y]
  Autism spectrum disorder [ICD-11: 6A02]
  Enuresis [ICD-11: 6C00]
  Hypo-osmolality/hyponatraemia [ICD-11: 5C72]
  Pituitary gland disorder [ICD-11: 5A60-5A61]
  Polyuria [ICD-11: MF55]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: V2R_HUMAN
• TTD ID: T66237
• Sequence:
  MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLA
  ALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQM
  VGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQ
  RNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGP
  SERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEA
  PLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTT
  ASSSLAKDTSS
• Function: The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Involved in renal water reabsorption. Receptor for arginine vasopressin.
• Reactome Pathway:
  G alpha (s) signalling events (R-HSA-418555)
  Vasopressin regulates renal water homeostasis via Aquaporins (R-HSA-432040)
  Vasopressin-like receptors (R-HSA-388479)

Molecular Interaction Atlas (MIA) of This DTT

7 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Conivaptan	DM1V329	Euvolemic hyponatremia	5C72	Approved	[2], [3]
Desmopressin	DMS3GVE	Diabetic complication	5A2Y	Approved	[4], [5], [6], [7], [8]
Mozavaptan	DMZ905C	Hyponatraemia	5C72	Approved	[9], [10], [11], [12]
Oxytocin	DMDL27I	Autism spectrum disorder	6A02	Approved	[13]
Tolvaptan	DMIWFRL	Hyponatraemia	5C72	Approved	[14], [15]
Vasopressin	DMQ2FPC	Diabetes insipidus	5A61.5	Approved	[1]
ATOSIBAN	DMB7WYM	N. A.	N. A.	Phase 4	[16]

6 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lixivaptan	DMDN4ZP	Hyponatraemia	5C72	Phase 3	[17]
Satavaptan	DME5PN3	Acute and chronic heart failure	BD1Z	Phase 3	[18], [11], [5]
ASP-7035	DMTF24A	Nocturia	MF55	Phase 2	[19]
SPD-556	DM9OPK3	Heart failure	BD10-BD13	Phase 2	[13]
SSR149415	DMCMD93	Anxiety disorder	6B00-6B0Z	Phase 2	[20]
VA-106483	DM1ODP6	Nocturia	MF55	Phase 2	[21]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OPC-51803	DMDCOSP	Urinary incontinence	MF50.2	Discontinued in Phase 1	[22]
OX 19	DM5UYI7	Urinary incontinence	MF50.2	Discontinued in Phase 1	[23]
VNA-932	DMKRG0I	Urinary incontinence	MF50.2	Discontinued in Phase 1	[24], [25]
JTV-605	DM89TXB	Dysmenorrhea	GA34.3	Terminated	[9]

34 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ARGENINE VASOPRESSIN	DM8KN0Q	Discovery agent	N.A.	Investigative	[26]
CL-385004	DMLQZGJ	Discovery agent	N.A.	Investigative	[9]
d(CH2)5[D-Ile2,Ile4]AVP	DMAX7LW	Discovery agent	N.A.	Investigative	[27]
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT	DM1BMT7	Discovery agent	N.A.	Investigative	[28]
d(CH2)5[Tyr(Me)2]AVP	DMHTSAX	Discovery agent	N.A.	Investigative	[27]
DVDAVP	DM53079	Discovery agent	N.A.	Investigative	[26]
D[Arg4,Dab8]VP	DMCU8HK	Discovery agent	N.A.	Investigative	[26]
D[Arg4,Lys8]VP	DM69OVM	Discovery agent	N.A.	Investigative	[26]
D[Arg4,Orn8]VP	DM8D4QT	Discovery agent	N.A.	Investigative	[26]
D[Arg4]AVP	DM76Q2B	Discovery agent	N.A.	Investigative	[26]
D[Cha4,Dab8]VP	DMCLUXI	Discovery agent	N.A.	Investigative	[26]
D[Cha4,Dap8]VP	DMAPZKB	Discovery agent	N.A.	Investigative	[26]
D[Cha4,Lys8]VP	DM0GO7U	Discovery agent	N.A.	Investigative	[26]
D[Cha4,Orn8]VP	DMZWTJK	Discovery agent	N.A.	Investigative	[26]
D[Cha4]AVP	DM8FCX5	Discovery agent	N.A.	Investigative	[26]
D[D-3-Pal2]AVP	DMD4V6U	Discovery agent	N.A.	Investigative	[26]
D[Leu4,Dab8]VP	DMNSXG9	Discovery agent	N.A.	Investigative	[26]
D[Leu4,Dap8]VP	DME3HK8	Discovery agent	N.A.	Investigative	[26]
D[Leu4,Lys8]VP	DMDBU7Q	Discovery agent	N.A.	Investigative	[26]
D[Leu4,Orn8]VP	DMJCW8Y	Discovery agent	N.A.	Investigative	[26]
D[Leu4]AVP	DMREZT7	Discovery agent	N.A.	Investigative	[26]
D[Orn4,Lys8]VP	DMNQTBU	Discovery agent	N.A.	Investigative	[26]
D[Orn4,Orn8]VP	DMONV0M	Discovery agent	N.A.	Investigative	[26]
D[Orn4]AVP	DMJNT95	Discovery agent	N.A.	Investigative	[26]
d[Pen1,Tyr(Me)2]AVP	DMT8KI6	Discovery agent	N.A.	Investigative	[27]
D[Val4]AVP	DM3GM8E	Discovery agent	N.A.	Investigative	[26]
FR161282	DMZSFEP	Discovery agent	N.A.	Investigative	[9]
L-372662	DMQV974	Discovery agent	N.A.	Investigative	[29]
VP-343	DMT03VB	Discovery agent	N.A.	Investigative	[9]
YM 218	DMPYM3J	Discovery agent	N.A.	Investigative	[30]
YM 471	DM5BFL4	Discovery agent	N.A.	Investigative	[31]
YM-35278	DMXRZ6N	Discovery agent	N.A.	Investigative	[32]
[Phe3]OT	DMK18CS	Discovery agent	N.A.	Investigative	[33]
[Val4]AVP	DMW82ZT	Discovery agent	N.A.	Investigative	[34]

References

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