Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT4TFGN)

• DTT Name: Vasopressin V1a receptor (V1AR)
• Synonyms: Vascular/hepatic-type arginine vasopressin receptor; V1aR; V1a vasopressin receptor; Antidiuretic hormone receptor 1a; AVPR1; AVPR V1a
• Gene Name: AVPR1A
• DTT Type: Successful target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: V1AR_HUMAN
• TTD ID: T79232
• Sequence:
  MRLSAGPDAGPSGNSSPWWPLATGAGNTSREAEALGEGNGPPRDVRNEELAKLEIAVLAV
  TFAVAVLGNSSVLLALHRTPRKTSRMHLFIRHLSLADLAVAFFQVLPQMCWDITYRFRGP
  DWLCRVVKHLQVFGMFASAYMLVVMTADRYIAVCHPLKTLQQPARRSRLMIAAAWVLSFV
  LSTPQYFVFSMIEVNNVTKARDCWATFIQPWGSRAYVTWMTGGIFVAPVVILGTCYGFIC
  YNIWCNVRGKTASRQSKGAEQAGVAFQKGFLLAPCVSSVKSISRAKIRTVKMTFVIVTAY
  IVCWAPFFIIQMWSVWDPMSVWTESENPTITITALLGSLNSCCNPWIYMFFSGHLLQDCV
  QSFPCCQNMKEKFNKEDTDSMSRRQTFYSNNRSPTNSTGMWKDSPKSSKSIKFIPVST
• Function: The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system. Has been involved in social behaviors, including affiliation and attachment. Receptor for arginine vasopressin.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  Neuroactive ligand-receptor interaction (hsa04080)
  Vascular smooth muscle contraction (hsa04270)
• Reactome Pathway:
  G alpha (q) signalling events (R-HSA-416476)
  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]
Desmopressin	DMS3GVE	Diabetic complication	5A2Y	Approved	[3]
Felypressin	DMHLP9C	Localisation	N.A.	Approved	[4]
Mozavaptan	DMZ905C	Hyponatraemia	5C72	Approved	[5]
Oxytocin	DMDL27I	Autism spectrum disorder	6A02	Approved	[6]
Terlipressin	DMT9FH3	Hypertension	BA00-BA04	Approved	[1]
ATOSIBAN	DMB7WYM	N. A.	N. A.	Phase 4	[7]

10 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Balovaptan	DMKMTDG	Autism spectrum disorder	6A02	Phase 3	[8]
FE-202158	DM3CVHQ	Sepsis	1G40-1G41	Phase 2	[9]
PMX-53	DMZUAJ4	Atopic dermatitis	EA80	Phase 2	[10]
RG7314	DMB4M6O	Autism spectrum disorder	6A02	Phase 2	[11]
SRX-246	DMMU41F	Anxiety disorder	6B00-6B0Z	Phase 2	[12]
SRX246	DMKOTUJ	Huntington disease	8A01.10	Phase 2	[13]
SSR149415	DMCMD93	Anxiety disorder	6B00-6B0Z	Phase 2	[14]
VA-111913	DMAYWXD	Dysmenorrhea	GA34.3	Phase 2	[15]
NMRA-511	DM3V9OJ	Anxiety disorder	6B00-6B0Z	Phase 1	[16]
SRX-251	DMO1N8A	Dysmenorrhea	GA34.3	Phase 1	[17]

10 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID25776143-Compound-1	DMGHSR9	N. A.	N. A.	Patented	[18]
PMID25776143-Compound-2	DMTZRFP	N. A.	N. A.	Patented	[18]
PMID25776143-Compound-3	DMCULI1	N. A.	N. A.	Patented	[18]
PMID25776143-Compound-4	DMMVETJ	N. A.	N. A.	Patented	[18]
PMID25776143-Compound-7	DM7QIMN	N. A.	N. A.	Patented	[18]
PMID25776143-Compound-8	DMUKFJ0	N. A.	N. A.	Patented	[18]
PMID28906174-Compound-figure1g	DMECU90	N. A.	N. A.	Patented	[19]
Pyrrolidine derivative 13	DM3VA8P	N. A.	N. A.	Patented	[19]
Tetra-azabenzo[e]azulene derivative 1	DMLRY53	N. A.	N. A.	Patented	[18]
Tetra-azabenzo[e]azulene derivative 2	DMUEI4N	N. A.	N. A.	Patented	[18]

4 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OPC-21268	DM7OVMH	Cardiac disease	BA00-BE2Z	Discontinued in Phase 2	[20]
PF-3274167	DMD42MN	Female sexual arousal dysfunction	HA01.1	Discontinued in Phase 1	[21]
JTV-605	DM89TXB	Dysmenorrhea	GA34.3	Terminated	[20]
L-371257	DMCRQTH	N. A.	N. A.	Terminated	[21]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
NOX-F37	DM83DSA	Acute and chronic heart failure	BD1Z	Preclinical	[22]

53 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1'-tosylspiro[indene-1,4'-piperidine]	DM9SYEP	Discovery agent	N.A.	Investigative	[21]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[23]
ARGENINE VASOPRESSIN	DM8KN0Q	Discovery agent	N.A.	Investigative	[24]
CL-385004	DMLQZGJ	Discovery agent	N.A.	Investigative	[20]
D(CH2)5[Tyr(Me)2,Thr4,Orn8(5/6C-Flu),Tyr-NH29]VT	DMVHMGA	Discovery agent	N.A.	Investigative	[25]
D(CH2)5[Tyr(Me)2,Thr4,Orn8,Tyr9-NH2]VT	DM1BMT7	Discovery agent	N.A.	Investigative	[25]
d(CH2)5[Tyr(Me)2]AVP	DMHTSAX	Discovery agent	N.A.	Investigative	[26]
DesGly-NH2,d(CH2)5[D-Tyr2,Thr4,Orn8(5/6C-Flu)]VT	DMJK0H5	Discovery agent	N.A.	Investigative	[25]
DVDAVP	DM53079	Discovery agent	N.A.	Investigative	[24]
D[Arg4,Dab8]VP	DMCU8HK	Discovery agent	N.A.	Investigative	[24]
D[Arg4,Lys8]VP	DM69OVM	Discovery agent	N.A.	Investigative	[24]
D[Arg4,Orn8]VP	DM8D4QT	Discovery agent	N.A.	Investigative	[24]
D[Arg4]AVP	DM76Q2B	Discovery agent	N.A.	Investigative	[24]
D[Cha4,Dab8]VP	DMCLUXI	Discovery agent	N.A.	Investigative	[24]
D[Cha4,Dap8]VP	DMAPZKB	Discovery agent	N.A.	Investigative	[24]
D[Cha4,Lys8]VP	DM0GO7U	Discovery agent	N.A.	Investigative	[24]
D[Cha4,Orn8]VP	DMZWTJK	Discovery agent	N.A.	Investigative	[24]
D[Cha4]AVP	DM8FCX5	Discovery agent	N.A.	Investigative	[24]
D[D-3-Pal2]AVP	DMD4V6U	Discovery agent	N.A.	Investigative	[24]
D[Leu4,Dab8]VP	DMNSXG9	Discovery agent	N.A.	Investigative	[24]
D[Leu4,Dap8]VP	DME3HK8	Discovery agent	N.A.	Investigative	[24]
D[Leu4,Lys8]VP	DMDBU7Q	Discovery agent	N.A.	Investigative	[24]
D[Leu4,Orn8]VP	DMJCW8Y	Discovery agent	N.A.	Investigative	[24]
D[Leu4]AVP	DMREZT7	Discovery agent	N.A.	Investigative	[24]
D[Lys8(5/6-Flu)]VT	DME2PKB	Discovery agent	N.A.	Investigative	[25]
D[Orn4,Lys8]VP	DMNQTBU	Discovery agent	N.A.	Investigative	[24]
D[Orn4,Orn8]VP	DMONV0M	Discovery agent	N.A.	Investigative	[24]
D[Orn4]AVP	DMJNT95	Discovery agent	N.A.	Investigative	[24]
D[Orn8(5/6C-Flu)]VT	DMH791N	Discovery agent	N.A.	Investigative	[25]
d[Pen1,Tyr(Me)2]AVP	DMT8KI6	Discovery agent	N.A.	Investigative	[27]
D[Thr4,Lys8(5/6C-Flu)]VT	DMS4F8O	Discovery agent	N.A.	Investigative	[25]
D[Thr4,Orn8(5/6C-Flu)]VT	DMBDZQA	Discovery agent	N.A.	Investigative	[25]
D[Val4]AVP	DM3GM8E	Discovery agent	N.A.	Investigative	[24]
HO-LVA	DMJQI7A	Discovery agent	N.A.	Investigative	[28]
Hoo-Phe-Orn-Pro-hle-Pff-Phe-NH2	DMHW2DU	Discovery agent	N.A.	Investigative	[10]
L-372662	DMQV974	Discovery agent	N.A.	Investigative	[21]
L023103	DM9KWUR	Discovery agent	N.A.	Investigative	[29]
LS-192629	DMUBF53	Discovery agent	N.A.	Investigative	[30]
Relcovaptan	DM3AWPB	Discovery agent	N.A.	Investigative	[31]
SSR126768A	DMF0X2S	Discovery agent	N.A.	Investigative	[32]
V1A F/U	DMH971B	Infertility	GB04	Investigative	[33]
YM 218	DMPYM3J	Discovery agent	N.A.	Investigative	[34]
YM 471	DM5BFL4	Discovery agent	N.A.	Investigative	[35]
[HO1][Lys8(5/6C-Flu)]VT	DMLZNK6	Discovery agent	N.A.	Investigative	[25]
[HO1][Orn8(5/6C-Flu)]VT	DMFK9V5	Discovery agent	N.A.	Investigative	[25]
[HO1][Orn8(5/6C-Rhm)]VT	DM7COAM	Discovery agent	N.A.	Investigative	[25]
[HO1][Thr4,Lys8(5/6C-Flu)]VT	DMT2UYR	Discovery agent	N.A.	Investigative	[25]
[HO1][Thr4,Orn8(5/6C-Flu)]VT	DM81B4W	Discovery agent	N.A.	Investigative	[25]
[Lys8(Alexa 488) ]PVA	DM7STF6	Discovery agent	N.A.	Investigative	[28]
[Lys8(Alexa 546) ]PVA	DM38L6U	Discovery agent	N.A.	Investigative	[28]
[Phe3]OT	DMK18CS	Discovery agent	N.A.	Investigative	[36]
[Thr4,Gly7]OT	DM7QAKB	Discovery agent	N.A.	Investigative	[6]
[Val4]AVP	DMW82ZT	Discovery agent	N.A.	Investigative	[37]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Sepsis with septic shock	1G41	Whole blood	8.89E-04	-0.12	-0.34

References

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