General Information of DTT (ID: TT4TFGN)

DTT Name Vasopressin V1a receptor (V1AR) DTT Info
Gene Name AVPR1A

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Patented Agent(s)
Investigative Drug(s)
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]
Felypressin DMHLP9C Localisation N.A. Approved [3]
Mozavaptan DMZ905C Hyponatraemia 5C72 Approved [4]
Oxytocin DMDL27I Autism spectrum disorder 6A02 Approved [5]
Terlipressin DMT9FH3 Hypertension BA00-BA04 Approved [6]
ATOSIBAN DMB7WYM N. A. N. A. Phase 4 [7]
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⏷ Show the Full List of 7 Approved Drug(s)
10 Clinical Trial Drug(s) Transported by This DTP
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]
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⏷ Show the Full List of 10 Clinical Trial Drug(s)
10 Patented Agent(s) Transported by This DTP
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]
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⏷ Show the Full List of 10 Patented Agent(s)
4 Discontinued Drug(s) Transported by This DTP
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]
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1 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
NOX-F37 DM83DSA Acute and chronic heart failure BD1Z Preclinical [22]
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53 Investigative Drug(s) Transported by This DTP
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 [5]
[Val4]AVP DMW82ZT Discovery agent N.A. Investigative [37]
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⏷ Show the Full List of 53 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Acute hemodynamic effects of conivaptan, a dual V(1A) and V(2) vasopressin receptor antagonist, in patients with advanced heart failure. Circulation. 2001 Nov 13;104(20):2417-23.
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 Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. Prog Brain Res. 2008;170:473-512.
4 Nonpeptide vasopressin antagonists: a new group of hormone blockers entering the scene. Exp Clin Endocrinol Diabetes. 1999;107(3):157-65.
5 Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist. J Biol Chem. 1997 Oct 17;272(42):26536-44.
6 Investigational vasopressin receptor modulators in the pipeline. Expert Opin Investig Drugs. 2009 Aug;18(8):1119-31.
7 The discovery of GSK221149A: a potent and selective oxytocin antagonist. Bioorg Med Chem Lett. 2008 Jan 1;18(1):90-4.
8 Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder. J Med Chem. 2020 Feb 27;63(4):1511-1525.
9 The selective vasopressin type 1a receptor agonist selepressin (FE 202158) blocks vascular leak in ovine severe sepsis*. Crit Care Med. 2014 Jul;42(7):e525-33.
10 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
11 Social Communication is an Emerging Target for Pharmacotherapy in Autism Spectrum Disorder - A Review of the Literature on Potential Agents. J Can Acad Child Adolesc Psychiatry. 2014 February; 23(1):20-30.
12 Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist. J Pharm Sci. 2013 Jun;102(6):2033-43.
13 Safety and Tolerability of SRX246, a Vasopressin 1a Antagonist, in Irritable Huntington's Disease Patients-A Randomized Phase 2 Clinical Trial. J Clin Med. 2020 Nov 16;9(11):3682.
14 Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22.
15 Clinical pipeline report, company report or official report of Avarx.
16 Clinical pipeline report, company report or official report of Neumora Therapeutics
17 Orally active vasopressin V1a receptor antagonist, SRX251, selectively blocks aggressive behavior. Pharmacol Biochem Behav. 2006 Feb;83(2):169-74.
18 Vasopressin V1a and V1b receptor modulators: a patent review (2012 - 2014).Expert Opin Ther Pat. 2015 Jun;25(6):711-22.
19 A patent review of oxytocin receptor antagonists 2013-2017.Expert Opin Ther Pat. 2017 Dec;27(12):1287-1290.
20 Nonpeptide vasopressin receptor antagonists: development of selective and orally active V1a, V2 and V1b receptor ligands. Prog Brain Res. 2002;139:197-210.
21 Oral oxytocin antagonists. J Med Chem. 2010 Sep 23;53(18):6525-38.
22 Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.
23 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
24 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.
25 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.
26 Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding. Eur J Biochem. 2000 Jul;267(13):4253-63.
27 Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 1998 Dec;125(7):1463-70.
28 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.
29 Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists. J Med Chem. 2005 Dec 1;48(24):7882-905.
30 Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a ... J Pharmacol Exp Ther. 2003 Jul;306(1):253-61.
31 Binding of [3H] SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem Biophys Res Commun. 1994 Feb 28;199(1):353-60.
32 SSR126768A (4-chloro-3-[(3R)-(+)-5-chloro-1-(2,4-dimethoxybenzyl)-3-methyl-2-oxo-2,3-dihydro-1H-indol-3-yl]-N-ethyl-N-(3-pyridylmethyl)-benzamide, ... J Pharmacol Exp Ther. 2004 Apr;309(1):414-24.
33 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: 366).
34 Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res. 2005 Mar;51(3):275-81.
35 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.
36 Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J. 1995 May 15;14(10):2176-82.
37 [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology. 2002 Dec;143(12):4655-64.