Page last updated: 2024-11-07

opc 21268

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Description

OPC 21268: structure given in first source; vasopressin V1 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID114904
CHEMBL ID296908
SCHEMBL ID3504368
MeSH IDM0187639

Synonyms (36)

Synonym
n-(3-{4-[4-(2-oxo-3,4-dihydro-2h-quinolin-1-yl)-piperidine-1-carbonyl]-phenoxy}-propyl)-acetamide
bdbm50029644
n-(3-(4-(4-(2-oxo-3,4-dihydroquinolin-1(2h)-yl)piperidine-1-carbonyl)phenoxy)propyl)acetamide
gtpl2196
opc-21268
1-(1-(4-(3-acetylaminopropoxy)benzoyl)-4-piperidyl)-3,4-dihydro-2(1h)-quinolinone
opc 21268
acetamide, n-(3-(4-((4-(3,4-dihydro-2-oxo-1(2h)-quinolinyl)-1-piperidinyl)carbonyl)phenoxy)propyl)-
opc-1268
CHEMBL296908 ,
L001417
n-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide
131631-89-5
opc-21268 hydrate
SCHEMBL3504368
n-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2h)quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide
AKOS024457877
EX-A593
J-006031
n-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2h)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]acetamide
NCGC00370961-01
n-(3-{4-[4-(2-oxo-3,4-dihydroquinolin-1(2h)-yl)piperidine-1-carbonyl]phenoxy}propyl)ethanimidic acid
DTXSID70927295
fuscoside
FT-0700164
Q27088205
1262770-69-3
BCP14853
opc-21268;opc21268
CS-0003694
HY-15009
acetamide, n-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2h)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-
MS-28145
1-[1-[4-(3-acetylaminopropoxy)benzoyl]-4-piperidyl]-3,4-dihydroquinolin-2(1h)-one
A856968
AC-35504

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" These compounds are structurally related to the 1-(4-piperidyl)-2(1H)-quinolinones, including OPC-21268, an orally bioavailable AVP V1 antagonist with high V1 specificity."( Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
Chihara, T; Kondo, K; Miyamoto, H; Mori, T; Nakaya, K; Ogawa, H; Tominaga, M; Yabuuchi, Y; Yamamura, Y; Yamashita, H, 1993
)
0.29
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" The dose-response curve for AVP was shifted to the right in parallel by OPC-31260 but not by OPC-21268."( Potent antagonistic action of OPC-31260, a vasopressin V2 receptor antagonist, on [Arg8]vasopressin-induced vasoconstriction in isolated simian femoral arteries.
Chiba, S; Tsukada, M, 1992
)
0.28
" produced a rightward parallel shift of the dose-response curves for AVP in a dose-dependent manner."( OPC-21268 antagonizes arginine vasopressin-induced vasoconstrictor response in the spinally-anesthetized dog.
Chihara, T; Mori, T; Nakamura, S; Onogawa, T; Tominaga, M; Yabuuchi, Y; Yamamura, Y; Yamashita, T, 1995
)
0.29
" Brain tissue sodium content was significantly reduced at the dosage of 300 mg/kg (P<0."( Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats.
Bemana, I; Nagao, S, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.68400.01237.983543.2770AID1645841
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Vasopressin V2 receptorHomo sapiens (human)Ki45.50000.00040.43453.9811AID217391; AID513686
Oxytocin receptorHomo sapiens (human)Ki0.17000.00010.07180.9780AID151801
Vasopressin V1a receptorRattus norvegicus (Norway rat)IC50 (µMol)0.44000.08201.04775.0000AID217060
Vasopressin V1a receptorRattus norvegicus (Norway rat)Ki0.02990.00080.03000.1100AID217234; AID217235; AID217238; AID513685
Vasopressin V2 receptorSus scrofa (pig)Ki10.00000.28500.28500.2850AID217688
Vasopressin V1a receptorHomo sapiens (human)Ki25.67000.00020.62357.0300AID217085; AID217088; AID217091; AID337610; AID513684
Oxytocin receptorRattus norvegicus (Norway rat)Ki0.23000.00090.04890.2300AID151933
Vasopressin V2 receptor Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00050.06380.5700AID213927
Vasopressin V2 receptor Rattus norvegicus (Norway rat)Ki16.66670.00030.97919.7000AID217688; AID513687
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (63)

Processvia Protein(s)Taxonomy
positive regulation of systemic arterial blood pressureVasopressin V2 receptorHomo sapiens (human)
renal water retentionVasopressin V2 receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVasopressin V2 receptorHomo sapiens (human)
activation of adenylate cyclase activityVasopressin V2 receptorHomo sapiens (human)
hemostasisVasopressin V2 receptorHomo sapiens (human)
positive regulation of cell population proliferationVasopressin V2 receptorHomo sapiens (human)
negative regulation of cell population proliferationVasopressin V2 receptorHomo sapiens (human)
positive regulation of gene expressionVasopressin V2 receptorHomo sapiens (human)
telencephalon developmentVasopressin V2 receptorHomo sapiens (human)
response to cytokineVasopressin V2 receptorHomo sapiens (human)
positive regulation of intracellular signal transductionVasopressin V2 receptorHomo sapiens (human)
cellular response to hormone stimulusVasopressin V2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionVasopressin V2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayVasopressin V2 receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinVasopressin V2 receptorHomo sapiens (human)
suckling behaviorOxytocin receptorHomo sapiens (human)
response to amphetamineOxytocin receptorHomo sapiens (human)
muscle contractionOxytocin receptorHomo sapiens (human)
cell surface receptor signaling pathwayOxytocin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationOxytocin receptorHomo sapiens (human)
heart developmentOxytocin receptorHomo sapiens (human)
lactationOxytocin receptorHomo sapiens (human)
memoryOxytocin receptorHomo sapiens (human)
response to xenobiotic stimulusOxytocin receptorHomo sapiens (human)
positive regulation of norepinephrine secretionOxytocin receptorHomo sapiens (human)
telencephalon developmentOxytocin receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicOxytocin receptorHomo sapiens (human)
response to estradiolOxytocin receptorHomo sapiens (human)
response to progesteroneOxytocin receptorHomo sapiens (human)
response to anoxiaOxytocin receptorHomo sapiens (human)
response to cytokineOxytocin receptorHomo sapiens (human)
social behaviorOxytocin receptorHomo sapiens (human)
response to cocaineOxytocin receptorHomo sapiens (human)
maternal behaviorOxytocin receptorHomo sapiens (human)
sperm ejaculationOxytocin receptorHomo sapiens (human)
eating behaviorOxytocin receptorHomo sapiens (human)
response to peptide hormoneOxytocin receptorHomo sapiens (human)
estrous cycleOxytocin receptorHomo sapiens (human)
positive regulation of blood pressureOxytocin receptorHomo sapiens (human)
digestive tract developmentOxytocin receptorHomo sapiens (human)
positive regulation of synapse assemblyOxytocin receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicOxytocin receptorHomo sapiens (human)
positive regulation of penile erectionOxytocin receptorHomo sapiens (human)
ERK1 and ERK2 cascadeOxytocin receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionOxytocin receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisOxytocin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayOxytocin receptorHomo sapiens (human)
female pregnancyOxytocin receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinOxytocin receptorHomo sapiens (human)
positive regulation of vasoconstrictionOxytocin receptorHomo sapiens (human)
maternal process involved in parturitionOxytocin receptorHomo sapiens (human)
cellular response to hormone stimulusOxytocin receptorHomo sapiens (human)
maternal aggressive behaviorVasopressin V1a receptorHomo sapiens (human)
positive regulation of systemic arterial blood pressureVasopressin V1a receptorHomo sapiens (human)
generation of precursor metabolites and energyVasopressin V1a receptorHomo sapiens (human)
activation of phospholipase C activityVasopressin V1a receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVasopressin V1a receptorHomo sapiens (human)
negative regulation of female receptivityVasopressin V1a receptorHomo sapiens (human)
grooming behaviorVasopressin V1a receptorHomo sapiens (human)
blood circulationVasopressin V1a receptorHomo sapiens (human)
positive regulation of cell population proliferationVasopressin V1a receptorHomo sapiens (human)
positive regulation of heart rateVasopressin V1a receptorHomo sapiens (human)
positive regulation of glutamate secretionVasopressin V1a receptorHomo sapiens (human)
myotube differentiationVasopressin V1a receptorHomo sapiens (human)
calcium-mediated signalingVasopressin V1a receptorHomo sapiens (human)
telencephalon developmentVasopressin V1a receptorHomo sapiens (human)
positive regulation of cell growthVasopressin V1a receptorHomo sapiens (human)
positive regulation of prostaglandin biosynthetic processVasopressin V1a receptorHomo sapiens (human)
positive regulation of cellular pH reductionVasopressin V1a receptorHomo sapiens (human)
social behaviorVasopressin V1a receptorHomo sapiens (human)
cellular response to water deprivationVasopressin V1a receptorHomo sapiens (human)
maternal behaviorVasopressin V1a receptorHomo sapiens (human)
sperm ejaculationVasopressin V1a receptorHomo sapiens (human)
response to corticosteroneVasopressin V1a receptorHomo sapiens (human)
negative regulation of transmission of nerve impulseVasopressin V1a receptorHomo sapiens (human)
transport across blood-brain barrierVasopressin V1a receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayVasopressin V1a receptorHomo sapiens (human)
positive regulation of vasoconstrictionVasopressin V1a receptorHomo sapiens (human)
cellular response to hormone stimulusVasopressin V1a receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by vasopressinVasopressin V1a receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
vasopressin receptor activityVasopressin V2 receptorHomo sapiens (human)
protein bindingVasopressin V2 receptorHomo sapiens (human)
peptide bindingVasopressin V2 receptorHomo sapiens (human)
peptide hormone bindingOxytocin receptorHomo sapiens (human)
peptide bindingOxytocin receptorHomo sapiens (human)
vasopressin receptor activityOxytocin receptorHomo sapiens (human)
oxytocin receptor activityOxytocin receptorHomo sapiens (human)
vasopressin receptor activityVasopressin V1a receptorHomo sapiens (human)
protein kinase C bindingVasopressin V1a receptorHomo sapiens (human)
protein bindingVasopressin V1a receptorHomo sapiens (human)
peptide hormone bindingVasopressin V1a receptorHomo sapiens (human)
V1A vasopressin receptor bindingVasopressin V1a receptorHomo sapiens (human)
peptide bindingVasopressin V1a receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
endosomeVasopressin V2 receptorHomo sapiens (human)
endoplasmic reticulumVasopressin V2 receptorHomo sapiens (human)
Golgi apparatusVasopressin V2 receptorHomo sapiens (human)
plasma membraneVasopressin V2 receptorHomo sapiens (human)
membraneVasopressin V2 receptorHomo sapiens (human)
endocytic vesicleVasopressin V2 receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneVasopressin V2 receptorHomo sapiens (human)
perinuclear region of cytoplasmVasopressin V2 receptorHomo sapiens (human)
plasma membraneVasopressin V2 receptorHomo sapiens (human)
plasma membraneOxytocin receptorHomo sapiens (human)
microvillusOxytocin receptorHomo sapiens (human)
adherens junctionOxytocin receptorHomo sapiens (human)
apical plasma membraneOxytocin receptorHomo sapiens (human)
plasma membraneOxytocin receptorHomo sapiens (human)
endosomeVasopressin V1a receptorHomo sapiens (human)
plasma membraneVasopressin V1a receptorHomo sapiens (human)
endocytic vesicleVasopressin V1a receptorHomo sapiens (human)
plasma membraneVasopressin V1a receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID217239Evaluated for the binding affinity towards Vasopressin V1a receptor in rat liver membrane using [3H]AVP as radioligand2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
AID513685Displacement of [3H]vasopressin from vasopressin V1a receptor in rat liver tissue2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Oral oxytocin antagonists.
AID182931In vivo dose required to inhibit AVP-induced pressor response in pithed rats by 50%2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
AID217688Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
AID217060Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
AID217694Selectivity ratio Vasopressin V2 receptor/Vasopressin V1 receptor of the compound2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
AID217091Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in human platelets.1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
AID513687Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Oral oxytocin antagonists.
AID217693Selectivity ratio (Ki) of affinity at rat Vasopressin V2 receptor to that of rat Vasopressin V1a receptor2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
AID217085Binding affinity at cloned human Vasopressin V1a receptor stably expressed in CHO cells, using [3H]AVP as radioligand2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
AID217519Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors.1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
AID513686Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Oral oxytocin antagonists.
AID217235Binding affinity towards Vasopressin V1a receptor in rat liver2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.
AID513683Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Oral oxytocin antagonists.
AID513684Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Oral oxytocin antagonists.
AID213767Inhibition expressed as percent change in diastolic blood pressure increased by AVP (30 milliunits / kg, iv) before and after oral administration at 22 uM/kg1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
AID217691Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
AID337610Binding affinity to vasopressin V1a receptor1994Journal of natural products, Oct, Volume: 57, Issue:10
Khusimol, a non-peptide ligand for vasopressin V1a receptors.
AID513682Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Oral oxytocin antagonists.
AID213927Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
AID217088Binding affinity towards Vasopressin V1a receptor in human liver2000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.
AID217692Evaluated for the binding affinity towards Vasopressin V2 receptor in rat kidney membrane using [3H]-AVP as radioligand2002Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
AID213762Inhibition dose for AVP (30 milliunits/kg, iv) induced vasoconstriction when orally administarted1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
AID217234Binding affinity at Vasopressin V1a receptor, performed using [3H]AVP on rat liver2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
AID151801Binding affinity was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from human. 1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
AID217238Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in rat liver.1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
AID151933Binding affinity was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from rats1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
AID217391Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346469Human OT receptor (Vasopressin and oxytocin receptors)1995Life sciences, , Volume: 57, Issue:24
Characterization of the human oxytocin receptor stably expressed in 293 human embryonic kidney cells.
AID1346453Human V2 receptor (Vasopressin and oxytocin receptors)1997Endocrinology, Oct, Volume: 138, Issue:10
The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
AID1346432Human V1A receptor (Vasopressin and oxytocin receptors)1997Endocrinology, Oct, Volume: 138, Issue:10
The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (129)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's90 (69.77)18.2507
2000's31 (24.03)29.6817
2010's6 (4.65)24.3611
2020's2 (1.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.39

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index14.39 (24.57)
Research Supply Index4.92 (2.92)
Research Growth Index4.12 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (2.26%)5.53%
Reviews6 (4.51%)6.00%
Case Studies3 (2.26%)4.05%
Observational0 (0.00%)0.25%
Other121 (90.98%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]