Page last updated: 2024-11-06

wy 48252

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Description

Wy 48252: leukotriene D4 antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60539
CHEMBL ID17344
SCHEMBL ID38043
MeSH IDM0158179

Synonyms (27)

Synonym
ritolukast
wy-48252
111974-60-8
ritolukast (usan/inn)
D02849
wy 48252
AKOS000278710
1,1,1-trifluoro-n-[3-(quinolin-2-ylmethoxy)phenyl]methanesulfonamide
CHEMBL17344 ,
c,c,c-trifluoro-n-[3-(quinolin-2-ylmethoxy)-phenyl]-methanesulfonamide
c,c,c-trifluoro-n-[3-(quinolin-2-ylmethoxy)-phenyl]-methanesulfonamide(wy-48,252)
c,c,c-trifluoro-n-[3-(quinolin-2-ylmethoxy)-phenyl]-methanesulfonamide( wy-48,252)
c,c,c-trifluoro-n-[3-(quinolin-2-ylmethoxy)-phenyl]-methanesulfonamide(wy 48252)
bdbm50006806
0e8r4gde2q ,
methanesulfonamide, 1,1,1-trifluoro-n-(3-(2-quinolinylmethoxy)phenyl)-
unii-0e8r4gde2q
1,1,1-trifluoro-alpha-2-quinolylmethanesulfon-m-anisidide
ritolukast [usan:inn]
ritolukastum
ritolukastum [inn-latin]
ritolukast [usan]
ritolukast [inn]
SCHEMBL38043
n-[3-[(2-quinolinyl)methoxy]phenyl]trifluoromethane sulfonamide
DTXSID90149795
Q27236668
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)3.30000.00462.018210.0000AID103805; AID7070
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)6.20000.00291.786810.0000AID160874; AID161013
Platelet-activating factor acetylhydrolaseHomo sapiens (human)IC50 (µMol)2.00000.00000.38373.9000AID103805
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Ki0.03500.00010.23581.5000AID55065
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)6.20000.00291.823210.0000AID160874; AID161013
Cysteinyl leukotriene receptor 2Homo sapiens (human)Ki0.03500.00020.94296.2000AID55237
Cysteinyl leukotriene receptor 1Homo sapiens (human)Ki0.03500.00021.56248.8720AID55237
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
peptide hormone processingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particle remodelingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
lipid oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
plasma lipoprotein particle oxidationPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phosphatidylcholine catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor metabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of inflammatory responsePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
platelet activating factor catabolic processPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
positive regulation of monocyte chemotaxisPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
immune responseCysteinyl leukotriene receptor 2Homo sapiens (human)
leukotriene signaling pathwayCysteinyl leukotriene receptor 2Homo sapiens (human)
neuropeptide signaling pathwayCysteinyl leukotriene receptor 2Homo sapiens (human)
inflammatory response to antigenic stimulusCysteinyl leukotriene receptor 1Homo sapiens (human)
calcium ion transportCysteinyl leukotriene receptor 1Homo sapiens (human)
chemotaxisCysteinyl leukotriene receptor 1Homo sapiens (human)
defense responseCysteinyl leukotriene receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationCysteinyl leukotriene receptor 1Homo sapiens (human)
respiratory gaseous exchange by respiratory systemCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of angiogenesisCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of vasoconstrictionCysteinyl leukotriene receptor 1Homo sapiens (human)
establishment of localization in cellCysteinyl leukotriene receptor 1Homo sapiens (human)
positive regulation of glial cell proliferationCysteinyl leukotriene receptor 1Homo sapiens (human)
leukotriene signaling pathwayCysteinyl leukotriene receptor 1Homo sapiens (human)
cellular response to hypoxiaCysteinyl leukotriene receptor 1Homo sapiens (human)
neuropeptide signaling pathwayCysteinyl leukotriene receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
1-alkyl-2-acetylglycerophosphocholine esterase activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
phospholipid bindingPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
hydrolase activity, acting on ester bondsPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
calcium-independent phospholipase A2 activityPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
leukotriene receptor activityCysteinyl leukotriene receptor 2Homo sapiens (human)
protein bindingCysteinyl leukotriene receptor 2Homo sapiens (human)
cysteinyl leukotriene receptor activityCysteinyl leukotriene receptor 2Homo sapiens (human)
G protein-coupled peptide receptor activityCysteinyl leukotriene receptor 2Homo sapiens (human)
leukotriene receptor activityCysteinyl leukotriene receptor 1Homo sapiens (human)
cysteinyl leukotriene receptor activityCysteinyl leukotriene receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityCysteinyl leukotriene receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
extracellular regionPlatelet-activating factor acetylhydrolaseHomo sapiens (human)
low-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
high-density lipoprotein particlePlatelet-activating factor acetylhydrolaseHomo sapiens (human)
cellular_componentCysteinyl leukotriene receptor 2Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 2Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 2Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 1Homo sapiens (human)
membraneCysteinyl leukotriene receptor 1Homo sapiens (human)
plasma membraneCysteinyl leukotriene receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
AID77371Relative inhibitor potency of the intraduodenally administered compound with Wy-48,252 against ovalbumin induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID160874Concentration for 50% inhibition of A-23187-stimulated radiolabeled 5-HETE and TXB2 synthesis by Prostaglandin G/H synthase1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID140620The compound was tested for inhibitory activity which inhibits prostaglandin E2[PGE2] synthesis by zymosan-activated mouse peritoneal macrophages1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID76998Inhibitory dose of the intragastrically administered compound (120 min before giving agonist) that produced a 50% inhibition of leukotriene D4 induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID161013Inhibitory concentration to inhibit Prostaglandin G/H synthase in the rat1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID76995Inhibitory dose of the intraduodenally administered compound (10 min before giving agonist) that produced a 50% inhibition of leukotriene D4 induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID77372Relative inhibitor potency of the intragastrically administered compound with Wy-48,252 against leukotriene D4 induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID180659The compound was tested for inhibitory activity against synthesis of immunoreactive thromboxane B2 in rat PMNs1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID76976Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after intravenous administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID103805Concentration for 50% inhibition of A-23187-stimulated radiolabeled 5-HETE and TXB2 synthesis by PMN 5-lipoxygenase1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID79847Compound was tested for LTD4 guinea pig trachea contraction.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID180658The compound was tested for inhibitory activity against synthesis of immunoreactive LTB41992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID76444Inhibition of ovalbumin-induced bronchoconstriction when compound was administered intraduodenally at a dose of 10 mg/kg in guinea pig1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID102661Binding studies using tritium-labelled leukotriene D41989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID76430Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after aerosol administration as 1% solution; NT means not tested1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID77369Relative inhibitor potency of the intraduodenally administered compound with Wy-48,252 against leukotrien D4 induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID76447Inhibition of ovalbumin-induced bronchoconstriction when compound was administered perorally at a dose of 25 mg/kg in guinea pig1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID55065Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig lung was determined using [3H]LTD41990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
AID23090Dissociation constant was determined In vitro in isolated guinea pig trachea after intraduodenal administration1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID79839Antagonistic activity against LTD4 induced contraction in guinea pig trachea1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID77097In vitro inhibition of LTD4-induced bronchoconstriction after intragastrical administration 120 min before agonist into isolated guinea pig trachea1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID55054Inhibitory activity to block binding of [3H]leukotriene D4 to LTD4 receptor sites in homogenized guinea pig lung at 10 uM1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID134182Compound was administered intragastrically and tested in a mouse ear edema assay; Inactive1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID54903Inhibitory activity to block binding of [3H]leukotriene D4 to LTD4 receptor sites in homogenized guinea pig lung1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID14020Oral bioavailability was determined; range 49-102%1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID25086Dissociation constant was determined1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID76996Inhibitory dose of the intraduodenally administered compound (10 min before giving agonist) that produced a 50% inhibition of ovalbumin induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID77091Examined in vitro for LTD4-induced bronchoconstriction in isolated guinea pig trachea by injecting intraduodenally1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID55072Compound was evaluated for its ability to displace [3H]LTD4 from LTD4 receptor in guinea pig lung membranes1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID19125Plasma half-life was determined; 0.5-17.7h1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID77101In vitro inhibition of ovalbumin-induced bronchoconstriction after intragastrical administration 120 min before agonist into isolated guinea pig trachea1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID76433Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after intravenous administration at a dose of 10 mg/kg1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID7070Inhibitory concentration to inhibit 5-lipoxygenase in the rat1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID76254Inhibition of Leukotriene D4 induced bronchoconstriction when compound was administered perorally at a dose of 25 mg/kg in guinea pig1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID77096In vitro for inhibition of ovalbumin-induced bronchoconstriction in isolated guinea pig trachea by injecting intraduodenally1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.
AID193108The compound was tested for inhibition in rat carrageenan paw edema assay1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID77122The inhibitory dose for antigen induced bronchoconstriction in guinea pig after peroral administration1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID76999Inhibitory dose of the intragastrically administered compound (120 min before giving agonist) that produced a 50% inhibition of ovalbumin induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID77373Relative inhibitor potency of the intragastrically administered compound with Wy-48,252 against ovalbumin induced bronchoconstriction in guinea pigs1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID80628The compound was tested for blocking of LTD4-induced contractions of guinea pig trachea1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID55237Binding affinity against Cysteinyl leukotriene D4 receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID132860The compound was tested for inhibitory activity which inhibits LTC4 synthesis by zymosan-activated mouse peritoneal macrophages1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
5-lipoxygenase: properties, pharmacology, and the quinolinyl(bridged)aryl class of inhibitors.
AID183975Compound at 100 mg/kg was administered intragastrically and tested in a rat carrageenan paw edema assay1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID75651Activity against leukotriene D4-induced contraction of guinea pig trachea, in the presence of glutathione1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
AID76252Inhibition of Leukotriene D4 induced bronchoconstriction when compound was administered intraduodenally at a dose of 25 mg/kg in guinea pig1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (46.67)18.7374
1990's8 (53.33)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.70

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 Index11.70 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.48 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]