Page last updated: 2024-12-07

l 648051

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

L 648051: antagonist of leukotriene D4 receptor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID122010
CHEMBL ID282253
SCHEMBL ID157166
MeSH IDM0147854

Synonyms (20)

Synonym
l-648051
4-((3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl)-gamma-oxobenzenebutanoic acid
l 648051
benzenebutanoic acid, 4-((3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl)-gamma-oxo-
4-apsob
CHEMBL282253
91541-18-3
4-(4-{[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl]sulfonyl}phenyl)-4-oxobutanoic acid
4-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propylsulfonyl]phenyl]-4-oxobutanoic acid
0lgz40mb45 ,
4-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)propylsulfonyl)-gamma-oxo-benzenebutanoic acid
unii-0lgz40mb45
SCHEMBL157166
DTXSID50238619
AKOS030530731
benzenebutanoic acid, 4-((3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl)-.gamma.-oxo-
4-((3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl)-.gamma.-oxobenzenebutanoic acid
4-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)propylsulfonyl)-gamma-oxobenzenebutanoic acid
ZAKKEARLDPTRLX-UHFFFAOYSA-N
4-(4-((3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl)phenyl)-4-oxobutanoic acid

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"41) and a short plasma half-life (2."( Tolerability and pharmacokinetics of L-648,051. A leukotriene D4-receptor antagonist, in healthy volunteers.
Biollaz, J; Distlerath, L; Hsieh, JY; Jaeger, A; Leuenberger, P; Schelling, JL; Stahl, E, 1988
)
0.27

Bioavailability

ExcerptReferenceRelevance
" Although the compound was well absorbed, it exhibited poor bioavailability due to efficient first-pass metabolism."( Disposition and metabolism of sodium 4-[(3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl]-gamma -oxobenzenebutanoate in rats and dogs.
deLuna, FA; Duncan, AE; Hsieh, JY; Pitzenberger, SM; Ramjit, HG; Tocco, DJ,
)
0.13

Dosage Studied

ExcerptRelevanceReference
" In the order of potency L-648,051 greater than FPL-55712 greater than L-649,923, these agents antagonized contractions to LTD4 and produced parallel rightward shifts in the dose-response curves."( Leukotriene and anti-IgE induced contractions of human isolated trachea: studies with leukotriene receptor antagonists and a novel 5-lipoxygenase inhibitor.
Charette, L; Denis, D; Jones, TR, 1988
)
0.27
" After a dosage of 10 mg/kg iv, L-648,051 declined rapidly with a half-life of approximately 2 min in rat and dog plasma."( Disposition and metabolism of sodium 4-[(3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl)sulfonyl]-gamma -oxobenzenebutanoate in rats and dogs.
deLuna, FA; Duncan, AE; Hsieh, JY; Pitzenberger, SM; Ramjit, HG; Tocco, DJ,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cysteinyl leukotriene receptor 2Homo sapiens (human)Ki6.20000.00020.94296.2000AID55237
Cysteinyl leukotriene receptor 1Homo sapiens (human)Ki6.20000.00021.56248.8720AID55237
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
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 (4)

Processvia Protein(s)Taxonomy
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 (3)

Processvia Protein(s)Taxonomy
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 (9)

Assay IDTitleYearJournalArticle
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.
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.
AID55053Inhibitory activity to block binding of [3H]leukotriene D4 to Cysteinyl leukotriene D4 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.
AID79493Compound was tested for LTD4 guinea pig trachea contraction1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID76084Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after aerosol administration as 1% solution1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID79332Antagonistic activity against LTD4 induced contraction in guinea pig trachea1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID55237Binding affinity against Cysteinyl leukotriene D4 receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID88895Partially blocking activity against LTD4 induced bronchoconstriction following 12 mg aerosol dose1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID76429Inhibition of leukotriene D4 induced bronchoconstriction in anesthetized guinea pigs after aerosol administration as 1% solution1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-199013 (61.90)18.7374
1990's8 (38.10)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: 10.94

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 Index10.94 (24.57)
Research Supply Index3.43 (2.92)
Research Growth Index4.38 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.94)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (25.00%)5.53%
Reviews3 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (62.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]