Page last updated: 2024-11-06

ablukast

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

Ablukast is a leukotriene receptor antagonist that was developed for the treatment of asthma. It is a selective antagonist of the cysteinyl leukotriene receptor 1 (CysLT1), which is involved in the inflammatory response in asthma. Ablukast is synthesized through a multi-step process starting from a commercially available compound. It has been shown to effectively reduce airway inflammation and bronchospasm in patients with asthma, leading to improved lung function and reduced symptoms. However, due to its low oral bioavailability and potential for adverse effects, ablukast is not currently marketed in many countries. Despite its limited clinical use, ablukast remains an important tool for researchers studying the role of leukotrienes in asthma and other inflammatory diseases. Further research is being conducted to explore its potential for other applications, such as the treatment of allergic rhinitis and chronic obstructive pulmonary disease.'

Cross-References

ID SourceID
PubMed CID57109
CHEMBL ID22016
SCHEMBL ID37501
MeSH IDM0152432

Synonyms (38)

Synonym
D02739
96566-25-5
ablukast (usan/inn)
ablukast
ro-23-3544
ro 23-3544/000
CHEMBL22016 ,
AKOS000278590
bdbm50009071
6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-pentyloxy]-chroman-2-carboxylic acid
6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-pentyloxy]-chroman-2-carboxylic acid(ro 23-3544)
6-acetyl-7-[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentoxy]-3,4-dihydro-2h-chromene-2-carboxylic acid
ro 23-3544
6-acetyl-7-(5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyloxy)-3,4-dihydro-2h-1-be nzopyran-2-carboxylic acid
131147-29-0
ablukast [usan:inn]
ablukastum [inn-latin]
000tkm5bbq ,
(+-)-6-acetyl-7-((5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyl)oxy)-2-chromancarboxylic acid
unii-000tkm5bbq
2h-1-benzopyran-2-carboxylic acid, 6-acetyl-7-((5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyl)oxy)-3,4-dihydro-, (+-)-
ablukastum
ablukast [usan]
(+/-)-6-acetyl-7-((5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyl)oxy)-2-chromancarboxylic acid
ro-23-3544/000
2h-1-benzopyran-2-carboxylic acid, 6-acetyl-7-((5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyl)oxy)-3,4-dihydro-, (+/-)-
ablukast [inn]
ro 23 3544/000
SCHEMBL37501
DTXSID20869277
6-acetyl-7-{[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyl]oxy}-3,4-dihydro-2h-1-benzopyran-2-carboxylic acid
Q4668103
MS-29252
HY-118958
CS-0078139
2h-1-benzopyran-2-carboxylic acid, 6-acetyl-7-[[5-(4-acetyl-3-hydroxy-2-propylphenoxy)pentyl]oxy]-3,4-dihydro-
AKOS040747736
122444-22-8

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" In this study, the dose-response curves of N-methyl LTC4 (NMLTC4), the nonmetabolizable LTC4 analogue, and the peptidoleukotrienes (LTC4, LTD4, and LTE4) were obtained in the absence and presence of the leukotriene antagonist Ro 23-3544 in cannulated frogs."( Cardiovascular effects of N-methyl leukotriene C4, a nonmetabolizable leukotriene C4 analogue, and the antagonism of leukotriene-induced hypotension by Ro 23-3544, in the American bullfrog, Rana catesbeiana.
Herman, CA; Sun, J, 1995
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)IC50 (µMol)36.00000.40002.23759.9000AID159037
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)6.00000.00091.230410.0000AID210502
Cysteinyl leukotriene receptor 1Homo sapiens (human)IC50 (µMol)4.00000.00030.948710.0000AID101444
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo 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 (16)

Processvia Protein(s)Taxonomy
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo 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 (5)

Processvia Protein(s)Taxonomy
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo 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 (34)

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.
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.
AID210502Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of TXB2 formation) in rat1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76825In vivo guinea pig bronchoconstriction against leukotriene E4 when administered a compound dose(mg/kg) intravenously1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76824In vivo guinea pig bronchoconstriction against leukotriene D4 when administered a compound dose (mg/kg) intravenously1989Journal 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.
AID78319In vivo guinea pig bronchoconstriction against leukotriene C4 when administered a compound dose (mg/kg) by aerosol administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
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.
AID78321In vivo guinea pig bronchoconstriction against leukotriene D4 when administered a compound dose (mg/kg) by aerosol administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID75789Duration of action of leukotriene E4 as time for inhibition to decrease to 40%, compound administered at a concentration of 1%,for 5 min by aerosol1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID75791Duration of action of leukotriene E4 as time for inhibition to decrease to 40%, compound was administered 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.
AID75786Duration of action of leukotriene D4 as time for inhibition to decrease to 40%, compound was administered 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.
AID54899Compound 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.
AID159037Inhibition of bovine heart Phosphodiesterase 1A1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID79494Compound 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.
AID77737Activity against platelet activating factor in guinea pig, no significant inhibition at concentration of 1% by aerosol; NA means inactive1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76229In vitro activity to inhibit leukotriene D4 induced contraction of guinea pig ileum1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID101444Compound was tested for inhibitory activity against LTD4 (leukotriene).1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID79332Antagonistic activity against LTD4 induced contraction in guinea pig trachea1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Peptide leukotrienes: current status of research.
AID180296Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of LTB4 formation) in rat1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76565Inhibitory activity to inhibit antigen induced bronchoconstriction in guinea pig1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID79514In vitro activity to inhibit leukotriene D4 induced contraction of guinea pig trachea1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76823In vivo guinea pig bronchoconstriction against leukotriene C4 when administered a compound dose (mg/kg) intravenously1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID75793Time taken for inhibition of antigen induced bronchoconstriction in guinea pig to decrease to 40%, compound was administered at a concentration of 1%, for 5 min by aerosol1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID78184In vitro guinea pig bronchoconstriction against leukotriene B4 when administered a compound dose (mg/kg) by aerosol administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID54902Inhibitory activity of compound to block binding of [3H]leukotriene D4 to Cysteinyl leukotriene D4 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.
AID76566Inhibitory activity to inhibit arachidonic acid induced bronchoconstriction1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID77733Activity against histamine induced bronchoconstriction in guinea pig, no significant inhibition at concentration of 1% by aerosol; NA means inactive1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID78322In vivo guinea pig bronchoconstriction against leukotriene E4 when administered a compound dose(mg/kg) by aerosol administration1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID155359Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of PGE-2 formation) in rat1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID77738Activity against platelet activating factor in guinea pig, no significant inhibition when compound dose (10 mg/kg) given intravenously; NA means inactive1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID55052Inhibitory activity of compound to block binding of [3H]leukotriene D4 to Cysteinyl L-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.
AID77734Activity against histamine induced bronchoconstriction in guinea pig, no significant inhibition when compound dose (10 mg/kg) given intravenously; NA means inactive1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID75784Duration of action of leukotriene D4 as time for inhibition to decrease to 40%, compound was administered at a concentration 1%, for 5 min by aerosol1989Journal 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 (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (33.33)18.7374
1990's6 (66.67)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: 12.22

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 Index12.22 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.22)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (11.11%)5.53%
Reviews2 (22.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]