Page last updated: 2024-12-07

fpl 55712

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Description

FPL 55712: inhibitor of SRS-A and LTC4 and LTD4 receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID23662025
SCHEMBL ID1890293
MeSH IDM0048819
PubMed CID105007
CHEMBL ID267475
CHEBI ID91977
SCHEMBL ID6059336
MeSH IDM0048819

Synonyms (45)

Synonym
fpl-55712
7-((3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxyl))-4-oxo-8-propyl-4h-chromene-2-carboxy late, sodium salt
4h-1-benzopyran-2-carboxylic acid, 7-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy)-4-oxo-8-propyl-, monosodium salt
40786-08-1
FT-0639668
SCHEMBL1890293
8o730gh8al ,
unii-8o730gh8al
7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]- 4-oxo-8-propyl-4h-1-benzopyran-2-carboxylic acid sodium salt
fpl55712
7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-4h-1-benzopyran-2-carboxylic acid sodium salt
ZDEVPOBNLIVGFA-UHFFFAOYSA-M
fpl-55712, >=97% (hplc), solid
4h-1-benzopyran-2-carboxylic acid, 7-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy)-4-oxo-8-propyl-, sodium salt (1:1)
sodium;7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propylchromene-2-carboxylate
DTXSID00961203
HMS3268H08
BRD-A96456596-001-01-4
NCGC00159548-01
fpl 55712
CHEMBL267475 ,
7-[3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy]-4-oxo-8-propyl-4h-chromene-2-carboxylic acid(fpl 55712)
7-[3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy]-4-oxo-8-propyl-4h-chromene-2-carboxylic acid
7-[3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy]-4-oxo-8-propyl-4h-chromene-2-carboxylic acid (fpl55712)
7-[3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy]-4-oxo-8-propyl-4h-chromene-2-carboxylic acid(fpl-55712)
bdbm50006812
7-[3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy]-4-oxo-4h-chromene-2-carboxylic acid(fpl 55,712)
7-[3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy]-4-oxo-8-propyl-4h-chromene-2-carboxylic acid;fpl-55,712
7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propylchromene-2-carboxylic acid
7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-4h-1-benzopyran-2-carboxylic acid
LMQBMWHHGVZWMR-UHFFFAOYSA-N ,
SCHEMBL6059336
40785-97-5
AKOS024457024
CHEBI:91977
Q27163775
7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-1-benzopyran-2-carboxylic acid
HMS3677A18
7-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy)-4-oxo-8-propyl-4h-chromene-2-carboxylic acid
unii-8q3m8gl2xv
fpl-55712 free base
8Q3M8GL2XV ,
4h-1-benzopyran-2-carboxylic acid, 7-(3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy)-4-oxo-8-propyl-
HMS3413A18
7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8-propyl-4h-1-benzopyran-2-carboxylicacid

Research Excerpts

Overview

PLP 55712 was shown to be a competitive antagonist, producing a parallel displacement of dose response curves to LTD4 with no depression of the maximum. The action is most likely due to receptor blockade of the vasoconstrictive endogenous leukotrienes.

ExcerptReferenceRelevance
"FPL 55712 was shown to be a competitive antagonist, producing a parallel displacement of dose response curves to LTD4 with no depression of the maximum."( Kinetics of action of two leukotriene antagonists on guinea pig ileum.
Ghelani, AM; Holroyde, MC, 1983
)
0.99
"FPL 55712 is an antagonist of LT receptor, whereas A63162 is an inhibitor of lipoxygenase."( Mediators and oxygen radicals in hyperpnea-induced airway constriction of guinea pigs.
Lai, YL; Lee, CF, 2000
)
1.03
"FPL 55712 appears to be a placental vasodilator whose action is most likely due to receptor blockade of the vasoconstrictive endogenous leukotrienes."( Placental vascular responses to leukotriene receptor antagonist FPL 55712.
Parisi, VM; Phernetton, TM; Rankin, JH, 1985
)
1.23

Treatment

Pretreatment with FPL 55712, a leukotriene synthesis blocker, caused an increase in TXB2 and PGE2 levels. The formation of 6-keto-PGF1 alpha remained unaltered.

ExcerptReferenceRelevance
"Pretreatment with FPL 55712, a leukotriene synthesis blocker, caused an increase in TXB2 and PGE2 levels, whereas the formation of 6-keto-PGF1 alpha remained unaltered."( Prostanoid imbalance in experimental acute necrotizing pancreatitis in rats.
Kort, WJ; van Ooijen, B; Vincent, JE; Westbroek, DL; Wilson, JH; Zijlstra, FJ, 1988
)
0.6
"Pretreatment with FPL 55712 (38 microM), a leukotriene receptor antagonist, or indomethacin (10 micrograms/ml of perfusate) completely prevented the increase in tracheal and pulmonary arterial pressure."( Leukotriene D4 increases pulmonary vascular permeability and pressure by different mechanisms in the rabbit.
Farrukh, IS; Gurtner, GH; Michael, JR; Sciuto, AM; Spannhake, EW, 1986
)
0.59

Dosage Studied

ExcerptRelevanceReference
" The dye leakage response to nasal capsaicin challenge was abolished by pretreatment with topical lidocaine, general substance P analogue, topical or general high dosage capsaicin."( Study on the dye leakage response of nasal mucosa following topical, capsaicin challenge in guinea pigs.
Asakura, K; Kataura, A; Kojima, T; Narita, S; Shirasaki, H, 1992
)
0.28
" A combination of FPL55712 (leukotriene antagonist), diphenhydramine (histamine antagonist), and indomethacin (cyclooxygenase inhibitor) shifted the dose-response curve of ET-1 to the right and suppressed the maximal constriction."( Multiple mechanisms of bronchoconstrictive responses to endothelin-1.
Hasegawa, S; Hirata, F; Ishii, Y; Ninomiya, H; Nomura, A; Ohse, H; Saotome, M; Uchida, Y, 1991
)
0.28
" Furthermore, an inverse dose-response relationship was observed between the extent of gastric lesions and the number of mast cells in the gastric mucosa."( The possible role of LTC4 in the pathogenesis of ethanol-induced gastric lesions in mice and their prevention by 5-lipoxygenase inhibitor AA-861, and leukotriene receptor antagonist FPL-55712.
Abe, T; Higa, A; Nawa, Y; Tanaka, K; Yoshida, T, 1991
)
0.28
" 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
" The LxA4 dose-response curve was parallel to that of leukotriene D4 (LTD4) with LxA4 being approximately 10,000 fold less potent than LTD4."( The contractile activities of lipoxin A4 and lipoxin B4 for guinea-pig airway tissues.
Crea, AE; Jacques, CA; Lee, TH; Spur, BW, 1988
)
0.27
" The dose-response curve was bimodal for LTC4 with two maxima at 10(-8) and 10(-16) M (X2."( Leukotrienes C4 and D4 stimulate the release of luteinizing hormone-releasing hormone from rat median eminence in vitro.
Dray, F; Gerozissis, K; Saadi, M, 1987
)
0.27
" L-Serine borate complex, 45 mM, used as an inhibitor of the degradation of LTC4 to LTD4 by the enzyme gamma-glutamyl transpeptidase, in paired airway segments (adjacent segments from the same branch), produced a small degree (about 3-fold) of shift to the right of the dose-response curve and reduction of the maximum response to LTC4."( Pharmacological evidence that human intralobar airways do not contain different receptors that mediate contractions to leukotriene C4 and leukotriene D4.
Bernstein, PR; Buckner, CK; Coursin, DB; Krell, RD; Laravuso, RB; Will, JA, 1986
)
0.27
" Aerosol pretreatment with the cyclooxygenase inhibitor indomethacin had no significant effect on either LTC4 or LTD4 dose-response curves; however, at the highest doses of these agonists a notable, nonsignificant inhibition of effects on both Rp and Cdyn was seen."( Pharmacology of aerosol leukotriene C4- and D4-induced alteration of pulmonary mechanics in anesthetized cynomolgus monkeys.
Giles, RE; Krell, RD; Williams, JC, 1986
)
0.27
" Maximum contraction occurred simultaneously with the maximum amount of histamine appearing in the superfusate, but the dose-response curves of ovalbumin were different for the two responses."( Studies on the relationship between contraction and mediator release produced by ovalbumin in superfused trachea isolated from the actively sensitized guinea pig.
Buckner, CK; Fishleder, RI, 1984
)
0.27
" The dose-response curve describing LTD4-induced changes in dynamic lung compliance (CDYN) and pulmonary resistance (RL) [as reflective indices of bronchoconstriction] was shifted to the left by approximately 20-fold by propranolol."( Propranolol potentiates leukotriene D4-induced bronchoconstriction and enhances antagonism by FPL 55712.
Kirchner, T; Weichman, BM, 1984
)
0.49
" Pure leukotrienes (C and D) in a dose-response fashion prevented the adherence of leukocytes to glass; the nonadherence of mononuclear cells was equal to that of polymorphonuclear cells."( Armed human monocytes challenged with a sensitizing cancer extract release substances pharmacologically similar to leukotrienes.
Bach, MK; Morton, DG; Phelan, K; Thomson, DM, 1982
)
0.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency4.46680.002014.677939.8107AID1476
Microtubule-associated protein tauHomo sapiens (human)Potency28.18380.180013.557439.8107AID1460
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency17.78280.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency25.11890.354828.065989.1251AID504847
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
[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)
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)1.58000.00001.18439.6140AID220176
Bile salt export pumpHomo sapiens (human)IC50 (µMol)10.00000.11007.190310.0000AID1449628
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)10.75500.00462.018210.0000AID6783; AID7087
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)IC50 (µMol)40.00000.40002.23759.9000AID159038
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)10.00000.00091.230410.0000AID212967
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Ki0.72500.00010.23581.5000AID55066; AID55067
Cysteinyl leukotriene receptor 2Homo sapiens (human)IC50 (µMol)0.51000.00102.405210.0000AID77996
Cysteinyl leukotriene receptor 1Homo sapiens (human)IC50 (µMol)2.25500.00030.948710.0000AID55234; AID77996
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cysteinyl leukotriene receptor 1Cavia porcellus (domestic guinea pig)Kb0.48000.00300.22100.4800AID55225
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (52)

Processvia Protein(s)Taxonomy
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
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 (26)

Processvia Protein(s)Taxonomy
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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 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 (16)

Processvia Protein(s)Taxonomy
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo 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 (108)

Assay IDTitleYearJournalArticle
AID76853Inhibition of LTE4-induced bronchoconstriction in guinea pig at dose of (1 ug/kg) given intravenously1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
AID76710Percent inhibition LTD4-induced contraction of guinea pig ileum at 30 uM of concentration; ND denotes no data1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Leukotriene receptor antagonists. 1. Synthesis and structure-activity relationships of alkoxyacetophenone derivatives.
AID79366Compound was evaluated for the inhibitory activity against Acetylcholine in guinea pig ileum1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Evaluation of rotenone and related compounds as antagonists of slow-reacting substance of anaphylaxis.
AID76845Inhibition of LTB4 induced bronchoconstriction in guinea pig at dose of (1 ug/kg) given intravenously1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
AID76848Inhibition of LTC4-induced bronchoconstriction in guinea pig at dose of (0.5 ug/kg) given intravenously1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
AID55064Compound is evaluated for its ability to inhibit [3H]LTD4 binding to Cysteinyl leukotriene D4 receptor in guinea pig lung membranes1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis and structure-activity relationship studies of a series of 5-aryl-4,6-dithianonanedioic acids and related compounds: a novel class of leukotriene antagonists.
AID78378Antagonistic effect on LTD4 induced changes in dynamic lung compliance (CDYN) in anesthetized guinea pigs, at dose 5 mg/kg when administered intravenously1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.
AID77998Ability to prevent constrictions induced by SRS-A (slow reacting substance of anaphylaxis) in guinea pig ileum1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Antagonists of slow-reacting substance of anaphylaxis. 1. Pyrido[2,1-b]quinazolinecarboxylic acid derivatives.
AID55229Binding constant was determined as affinity to displace [3H]LTD4 from Cysteinyl leukotriene D4 receptor on guinea pig lung membrane1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.
AID76850Inhibition of LTD4-induced bronchoconstriction in guinea pig at dose of (0.5 ug/kg) given intravenously1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
AID79977Inhibition of LTD4-induced contraction of guinea pig ileum.1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Leukotriene receptor antagonists. 1. Synthesis and structure-activity relationships of alkoxyacetophenone derivatives.
AID78106Compound was evaluated in vivo for collapse time in guinea pig anaphylaxis model at dose 10 mg/kg1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Evaluation of rotenone and related compounds as antagonists of slow-reacting substance of anaphylaxis.
AID55227Dissociation constant towards Cysteinyl leukotriene D4 receptor of guinea pig1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.
AID79367Compound was evaluated for the inhibitory activity against Histamine in guinea pig ileum1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Evaluation of rotenone and related compounds as antagonists of slow-reacting substance of anaphylaxis.
AID78533Antagonistic effect on LTD4 induced change in airway resistance (RL) in anesthetized guinea pigs, at dose 5 mg/kg when administered intravenously1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.
AID78130Compound was evaluated for the inhibitory activity against slow reacting substance of anaphylaxis (SRS-A) of guinea pig ileum1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Evaluation of rotenone and related compounds as antagonists of slow-reacting substance of anaphylaxis.
AID79368Compound was evaluated for the inhibitory activity against Serotonin in guinea pig ileum1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Evaluation of rotenone and related compounds as antagonists of slow-reacting substance of anaphylaxis.
AID78302Inhibition of LTC4 induced smooth muscle contraction of guinea pig ileum1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
AID76829In vivo inhibition of LTD4-induced bronchoconstriction in anesthetized guinea pig.1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships.
AID1133850Antagonism of slow reacting substance of anaphylaxis-induced contraction in guinea pig ileum treated 30 secs before SRS-A challenge1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Antagonists of slow reacting substance of anaphylaxis. Synthesis of a series of chromone-2-carboxylic acids.
AID76822In vivo antagonistic activity against leukotriene D4 (LTD4) in guinea pig lung1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Novel 1,3-bis(aryloxy)propanes as leukotriene D4 antagonists.
AID73699In vitro ability to antagonize a leukotriene D4 induced contraction of guinea pig trachea.1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Synthesis and structure-activity relationship studies of a series of 5-aryl-4,6-dithianonanedioic acids and related compounds: a novel class of 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.
AID55068Binding affinity against Cysteinyl leukotriene D4 receptor in guinea pig lung membranes using [3H]LTD4 as the radioligand.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.
AID78303In vitro inhibition of SRS-A-induced contractions in guinea pig ileum1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
AID75785Duration 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.
AID221990Ability to antagonize LTD4-induced contractions of human airway smooth muscle (bronchus) at 10 uM concentration1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.
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.
AID1124757Antiallergic activity against ip dosed passive peritoneal anaphylaxis rat model assessed as inhibition of histamine release in peritoneal fluid administered 30s prior to ovalbumin challenge measured per rat after 5 mins1979Journal of medicinal chemistry, Feb, Volume: 22, Issue:2
Aryloxyalkyloxy- and aralkyloxy-4-hydroxy-3-nitrocoumarins which inhibit histamine release in the rat and also antagonize the effects of a slow reacting substance of anaphylaxis.
AID78133In vitro Schultz-Dale Test against isolated guinea pig lung strips repeatedly challenged with antigen in the presence of an antihistamine (H1) at a concentration 30 uM.1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Acidic furo[3,2-b]indoles. A new series of potent antiallergy agents.
AID78329In vivo inhibition of LTE4 (leukotriene)-induced skin wheal formation in guinea pig and percent inhibition was reported at 100 mg/Kg administered perorally1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
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.
AID76737Percent inhibition of bronchospasm when administered at a dose of 2.5 mg/kg in guinea pig1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release.
AID76738Percent inhibition of bronchospasm when administered at a dose of 5 mg/kg in guinea pig1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release.
AID80455In vitro ability to antagonize LTC4-induced contractions of guinea pig smooth muscle (trachea) at 10 uM concentration.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.
AID78283Evaluated for inhibition of slow reacting substance of anaphylaxis (SRS-A) induced contractions in guinea pig ileum strips1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
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.
AID78324In vivo inhibition of LTE4 (leukotriene)-induced bronchoconstrictions in guinea pig and percent inhibition was reported at 10 mg/Kg administered intravenously1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
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.
AID55067Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig lung was determined using [3H]-LTD4 (0.2 nM)1990Journal 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.
AID78328In vivo inhibition of LTE4 (leukotriene)-induced skin wheal formation in guinea pig and percent inhibition was reported at 10 mg/Kg administered intravenously1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID76224Inhibitory potency against leukotriene E4 (LTE) induced bronchoconstriction in guinea pigs.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
AID76225Inhibitory potency against platelet activating factor (PAF) induced bronchoconstriction in guinea pigs.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
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.
AID76604Compound (50 mg/kg, intraperitoneally) was tested in spontaneously breathing, conscious guinea pigs challenged with aerosolized LTD4 (30-min pretreatment)1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Hydroxyacetophenone-derived antagonists of the peptidoleukotrienes.
AID77161Percent inhibition of the leukotriene D4-induced contraction of guinea pig tracheal spirals at 4 uM concentration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Hydroxyacetophenone-derived antagonists of the peptidoleukotrienes.
AID78863Compound was evaluated for inhibition of contraction in guinea pig ileum induced by leukotriene D4 (LTD4).1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
(Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4.
AID91643In vitro ability to antagonize LTC4-induced contractions of human smooth muscle (bronchus) at 10 uM concentration.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.
AID55212Binding affinity against LTD4 receptor in guinea pig lung membranes.1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID55214Antagonist activity was evaluated against Cysteinyl leukotriene D4 receptor induced contraction in guinea pig ileum1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl)oxy]methyl]acetophenone derivatives.
AID79183In vitro inhibition of responses induced by LTD4 in Isolated terminal guinea pig ileum segments at 0.1 ug/mL1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.
AID76080Inhibition of LTC4-induced contractions from guinea pig peripheral lung strips1990Journal 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.
AID75788Duration 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.
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.
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.
AID77110In vivo activity against bronchoconstrictions induced by LTD4 (0.2 ug/kg, iv) in anesthetized guinea pig following iv administration of compound1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.
AID80466Inhibition of ovalbumin-induced contraction (10 ng/mL) of guinea pig trachea at 10 uM1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Synthesis and structure-activity relationships of carboxylated chalcones: a novel series of CysLT1 (LTD4) receptor antagonists.
AID76223Inhibitory potency against leukotriene D4 (LTD) induced bronchoconstriction in guinea pigs.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
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.
AID78183In vitro guinea pig bronchoconstriction against leukotriene B4 (when administered at a concentration of 1%, by aerosol); Not active1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID76609Compound (50 mg/kg, intraperitoneally) was tested in spontaneously breathing, conscious guinea pigs challenged with aerosolized LTD4 (60-min pretreatment); NS means data were not statistically significant.1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Hydroxyacetophenone-derived antagonists of the peptidoleukotrienes.
AID76328In vivo inhibition of leukotriene-induced bronchoconstriction in guinea pigs following 10 mg/kg i.v. administration.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
AID159038Inhibition 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.
AID76073In vivo inhibition of leukotriene-induced bronchoconstriction in guinea pigs, was determined, by administering compound by aerosol route, after 77 min1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
AID55225Dissociation constant (KB) versus Cysteinyl leukotriene D4 receptor was evaluated in vitro in isolated guinea pig tracheal strips1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Hydroxyacetophenone-derived antagonists of the peptidoleukotrienes.
AID77736Activity against platelet activating factor in guinea pig (when administered at a concentration of 1%, by aerosol); Not active1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
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.
AID55063Dissociation constant was determined against Cysteinyl leukotriene D4 receptor of guinea pig lung membranes using radioligand binding assays.1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
(Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4.
AID75790Duration 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.
AID79198Compound was evaluated for antihistaminic activity against isolated guinea pig ileum; Not active1995Journal of medicinal chemistry, Jun-23, Volume: 38, Issue:13
(Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4.
AID76736Percent inhibition of bronchospasm when administered at a dose of 1 mg/kg in guinea pig1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Antiallergy agents. 1. Substituted 1,8-naphthyridin-2(1H)-ones as inhibitors of SRS-A release.
AID78320In vivo guinea pig bronchoconstriction against leukotriene C4 when administered at a concentration of 1%, by aerosol; NS means no significant inhibition.1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID73694Inhibition of LTD4-induced contraction in guinea pig ileum1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl)oxy]methyl]acetophenone derivatives.
AID77402Tested in vivo for antigen-induced systemic anaphylaxis after oral administration; inactive1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID55234Compound was tested for binding affinity against Cysteinyl leukotriene D4 receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID78325In vivo inhibition of LTE4 (leukotriene)-induced bronchoconstrictions in guinea pig and percent inhibition was reported at 100 mg/Kg administered perorally1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
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.
AID1124756Antagonism of slow reacting substance of anaphylaxis-induced effect in guinea pig ileum1979Journal of medicinal chemistry, Feb, Volume: 22, Issue:2
Aryloxyalkyloxy- and aralkyloxy-4-hydroxy-3-nitrocoumarins which inhibit histamine release in the rat and also antagonize the effects of a slow reacting substance of anaphylaxis.
AID7087The compound was tested for inhibitory activity against 5-lipoxygenase in rat RBL-1 cells1992Journal 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.
AID77732Activity against histamine induced bronchoconstriction in guinea pig (when administered at a concentration of 1%, by aerosol); Not active1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID74037In vivo activity against bronchoconstrictions induced by LTD4 (0.2 ug/kg, iv) in anesthetized guinea pig following id administration of compound1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.
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.
AID77735Activity against histamine induced bronchoconstriction in guinea pig, no significant inhibition when compound dose (10 mg/kg) given intravenously; Not active.1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID77400Tested in vivo for LTD4-induced bronchoconstriction after oral administration by Dermal wheal assay method; inactive1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID79874Inhibition of leukotriene-induced contractions of peripheral guinea pig lung strip1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID77996Inhibition of the spasmogenic activity of LTD4 in guinea pig parenchymal strips.1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.
AID79495Compound was tested for LTD4 induced guinea pig trachea contraction1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID55066Binding affinity against Cysteinyl leukotriene D4 receptor from guinea pig lung was determined using [3H]LTD4 (0.2 nM)1990Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 1. Initial structure-activity relationships.
AID55075In vitro binding affinity against cysteinyl leukotriene D4 receptor from guinea pig lung membrane1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
The development of a novel series of (quinolin-2-ylmethoxy)phenyl-containing compounds as high-affinity leukotriene receptor antagonists. 3. Structural variation of the acidic side chain to give antagonists of enhanced potency.
AID76219Inhibitory potency against histamine induced bronchoconstriction in guinea pigs.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
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.
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.
AID76567Inhibitory activity to inhibit arachidonic acid induced bronchoconstriction (when administered at a concentration of 1%, by aerosol); Not active1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID77048Ability to inhibit the contraction induced by 8 nM LTE4 on isolated guinea pig tracheal strips at 4 uM dose; % antagonism / % basal tension1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
Synthesis and pharmacological characterization of a series of leukotriene analogues with antagonist and agonist activities.
AID76221Inhibitory potency against leukotriene C4 (LTC) induced bronchoconstriction in guinea pigs.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted (aryloxy)alkanoic acids as antagonists of slow-reacting substance of anaphylaxis.
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.
AID77739Activity against platelet activating factor in guinea pig, no significant inhibition when compound dose (10 mg/kg) given intravenously; Not active.1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID75792Time taken for inhibition of antigen induced bronchoconstriction in guinea pig 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.
AID55061Displacement of [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranes1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
Synthesis and structure-activity relationships of carboxylated chalcones: a novel series of CysLT1 (LTD4) receptor antagonists.
AID80456In vitro ability to antagonize LTD4-induced contractions of guinea pig smooth muscle (trachea) at 10 uM concentration.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.
AID75787Duration of action of leukotriene D4 as time for inhibition to decrease to 40%, when 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.
AID220176Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta.1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.
AID6783Inhibition of rat neutrophil 5- Lipoxygenase (5-LO), (at a concentration of 0.2 nM ),1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Substituted arylmethyl phenyl ethers. 1. A novel series of 5-lipoxygenase inhibitors and leukotriene antagonists.
AID212967Inhibition of human platelet thromboxane synthase (TXA2) was determined in human platelets1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (394)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990306 (77.66)18.7374
1990's82 (20.81)18.2507
2000's3 (0.76)29.6817
2010's1 (0.25)24.3611
2020's2 (0.51)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.65

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 Index8.65 (24.57)
Research Supply Index5.98 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.65)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials2 (0.51%)5.53%
Reviews0 (0.00%)6.00%
Reviews12 (3.05%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies2 (0.51%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
Other377 (95.93%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]