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Pharmacological characterization of the cysteinyl-leukotriene antagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.
Capra V, Bolla M, Belloni PA, Mezzetti M, Folco GC, Nicosia S, Rovati GE. Capra V, et al. Br J Pharmacol. 1998 Feb;123(3):590-8. doi: 10.1038/sj.bjp.0701636. Br J Pharmacol. 1998. PMID: 9504401 Free PMC article.
We investigated the pharmacological profile of the cysteinyl-LT antagonists CGP 45715A (iralukast), a structural analogue of LTD4 and CGP 57698, a quinoline type antagonist, in human airways in vitro, by performing binding studies on human lung parenchyma mem …
We investigated the pharmacological profile of the cysteinyl-LT antagonists CGP 45715A (iralukast), a structural analog …
A review on leukotrienes and their receptors with reference to asthma.
Singh RK, Tandon R, Dastidar SG, Ray A. Singh RK, et al. J Asthma. 2013 Nov;50(9):922-31. doi: 10.3109/02770903.2013.823447. Epub 2013 Aug 16. J Asthma. 2013. PMID: 23859232 Review.
Most common among them are classical CysLT1 receptor antagonists such as montelukast, zafirlukast, pranlukast, pobilukast, iralukast, cinalukast and MK571. The pharmacological role of CysLT2 receptor, however, is less defined and there is no specific antagonist available s …
Most common among them are classical CysLT1 receptor antagonists such as montelukast, zafirlukast, pranlukast, pobilukast, iralukast, …
Comparative effects of a glucocorticosteroid, theophylline and the peptido-leukotriene-antagonist CGP 45715A on antigen-induced early and late phase airway response and inflammatory cell influx in sensitised guinea pigs.
Heuer HO, Leon I, Anderson GP, Jennewein HM. Heuer HO, et al. Eur J Pharmacol. 1999 Mar 19;369(2):225-31. doi: 10.1016/s0014-2999(99)00080-1. Eur J Pharmacol. 1999. PMID: 10206183
Methylprednisolone (40 mg/kg p.o. 1 h before ovalbumin) did not inhibit the immediate response, but the late phase response. In contrast the cysteinyl-leukotriene antagonist CGP 45715A (Iralukast; 30 mg/kg p.o. 2 h before ovalbumin) neither interfered with th …
Methylprednisolone (40 mg/kg p.o. 1 h before ovalbumin) did not inhibit the immediate response, but the late phase response. In contrast the …
Trace-level quantitation of iralukast in human plasma by microbore liquid chromatography/tandem mass spectrometry.
Majumdar TK, Bakhtiar R, Melamed D, Tse FL. Majumdar TK, et al. Rapid Commun Mass Spectrom. 2000;14(6):476-81. doi: 10.1002/(SICI)1097-0231(20000331)14:6<476::AID-RCM898>3.0.CO;2-6. Rapid Commun Mass Spectrom. 2000. PMID: 10717659 Clinical Trial.
Iralukast (CGP 45715A) is a potent peptido-leukotriene antagonist that is active in various in vitro and animal models for the treatment of asthma. ...First, iralukast appeared to be light sensitive and unstable at room temperature under acidic conditi …
Iralukast (CGP 45715A) is a potent peptido-leukotriene antagonist that is active in various in vitro and animal models …
The action of the peptidoleukotriene LTD4 on intracellular calcium in rat mesangial cells.
Ochsner M. Ochsner M. Experientia. 1996 Sep 15;52(9):856-64. doi: 10.1007/BF01938870. Experientia. 1996. PMID: 8841513
The dose-dependent effect of CGP 45715A on the LTD4-induced Ca2+ response of glomerular mesangial cells has been studied. Our results demonstrate that the LTD4-dependent increase in the cytosolic Ca2+ concentration primarily involves an InsP3-mediated release of Ca2 …
The dose-dependent effect of CGP 45715A on the LTD4-induced Ca2+ response of glomerular mesangial cells has been studied. Our …
Physics-driven identification of clinically approved and investigation drugs against human neutrophil serine protease 4 (NSP4): A virtual drug repurposing study.
Ahmad J, Ikram S, Hafeez AB, Durdagi S. Ahmad J, et al. J Mol Graph Model. 2020 Dec;101:107744. doi: 10.1016/j.jmgm.2020.107744. Epub 2020 Sep 4. J Mol Graph Model. 2020. PMID: 33032202
Based on our rigorous filtration, we found that following molecules Becatecarin, Iogulamide, Delprostenate and Iralukast are predicted to block the activity of NSP4 by interacting with core catalytic residues. ...
Based on our rigorous filtration, we found that following molecules Becatecarin, Iogulamide, Delprostenate and Iralukast are predicte …
Autocrine activity of cysteinyl leukotrienes in human vascular endothelial cells: Signaling through the CysLT₂ receptor.
Capra V, Carnini C, Accomazzo MR, Di Gennaro A, Fiumicelli M, Borroni E, Brivio I, Buccellati C, Mangano P, Carnevali S, Rovati G, Sala A. Capra V, et al. Prostaglandins Other Lipid Mediat. 2015 Jul;120:115-25. doi: 10.1016/j.prostaglandins.2015.03.007. Epub 2015 Apr 1. Prostaglandins Other Lipid Mediat. 2015. PMID: 25839425
We also demonstrate here that the CysLT1R antagonist zafirlukast, pranlukast, pobilukast and iralukast also possess CysLT2R antagonistic activity, which could help in reconsidering previous data on the role of cysteinyl-LTs in the cardiovascular system. ...
We also demonstrate here that the CysLT1R antagonist zafirlukast, pranlukast, pobilukast and iralukast also possess CysLT2R antagonis …
Iralukast Novartis AG.
Bramley A. Bramley A. IDrugs. 1998 May;1(1):147-50. IDrugs. 1998. PMID: 18465520
Iralukast is an LTD4 and LTE4 antagonist under development by Novartis and in phase II clinical trials as a potential treatment for asthma [244117], [177071]. In a double-blind, placebo-controlled trial in 16 patients with mild to moderate asthma, a single 1.5 mg inhaled d …
Iralukast is an LTD4 and LTE4 antagonist under development by Novartis and in phase II clinical trials as a potential treatment for a …
Anti-inflammatory agents and allergen-induced beta2-receptor dysfunction in isolated human bronchi.
Song P, Crimi E, Milanese M, Duan J, Rehder K, Brusasco V. Song P, et al. Am J Respir Crit Care Med. 1998 Dec;158(6):1809-14. doi: 10.1164/ajrccm.158.6.9801105. Am J Respir Crit Care Med. 1998. PMID: 9847272
Human bronchial rings (2 to 4 mm) from surgery were passively sensitized to house dust mite and challenged (1) with allergen only, (2) with allergen plus indomethacin (10(-)5 M), (3) with allergen plus nedocromil sodium (10(-)7 M to 10(-)5 M), (4) with allergen plus the H1-recept …
Human bronchial rings (2 to 4 mm) from surgery were passively sensitized to house dust mite and challenged (1) with allergen only, (2) with …
18 results