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Chemical Compound Review

Tomelukast     1-[2-hydroxy-3-propyl-4-[4- (2H-tetrazol-5...

Synonyms: Tomelukastum, SureCN3944, CHEMBL162358, AG-J-77739, SureCN5325407, ...
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Disease relevance of Tomelukast


High impact information on Tomelukast

  • In the presence of tumor necrosis factor-alpha (TNF-alpha), the PPAR(alpha) agonists WY14643 and LY171883 as well as the lipid-lowering compound clofibrate potentiated expression, secretion, and activity of group IIA sPLA(2) in mesangial cells [6].
  • Several LTD4 receptor antagonists (ICI-198615, WY-48252, WY-49511, FPL-55712, and LY-171883) displaced [3H]ICI-198615 specific binding, with a rank order of potency equivalent to that described in the guinea pig tracheal smooth muscle contraction system [7].
  • This study clearly demonstrates that LY-171883 stimulates the activity of BK(Ca) channels in a manner unlikely to be linked to its blockade of leukotriene receptors or stimulation of peroxisome proliferator-activated receptors [3].
  • The LY-171883-stimulated activity of BK(Ca) channels is dependent on membrane potential, and results mainly from an increase in mean open time and a decrease in mean closed time [3].
  • Under the current-clamp condition, LY-171883 (30 microM) caused membrane hyperpolarization as well as decreased the firing rate of action potentials in GH(3) cells [3].

Chemical compound and disease context of Tomelukast


Biological context of Tomelukast

  • Reversal of significantly increased coronary vascular resistance coupled with improved functional recovery in hearts treated with LY171883 demonstrates an important contribution of endogenously produced leukotrienes to coronary vascular impairment and functional stunning of the globally ischaemic, reperfused heart [12].
  • RESULTS: There was no significant difference at any time point in the experimental protocol between mean arterial blood pressure or pressure-rate index in cats given LY-171883 (3 and cats given vehicle [13].
  • Dose-related antagonism of leukotriene D4-induced bronchoconstriction by p.o. administration of LY-171883 in nonasthmatic subjects [14].
  • The data indicate that 0.3% LY171883 sufficiently increased mitochondrial and peroxisomal beta-oxidation such that fatty acids generated by lipogenesis were preferentially oxidized rather than esterified to triglycerides [15].
  • The effect of LY171883 on lipid metabolism was studied further in rats maintained on a fat-free diet [15].

Anatomical context of Tomelukast


Associations of Tomelukast with other chemical compounds


Gene context of Tomelukast


Analytical, diagnostic and therapeutic context of Tomelukast

  • The peptide leukotriene receptor antagonist, LY-171883, was given intravenously only during the reperfusion period (3 bolus; 3 x h-1 infusion) [13].
  • The mutation frequency and spectrum of the 61st codon of H-ras was determined for 64 independent, archived lesions from the LY171883 2 year oncogenicity study using the polymerase chain reaction (PCR), allele specific oligo hybridization (ASO) and DNA sequencing [2].
  • Fatty acid synthetase activity increased comparably in all treatment groups, indicating that 0.3% LY171883 did not prevent the lipogenic response to a fat-free diet [15].
  • We have investigated the inhibitory activity of the p.o. LTD4 antagonist LY-171883 (1-[2-hydroxy-3-propyl]-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]et hanone) on LTD4-induced bronchoconstriction in nonasthmatic subjects, in a double-blind, placebo controlled, randomized, cross-over study [14].
  • LY171883 (4 mg/kg/h) and DEC (40 mg/kg/h) were administered via the aural vein from 30 min before the tourniquet and during the experiment in each tourniquet group [9].


  1. Hepatocellular DNA synthesis in rats given peroxisome proliferating agents: comparison of WY-14,643 to clofibric acid, nafenopin and LY171883. Eacho, P.I., Lanier, T.L., Brodhecker, C.A. Carcinogenesis (1991) [Pubmed]
  2. H-ras 61st codon activation in archival proliferative hepatic lesions isolated from female B6C3F1 mice exposed to the leukotriene D4-antagonist, LY171883. Helvering, L.M., Richardson, F.C., Horn, D.M., Rexroat, M.A., Engelhardt, J.A., Richardson, K.K. Carcinogenesis (1994) [Pubmed]
  3. Enhanced activity of Ca2+-activated K+ channels by 1-[2-hydroxy-3-propyl-4-[(1H-tetrazol-5-yl)butoxyl]phenyl] ethanone (LY-171883) in neuroendocrine and neuroblastoma cell lines. Li, P.C., Liang, J.T., Huang, H.T., Lin, P.H., Wu, S.N. J. Cell. Physiol. (2002) [Pubmed]
  4. Protective effect of a selective leukotriene antagonist in endotoxemia in the rat. Cook, J.A., Wise, W.C., Halushka, P.V. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  5. Hemodynamic effects of heat-killed group B beta-hemolytic streptococcus in newborn lambs: role of leukotriene D4. Schreiber, M.D., Covert, R.F., Torgerson, L.J. Pediatr. Res. (1992) [Pubmed]
  6. Potentiation of TNF-alpha-stimulated group IIA phospholipase A(2) expression by peroxisome proliferator-activated receptor alpha activators in rat mesangial cells. Scholz-Pedretti, K., Gans, A., Beck, K.F., Pfeilschifter, J., Kaszkin, M. J. Am. Soc. Nephrol. (2002) [Pubmed]
  7. Binding of radiolabeled high affinity antagonist to leukotriene D4 receptor in guinea pig lung membranes: interconversion of agonist-receptor binding affinity states. O'Sullivan, B.P., Mong, S. Mol. Pharmacol. (1989) [Pubmed]
  8. Hepatic peroxisomal changes induced by a tetrazole-substituted alkoxyacetophenone in rats and comparison with other species. Eacho, P.I., Foxworthy, P.S., Johnson, W.D., Hoover, D.M., White, S.L. Toxicol. Appl. Pharmacol. (1986) [Pubmed]
  9. Protective effect of peptide leukotriene antagonist on renal failure induced by a tourniquet in rabbits. Tanaka, T., Kita, T., Liu, R., Tanaka, N. Forensic Sci. Int. (1995) [Pubmed]
  10. Endotoxemia in rats--influence of lipoxygenase blocker versus leukotriene receptor antagonist (BW755C vs LY171883). Bahrami, S., Paul, E., Redl, H., Schlag, G., Mihm, F. Prog. Clin. Biol. Res. (1988) [Pubmed]
  11. Adrenalectomy exacerbates paw edema without interfering with desensitization induced by PAF-acether in rats. Silva, P.M., Martins, M.A., Castro-Faria-Neto, H.C., Cordeiro, R.S., Vargaftig, B.B. Braz. J. Med. Biol. Res. (1988) [Pubmed]
  12. Leukotrienes D4 and E4 produced in myocardium impair coronary flow and ventricular function after two hours of global ischaemia in rat heart. Lee, C.C., Appleyard, R.F., Byrne, J.G., Cohn, L.H. Cardiovasc. Res. (1993) [Pubmed]
  13. Peptide leukotriene receptor antagonism in myocardial ischaemia and reperfusion. Hock, C.E., Beck, L.D., Papa, L.A. Cardiovasc. Res. (1992) [Pubmed]
  14. Dose-related antagonism of leukotriene D4-induced bronchoconstriction by p.o. administration of LY-171883 in nonasthmatic subjects. Phillips, G.D., Rafferty, P., Robinson, C., Holgate, S.T. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  15. Effect of the peroxisome proliferator LY171883 on triglyceride accumulation in rats fed a fat-free diet. Foxworthy, P.S., Eacho, P.I. Biochem. Pharmacol. (1991) [Pubmed]
  16. Interaction of LY171883 and other peroxisome proliferators with fatty-acid-binding protein isolated from rat liver. Cannon, J.R., Eacho, P.I. Biochem. J. (1991) [Pubmed]
  17. LY171883, 1-less than 2-hydroxy-3-propyl-4-less than 4-(1H-tetrazol-5-yl) butoxy greater than phenyl greater than ethanone, an orally active leukotriene D4 antagonist. Fleisch, J.H., Rinkema, L.E., Haisch, K.D., Swanson-Bean, D., Goodson, T., Ho, P.P., Marshall, W.S. J. Pharmacol. Exp. Ther. (1985) [Pubmed]
  18. Effect of ciprofibrate, bezafibrate, and LY171883 on peroxisomal beta-oxidation in cultured rat, dog, and rhesus monkey hepatocytes. Foxworthy, P.S., White, S.L., Hoover, D.M., Eacho, P.I. Toxicol. Appl. Pharmacol. (1990) [Pubmed]
  19. Heterogeneity of binding sites for ICI 198,615 in human lung parenchyma. Rovati, G.E., Giovanazzi, S., Mezzetti, M., Nicosia, S. Biochem. Pharmacol. (1992) [Pubmed]
  20. Role of 5-lipoxygenase pathway in the regulation of RAW 264.7 macrophage proliferation. Nieves, D., Moreno, J.J. Biochem. Pharmacol. (2006) [Pubmed]
  21. Peroxisome proliferator-activated receptor-gamma agonists increase vascular endothelial growth factor expression in human vascular smooth muscle cells. Yamakawa, K., Hosoi, M., Koyama, H., Tanaka, S., Fukumoto, S., Morii, H., Nishizawa, Y. Biochem. Biophys. Res. Commun. (2000) [Pubmed]
  22. Peroxisome proliferator-activated receptor and farnesoid X receptor ligands differentially regulate sebaceous differentiation in human sebaceous gland organ cultures in vitro. Downie, M.M., Sanders, D.A., Maier, L.M., Stock, D.M., Kealey, T. Br. J. Dermatol. (2004) [Pubmed]
  23. Peroxisome-proliferator-activated receptor alpha agonists inhibit cyclo-oxygenase 2 and vascular endothelial growth factor transcriptional activation in human colorectal carcinoma cells via inhibition of activator protein-1. Grau, R., Punzón, C., Fresno, M., Iñiguez, M.A. Biochem. J. (2006) [Pubmed]
  24. Ligand-dependent interaction of hepatic fatty acid-binding protein with the nucleus. Lawrence, J.W., Kroll, D.J., Eacho, P.I. J. Lipid Res. (2000) [Pubmed]
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