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Chemical Compound Review

Azlaire     N-[4-oxo-2-(2H-tetrazol-5- yl)chromen-7-yl]...

Synonyms: SureCN3694, ONO-RS 411, CID4887, AC1L3GIT, LS-27327, ...
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Disease relevance of ONO-RS 411


High impact information on ONO-RS 411


Chemical compound and disease context of ONO-RS 411


Biological context of ONO-RS 411

  • Provocation of bronchoconstriction was completely inhibited in subjects whose plasma ONO-1078 levels were more than 0.5 microgram/ml [15].
  • We conclude that (1) ONO-1078 attenuates LPS-induced acute lung injury; and (2) this effect appears mainly a result of its potent antagonistic actions against peptide leukotrienes and also, in part, the suppression of neutrophil chemotaxis [2].
  • Mean morning home PEFR increased by 10.8 to 18.61/min (95% CI 0.2 to 29.3 l/min) in patients treated with pranlukast compared with a slight deterioration in those given placebo [16].
  • We conclude that LTC(4) S genotype is predictive of the clinical response to a cysLT(1) antagonist, pranlukast, in Japanese patients with moderate asthma [17].
  • We examined the interaction between the clinical response to a cysLT(1) antagonist, pranlukast, and DNA sequence variant A(-444)C in leukotriene C(4) synthase (LTC(4) S) gene in Japanese patients with moderate asthma [17].

Anatomical context of ONO-RS 411

  • In the placebo group concentrations of serum eosinophil cationic protein and exhaled nitric oxide increased (p = 0.007 and p = 0.025, respectively), compared with no change in the ONO-1078 group [18].
  • Effect of the leukotriene receptor antagonist pranlukast on cellular infiltration in the bronchial mucosa of patients with asthma [19].
  • As pranlukast pretreatment did not affect plasma extravasation induced by mast cell degranulation, and depletion of platelets did not influence the pranlukast-inhibitable plasma extravasation induced by rhC5a injection, cys-LTs are most likely produced by transcellular biosynthesis involving PMNs and vascular wall cells [20].
  • ONO-1078 antagonizes diarrhea-causing changes in ion transport and smooth muscle contraction induced by peptidoleukotrienes in rat and human colon in vitro [21].
  • To do this we tested the effects of the selective and potent LTD(4) antagonist pranlukast on airway responses to ovalbumin (OVA) challenge of naive recipients of CD4(+) T cells isolated from the cervical lymph nodes of OVA-sensitized donor rats [22].

Associations of ONO-RS 411 with other chemical compounds


Gene context of ONO-RS 411


Analytical, diagnostic and therapeutic context of ONO-RS 411

  • METHODS: Ten atopic, nonsmoking patients with mild asthma and previously demonstrated early- and late-phase allergen-induced asthmatic responses participated in a double-blind, placebo-controlled, cross-over study, comparing treatment with either 450 mg pranlukast given twice daily or placebo for 5.5 days [28].
  • In clinical trials, pranlukast was well tolerated in adult and paediatric patients with asthma, with an adverse event profile similar to that of placebo [29].
  • Using fibreoptic bronchoscopy, bronchial biopsy specimens were obtained before and after treatment with either pranlukast (n = 10) or placebo (n = 7) [19].
  • Pranlukast attenuated neurological deficits, reduced infarct volume and ameliorated neuron loss in the ischemic core 24 h after reperfusion; it reduced infarct volume, ameliorated neuron loss and inhibited astrocyte proliferation in the boundary zone 14 days after reperfusion [30].
  • Flow cytometry demonstrated that pranlukast and MK-571 inhibit NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells in a dose-related manner [31].


  1. Churg-Strauss syndrome after corticosteroid withdrawal in an asthmatic patient treated with pranlukast. Kinoshita, M., Shiraishi, T., Koga, T., Ayabe, M., Rikimaru, T., Oizumi, K. J. Allergy Clin. Immunol. (1999) [Pubmed]
  2. Effects of ONO-1078, a peptide leukotriene antagonist, on endotoxin-induced acute lung injury. Ishizaka, A., Hasegawa, N., Sakamaki, F., Tasaka, S., Nakamura, H., Kishikawa, K., Yamada, A., Obata, T., Sayama, K., Urano, T. Am. J. Respir. Crit. Care Med. (1994) [Pubmed]
  3. The effect of an oral leukotriene antagonist, ONO-1078, on allergen-induced immediate bronchoconstriction in asthmatic subjects. Taniguchi, Y., Tamura, G., Honma, M., Aizawa, T., Maruyama, N., Shirato, K., Takishima, T. J. Allergy Clin. Immunol. (1993) [Pubmed]
  4. Effects of ONO-1078 (pranlukast) on cytokine production in peripheral blood mononuclear cells of patients with bronchial asthma. Tohda, Y., Nakahara, H., Kubo, H., Haraguchi, R., Fukuoka, M., Nakajima, S. Clin. Exp. Allergy (1999) [Pubmed]
  5. Efficacy of leukotriene receptor antagonist in bronchial hyperresponsiveness and hypersensitivity to analgesic in aspirin-intolerant asthma. Yoshida, S., Sakamoto, H., Ishizaki, Y., Onuma, K., Shoji, T., Nakagawa, H., Hasegawa, H., Nakabayashi, M., Amayasu, H. Clin. Exp. Allergy (2000) [Pubmed]
  6. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Lynch, K.R., O'Neill, G.P., Liu, Q., Im, D.S., Sawyer, N., Metters, K.M., Coulombe, N., Abramovitz, M., Figueroa, D.J., Zeng, Z., Connolly, B.M., Bai, C., Austin, C.P., Chateauneuf, A., Stocco, R., Greig, G.M., Kargman, S., Hooks, S.B., Hosfield, E., Williams, D.L., Ford-Hutchinson, A.W., Caskey, C.T., Evans, J.F. Nature (1999) [Pubmed]
  7. Leukotriene C4 is a tight-binding inhibitor of microsomal glutathione transferase-1. Effects of leukotriene pathway modifiers. Bannenberg, G., Dahlén, S.E., Luijerink, M., Lundqvist, G., Morgenstern, R. J. Biol. Chem. (1999) [Pubmed]
  8. The effect of pranlukast on allergen-induced bone marrow eosinophilopoiesis in subjects with asthma. Parameswaran, K., Watson, R., Gauvreau, G.M., Sehmi, R., O'Byrne, P.M. Am. J. Respir. Crit. Care Med. (2004) [Pubmed]
  9. Role for cysteinyl leukotrienes in allergen-induced change in circulating dendritic cell number in asthma. Parameswaran, K., Liang, H., Fanat, A., Watson, R., Snider, D.P., O'Byrne, P.M. J. Allergy Clin. Immunol. (2004) [Pubmed]
  10. Effect of pranlukast on bronchial inflammation in patients with asthma. Yoshida, S., Ishizaki, Y., Shoji, T., Onuma, K., Nakagawa, H., Nakabayashi, M., Akahori, K., Hasegawa, H., Amayasu, H. Clin. Exp. Allergy (2000) [Pubmed]
  11. Effects of anti-inflammatory therapies on recurrent and low-grade respiratory syncytial virus infections in a murine model of asthma. Matsuse, H., Kondo, Y., Machida, I., Kawano, T., Saeki, S., Tomari, S., Obase, Y., Fukushima, C., Mizuta, Y., Kohno, S. Ann. Allergy Asthma Immunol. (2006) [Pubmed]
  12. Challenge studies of a leukotriene receptor antagonist. Okudaira, H. Chest (1997) [Pubmed]
  13. Therapeutic effect of pranlukast, a selective cysteinyl leukotriene receptor antagonist, on bronchial asthma. Oosaki, R., Mizushima, Y., Kashii, T., Kawasaki, A., Kobayashi, M. Int. Arch. Allergy Immunol. (1997) [Pubmed]
  14. Effect of leukotriene antagonist on experimental delayed cerebral vasospasm. Kobayashi, H., Ide, H., Handa, Y., Aradachi, H., Arai, Y., Kubota, T. Neurosurgery (1992) [Pubmed]
  15. Inhibition of analgesic-induced asthma by leukotriene receptor antagonist ONO-1078. Yamamoto, H., Nagata, M., Kuramitsu, K., Tabe, K., Kiuchi, H., Sakamoto, Y., Yamamoto, K., Dohi, Y. Am. J. Respir. Crit. Care Med. (1994) [Pubmed]
  16. Pranlukast, a novel leukotriene receptor antagonist: results of the first European, placebo controlled, multicentre clinical study in asthma. Barnes, N.C., Pujet, J.C. Thorax (1997) [Pubmed]
  17. Leukotriene C4 synthase gene A(-444)C polymorphism and clinical response to a CYS-LT(1) antagonist, pranlukast, in Japanese patients with moderate asthma. Asano, K., Shiomi, T., Hasegawa, N., Nakamura, H., Kudo, H., Matsuzaki, T., Hakuno, H., Fukunaga, K., Suzuki, Y., Kanazawa, M., Yamaguchi, K. Pharmacogenetics (2002) [Pubmed]
  18. Leukotriene antagonist prevents exacerbation of asthma during reduction of high-dose inhaled corticosteroid. The Tokyo Joshi-Idai Asthma Research Group. Tamaoki, J., Kondo, M., Sakai, N., Nakata, J., Takemura, H., Nagai, A., Takizawa, T., Konno, K. Am. J. Respir. Crit. Care Med. (1997) [Pubmed]
  19. Effect of the leukotriene receptor antagonist pranlukast on cellular infiltration in the bronchial mucosa of patients with asthma. Nakamura, Y., Hoshino, M., Sim, J.J., Ishii, K., Hosaka, K., Sakamoto, T. Thorax (1998) [Pubmed]
  20. Roles of leukocytosis and cysteinyl leukotriene in polymorphonuclear leukocyte-dependent plasma extravasation. Tokita, K., Uchida, Y., Yamamoto, T. J. Leukoc. Biol. (2006) [Pubmed]
  21. ONO-1078 antagonizes diarrhea-causing changes in ion transport and smooth muscle contraction induced by peptidoleukotrienes in rat and human colon in vitro. Tominaga, M., Tsukada, H., Hosokawa, M., Nakamura, H., Taniguchi, T., Ueda, S., Sakai, M., Okuma, M. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  22. Role of cysteinyl leukotrienes in CD4(+) T cell-driven late allergic airway responses. Hojo, M., Suzuki, M., Maghni, K., Hamid, Q., Powell, W.S., Martin, J.G. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  23. Cysteinyl leukotrienes induce nuclear factor kappa b activation and RANTES production in a murine model of asthma. Kawano, T., Matsuse, H., Kondo, Y., Machida, I., Saeki, S., Tomari, S., Mitsuta, K., Obase, Y., Fukushima, C., Shimoda, T., Kohno, S. J. Allergy Clin. Immunol. (2003) [Pubmed]
  24. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Sarau, H.M., Ames, R.S., Chambers, J., Ellis, C., Elshourbagy, N., Foley, J.J., Schmidt, D.B., Muccitelli, R.M., Jenkins, O., Murdock, P.R., Herrity, N.C., Halsey, W., Sathe, G., Muir, A.I., Nuthulaganti, P., Dytko, G.M., Buckley, P.T., Wilson, S., Bergsma, D.J., Hay, D.W. Mol. Pharmacol. (1999) [Pubmed]
  25. Effect of pranlukast, an oral leukotriene receptor antagonist, on leukotriene D4 (LTD4) challenge in normal volunteers. O'Shaughnessy, T.C., Georgiou, P., Howland, K., Dennis, M., Compton, C.H., Barnes, N.C. Thorax (1997) [Pubmed]
  26. Prognostic significance of multidrug resistance protein in adult T-cell leukemia. Ohno, N., Tani, A., Chen, Z.S., Uozumi, K., Hanada, S., Akiba, S., Ren, X.Q., Furukawa, T., Sumizawa, T., Arima, T., Akiyama, S.I. Clin. Cancer Res. (2001) [Pubmed]
  27. Pranlukast inhibits NF-kappaB activation and MUC2 gene expression in cultured human epithelial cells. Ishinaga, H., Takeuchi, K., Kishioka, C., Suzuki, S., Basbaum, C., Majima, Y. Pharmacology (2005) [Pubmed]
  28. Pranlukast, a cysteinyl leukotriene receptor antagonist, attenuates allergen-induced early- and late-phase bronchoconstriction and airway hyperresponsiveness in asthmatic subjects. Hamilton, A., Faiferman, I., Stober, P., Watson, R.M., O'Byrne, P.M. J. Allergy Clin. Immunol. (1998) [Pubmed]
  29. Pranlukast: a review of its use in the management of asthma. Keam, S.J., Lyseng-Williamson, K.A., Goa, K.L. Drugs (2003) [Pubmed]
  30. Increased expression of cysteinyl leukotriene receptor-1 in the brain mediates neuronal damage and astrogliosis after focal cerebral ischemia in rats. Fang, S.H., Wei, E.Q., Zhou, Y., Wang, M.L., Zhang, W.P., Yu, G.L., Chu, L.S., Chen, Z. Neuroscience (2006) [Pubmed]
  31. Pranlukast inhibits NF-kappa B activation in human monocytes/macrophages and T cells. Ichiyama, T., Hasegawa, S., Umeda, M., Terai, K., Matsubara, T., Furukawa, S. Clin. Exp. Allergy (2003) [Pubmed]
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