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Chemical Compound Review

LS-74670     calcium(Z)-7-[5- (phenylsulfonylamino)-6...

Synonyms: AC1O60SO, S 1452, 132747-47-8
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Disease relevance of S 1452


High impact information on S 1452


Chemical compound and disease context of S 1452

  • These results indicate that TxA(2) as well as histamine may play an important role in antigen-induced nasal plasma exudation in guinea pigs, and S-1452 can be expected to be useful for the treatment of allergic rhinitis [8].
  • Furthermore, we examined the effect of S-1452, a TXA2 receptor antagonist, on the antigen-induced airway obstruction and AHR in guinea pigs [9].
  • During the 3-hr observation period following endotoxin administration, ibuprofen and S-1452 showed only early protection and TCV-309 showed late attenuation of the endotoxin-induced hypotension [10].

Biological context of S 1452

  • IC50 values to CDDP using MTT assay were decreased 2.1- and 4.6-fold respectively by treatment with 250 or 500 microM S-1452, for a 2 h simultaneous drug exposure, and those of PC-9/CDDP, a CDDP-resistant cell line, were decreased 3.1- and 6.1-fold [5].
  • These results suggest that although S-1452 is rapidly eliminated in plasma, its inhibitory effects on platelet aggregation persist for a longer period [11].
  • In addition, 0.1 mg x kg(-1) S-1452, a thromboxane A2 antagonist, or saline was given intravenously 5 min before UNDW inhalation in sensitized animals [12].
  • To study the pharmacokinetics of a new thromboxane A2 (TXA2) receptor antagonist, S-1452, eight healthy volunteers were given placebo or S-1452 orally on four occasions in step-wise increasing doses of 10 mg, 25 mg, and 50 mg separated by 2-week intervals [11].
  • Bleeding time was slightly prolonged after a single dose of S-1452 [11].

Anatomical context of S 1452

  • Exposure of the nasal cavity of guinea pigs to aerosolized U-46619, a TxA2 mimetic, also resulted in a marked increase in intranasal pressure, and this could be almost completely suppressed by S-1452 [13].
  • The in vitro uptake of lipo [14C] S-145-Me by fresh human neutrophils and an eosinophil cell line was respectively 7 times and 3.5 times higher than that of [14C] S-1452 [14].
  • The accumulation of inflammatory cells by antigen provocation in bronchial alveolar lavage fluid (BALF) was inhibited by ketotifen but not by S-1452 [15].
  • S-1452, a potent and selective TXA2 receptor antagonist, blocks the receptors of vascular smooth muscle cells (VSMC) as well as platelets [16].
  • For the short-term study, eighteen rabbits after balloon injury of iliac artery were assigned to 3 groups; systemic administration of S-1452, single local administration of S-1452 using a local delivery balloon, and single local administration of saline solution [16].

Associations of S 1452 with other chemical compounds


Gene context of S 1452


Analytical, diagnostic and therapeutic context of S 1452


  1. Effect of a novel thromboxane A2 receptor antagonist, S-1452, on postischemic brain injury in rats. Matsuo, Y., Izumiyama, M., Onodera, H., Kurosawa, A., Kogure, K. Stroke (1993) [Pubmed]
  2. Effects of aerosol administration of a thromboxane receptor antagonist (S-1452) on experimental asthma in guinea pigs. Saito, M., Fujimura, M., Mizuhashi, K., Shintani, H., Matsuda, T. Allergy (1994) [Pubmed]
  3. Involvement of thromboxane A2 in bronchial hyperresponsiveness but not lung inflammation induced by bacterial lipopolysaccharide in guinea pigs. Arimura, A., Asanuma, F., Yagi, H., Kurosawa, A., Harada, M. Eur. J. Pharmacol. (1993) [Pubmed]
  4. Role of thromboxane derived from COX-1 and -2 in hepatic microcirculatory dysfunction during endotoxemia in mice. Katagiri, H., Ito, Y., Ishii, K., Hayashi, I., Suematsu, M., Yamashina, S., Murata, T., Narumiya, S., Kakita, A., Majima, M. Hepatology (2004) [Pubmed]
  5. Modulation of sensitivity to cis-diamminedichloroplatinum (II) by thromboxane A2 receptor antagonists in non-small-cell lung cancer cell lines. Kasahara, K., Fujimura, M., Bando, T., Shibata, K., Shirasaki, H., Matsuda, T. Br. J. Cancer (1996) [Pubmed]
  6. Contribution of thromboxane A2 to the antigen-induced immediate asthmatic response mediated by IgG1 antibody by augmentation of bronchial responsiveness in guinea-pigs. Arimura, A., Asanuma, F., Kurosawa, A., Harada, M. Br. J. Pharmacol. (1994) [Pubmed]
  7. Up-regulation of ICH-1L protein by thromboxane A2 antagonists enhances cisplatin-induced apoptosis in non-small-cell lung-cancer cell lines. Fujimura, M., Kasahara, K., Shirasaki, H., Heki, U., Iwasa, K., Ueda, A., Matsuda, T. J. Cancer Res. Clin. Oncol. (1999) [Pubmed]
  8. Inhibitory effect of a TP-receptor antagonist, S-1452, on antigen-induced nasal plasma exudation in guinea pig model for allergic rhinitis. Yasui, K., Asanuma, F., Arimura, A. Pharmacology (2001) [Pubmed]
  9. Time course study for airway inflammation and responsiveness by repeated provocation of aeroantigen in guinea pigs. Takeda, H., Kogame, A., Tanaka, H., Nagai, H. Prostaglandins (1997) [Pubmed]
  10. Role of platelet-activating factor and prostanoids in hemodynamic changes in rat experimental endotoxic shock. Ebara, T., Miura, K., Matsuura, T., Imanishi, M., Yamano, Y., Kim, S., Iwao, H. Jpn. J. Pharmacol. (1996) [Pubmed]
  11. Pharmacokinetics of a new thromboxane A2 receptor antagonist, S-1452, and its effect on platelet aggregation in healthy volunteers. Fujimura, A., Shiga, T., Kumagai, Y., Ohashi, K., Ebihara, A., Kotegawa, T. Journal of clinical pharmacology. (1996) [Pubmed]
  12. A guinea-pig model of ultrasonically nebulized distilled water-induced bronchoconstriction. Fujimura, M., Amemiya, M., Myou, S., Mizuguchi, M., Matsuda, T. Eur. Respir. J. (1997) [Pubmed]
  13. Involvement of thromboxane A2 in antigen-induced nasal blockage in guinea pigs. Yasui, K., Asanuma, F., Furue, Y., Arimura, A. Int. Arch. Allergy Immunol. (1997) [Pubmed]
  14. Application of lipid microspheres to prepare a thromboxane A2 receptor antagonist aerosol for inhalation. Takenaga, M., Nakagawa, T., Igarashi, R., Mizushima, Y. Journal of drug targeting. (1993) [Pubmed]
  15. The effect of a novel thromboxane A2 (TXA2) receptor antagonist (S-1452) on the antigen-induced bronchoconstriction and airway hyperresponsiveness in guinea pigs. Nagai, H., Arimura, A., Yoshitake, K., Iwama, T., Sakurai, T., Koda, A. Prostaglandins Leukot. Essent. Fatty Acids (1993) [Pubmed]
  16. Effects of the thromboxane A2 receptor antagonist on platelet deposition and intimal hyperplasia after balloon injury. Yamagami, S., Miyauchi, K., Kimura, T., Goh, Y., Daida, H., Yamaguchi, H. Japanese heart journal. (1999) [Pubmed]
  17. Role of platelet-activating factor and thromboxane A2 in radical production during ischemia and reperfusion of the rat brain. Matsuo, Y., Kihara, T., Ikeda, M., Ninomiya, M., Onodera, H., Kogure, K. Brain Res. (1996) [Pubmed]
  18. Effects of RS-601, a novel leukotriene D(4)/thromboxane A(2) dual receptor antagonist, on asthmatic responses in guinea pigs. Yamada, T., Takahashi, Y., Ishizaki, M., Musoh, K., Ohashi, T., Tanaka, H., Inagaki, N., Nagai, H. Pharmacology (2003) [Pubmed]
  19. Effects of selective cyclooxygenase inhibitors on ischemia/reperfusion-induced hepatic microcirculatory dysfunction in mice. Ito, Y., Katagiri, H., Ishii, K., Kakita, A., Hayashi, I., Majima, M. European surgical research. Europäische chirurgische Forschung. Recherches chirurgicales européennes. (2003) [Pubmed]
  20. Role of thromboxane A2, endothelin-1 and endothelin-3 in rat nephrotoxic serum nephritis. Zhou, L., Ida, T., Marumo, F. Tohoku J. Exp. Med. (1996) [Pubmed]
  21. Effect of thromboxane A2 inhibitors on allergic pulmonary inflammation in mice. Shi, H., Yokoyama, A., Kohno, N., Hirasawa, Y., Kondo, K., Sakai, K., Hiwada, K. Eur. Respir. J. (1998) [Pubmed]
  22. Antiproteinuric effect of a thromboxane receptor antagonist, S-1452, on rat diabetic nephropathy and murine lupus nephritis. Matsuo, Y., Takagawa, I., Koshida, H., Kawabata, T., Nakamura, M., Ida, T., Zhou, L., Marumo, F. Pharmacology (1995) [Pubmed]
  23. Effect of treatment at night with S-1452, a thromboxane A2 receptor antagonist, on the morning rise in platelet aggregation. Fujimura, A., Kumagai, K., Ohashi, K., Ebihara, A. Eur. J. Clin. Pharmacol. (1992) [Pubmed]
  24. Delayed hypotensive effect of the thromboxane A2/prostaglandin H2 receptor antagonist S-1452 in spontaneously hypertensive rats. Sugimoto, K.I., Shiga, T., Fujimura, A. Clin. Exp. Pharmacol. Physiol. (2000) [Pubmed]
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