Detail of "53902-12-8"

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Pharmacological studies on the release of slow-reacting substance of anaphylaxis during anti-immunoglobulin E antibody-mediated passive peritoneal anaphylaxis in rats

Pharmacological studies on the release of slow-reacting substance of anaphylaxis during anti-immunoglobulin E antibody-mediated passive peritoneal anaphylaxis in rats. Nagai, Hiroichi; Yamada, Hiroaki; Matsuura, Naosuke; Iwamoto, Teiji; Choi, Soo Hyung; Koda, Akihide (Dep. Pharmacol., Gifu Pharm. Univ., Gifu 502, Japan). J. Pharmacobio-Dyn., 10(1), 49-54 (English) 1987.Some commonly used reagents like 53-86-1 and 34580-13-7 are used in this experiment. CODEN: JOPHDQ. ISSN: 0386-846X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The release of slow-reacting substance of anaphylaxis (SRS-A) by antiimmunoglobulin E (e)-antibody mediated passive peritoneal anaphylaxis (PPA) in rats was investigated immunopharmacol. A significant amt. of SRS-A was released by anti-e-antibody in the peritoneal cavity of rats passively sensitized with IgE. The amt. of SRS-A released by anti-e-antibody was about one third less than that released in an anti-g-antibody and IgG2a system. The release of SRS-A was initiated at 2 min and reached its max. 5 to 10 min after the injection of anti-e-antibody. Disodium cromoglycate [15826-37-6], tranilast [53902-12-8] and ketotifen [34580-13-7] inhibited the release of both SRS-A and histamine [51-45-6] caused by anti-e-antibody mediated PPA. Glucocorticoids (hydrocortisone [50-23-7], prednisolone [50-24-8] and dexamethasone [50-02-2]) and also p-Bromophenacyl bromide [99-73-0] inhibited the release of both mediators. AA-861 [80809-81-0], a potent 5-lipoxygenase inhibitor, inhibited the release of SRS-A but not histamine. Indomethacin [53-86-1] slightly enhanced the release of SRS-A and inhibited the release of histamine. Cytarabine [147-94-4] resulted in leucopenia and inhibited the release of histamine but not SRS-A during PPA. Dextran sulfate [9042-14-2] reduced the no. of glass adherent peritoneal cells and inhibited the release of SRS-A but not histamine. These results suggest the suitability of anti-e-antibody mediated rat PPA for investigating the effect of anti-allergic agents on the release of SRS-A. .

Anti-allergic effect of the metabolites and photoproducts of tranilast

Anti-allergic effect of the metabolites and photoproducts of tranilast. Kojima, Masami; Tsutsumi, Naoyuki; Ujiie, Arao; Naito, Jun (Cent. Res. Lab., Kissei Pharm. Co., Ltd., Matsumoto 399-65, Japan). Oyo Yakuri, 28(4), 623-8 (Japanese) 1984. CODEN: OYYAA2. ISSN: 0369-8033. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Metabolites and photoproducts of tranilast (I) [53902-12-8] were tested for antiallergic effect, in comparison with the parent drug, on the 48 h homologous passive cutaneous anaphylaxis (PCA) in rats. In addn., the effect of cis-tranilast one of the photoproducts, on the spontaneous and allergic histamine release from rat peritoneal exudate cells (PEC) was also tested. Tranilast, (37.5-150 mg/kg, orally) dose-dependently inhibited the homologous PCA; the inhibition was nearly complete at 150 mg/kg. N-(4-Hydroxy-3-methoxycinnamoyl)anthranilic acid (N-3) [93755-77-2], a 4-demethylated metabolite, showed an equipotent inhibitory effect. Virtually no effect was seen with 2-(3,4-dimethoxystyryl)-3,1-benzoxazine-4-one (N-6) [93755-78-3], a dehydrated-ring metabolite, and with 1,3-di(2-carboxyphenylcarbamoyl)-2,4-di(3,4-dimethoxyphenyl)cyclo butane (N-13) [93755-79-4] and 1,2-di(2-carboxyphenylcarbamoyl)-3,4-di(3,4-dimethoxyphenyl)cyclo butane (N-14) [93755-80-7], 2 photoproducts which are dimers of tranilast. The cis-isomer showed dose-dependent inhibition, but the effect was smaller than that of tranilast. Both tranilast and cis-isomer, (10-6-10-3 M), concn.-dependently inhibited the antigen-induced histamine release from rat PEC sensitized with anti-DNP-As rat serum, but the effect of tranilast was more potent than that of the cis-isomer. Neither tranilast nor the cis-isomer (10-5-10-3 M) affected the spontaneous histamine release from rat PEC, but ketotifen, 10-3 M, enhanced it. Apparently, the antiallergic effects of transilast do not occur through its metabolite or photoproducts such as N-6, N-13, N-14, or cis-isomer.