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[Inhibitory effect on the release of mediators from rat peritoneal exudate cells and the antagonistic effect against mediators of MY-5116 and other anti-allergic agents].
Nihon Yakurigaku Zasshi. 1986 Sep; 88(3):229-37.NY

Abstract

The effects of a new anti-allergic agent, MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylate, and its main metabolite, MY-1250: 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylic acid, on 48 hr homologous PCA (PCA) in rats and the release of histamine and SRS from rat peritoneal exudate cells (PEC) induced by IgE antibody in comparison with other anti-allergic agents were investigated. Also, the effects of MY-5116 and MY-1250 on antagonistic action against histamine and LTD4 were studied. MY-5116, tranilast and ketotifen inhibited PCA at oral doses of more than 3 mg/kg, 300 mg/kg and 0.3 mg/kg, respectively. MY-1250, DSCG and tranilast inhibited significantly the release of histamine from PEC induced by the antigen-antibody reaction in a dose-dependent manner, and the values of IC50 were 4.9 X 10(-8), 4.8 X 10(-6) and 4.6 X 10(-6) g/ml, respectively. Ketotifen inhibited significantly the release of histamine at a concentration of 10(-5) g/ml, but it accelerated significantly the release of histamine from PEC at a concentration of 10(-4) g/ml. MY-1250 and tranilast suppressed the release of SRS from PEC induced by the antigen-antibody reaction. The values of IC50 of MY-1250 and tranilast were 1.5 X 10(-6) and 2.1 X 10(-6) g/ml, respectively. MY-1250 suppressed slightly the release of SRS from PEC induced by A23187. MY-5116 showed no effect on the increase of vascular permeability induced by histamine, bradykinin and serotonin in rats.(ABSTRACT TRUNCATED AT 250 WORDS)

Authors

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Pub Type(s)

Comparative Study
Journal Article

Language

jpn

PubMed ID

2431983

Citation

Yamada, N, et al. "[Inhibitory Effect On the Release of Mediators From Rat Peritoneal Exudate Cells and the Antagonistic Effect Against Mediators of MY-5116 and Other Anti-allergic Agents]." Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica, vol. 88, no. 3, 1986, pp. 229-37.
Yamada N, Takahashi K, Endoh K, et al. [Inhibitory effect on the release of mediators from rat peritoneal exudate cells and the antagonistic effect against mediators of MY-5116 and other anti-allergic agents]. Nihon Yakurigaku Zasshi. 1986;88(3):229-37.
Yamada, N., Takahashi, K., Endoh, K., & Arai, Y. (1986). [Inhibitory effect on the release of mediators from rat peritoneal exudate cells and the antagonistic effect against mediators of MY-5116 and other anti-allergic agents]. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica, 88(3), 229-37.
Yamada N, et al. [Inhibitory Effect On the Release of Mediators From Rat Peritoneal Exudate Cells and the Antagonistic Effect Against Mediators of MY-5116 and Other Anti-allergic Agents]. Nihon Yakurigaku Zasshi. 1986;88(3):229-37. PubMed PMID: 2431983.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Inhibitory effect on the release of mediators from rat peritoneal exudate cells and the antagonistic effect against mediators of MY-5116 and other anti-allergic agents]. AU - Yamada,N, AU - Takahashi,K, AU - Endoh,K, AU - Arai,Y, PY - 1986/9/1/pubmed PY - 1986/9/1/medline PY - 1986/9/1/entrez SP - 229 EP - 37 JF - Nihon yakurigaku zasshi. Folia pharmacologica Japonica JO - Nihon Yakurigaku Zasshi VL - 88 IS - 3 N2 - The effects of a new anti-allergic agent, MY-5116: isoamyl 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylate, and its main metabolite, MY-1250: 5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c] quinoline-2-carboxylic acid, on 48 hr homologous PCA (PCA) in rats and the release of histamine and SRS from rat peritoneal exudate cells (PEC) induced by IgE antibody in comparison with other anti-allergic agents were investigated. Also, the effects of MY-5116 and MY-1250 on antagonistic action against histamine and LTD4 were studied. MY-5116, tranilast and ketotifen inhibited PCA at oral doses of more than 3 mg/kg, 300 mg/kg and 0.3 mg/kg, respectively. MY-1250, DSCG and tranilast inhibited significantly the release of histamine from PEC induced by the antigen-antibody reaction in a dose-dependent manner, and the values of IC50 were 4.9 X 10(-8), 4.8 X 10(-6) and 4.6 X 10(-6) g/ml, respectively. Ketotifen inhibited significantly the release of histamine at a concentration of 10(-5) g/ml, but it accelerated significantly the release of histamine from PEC at a concentration of 10(-4) g/ml. MY-1250 and tranilast suppressed the release of SRS from PEC induced by the antigen-antibody reaction. The values of IC50 of MY-1250 and tranilast were 1.5 X 10(-6) and 2.1 X 10(-6) g/ml, respectively. MY-1250 suppressed slightly the release of SRS from PEC induced by A23187. MY-5116 showed no effect on the increase of vascular permeability induced by histamine, bradykinin and serotonin in rats.(ABSTRACT TRUNCATED AT 250 WORDS) SN - 0015-5691 UR - https://www.unboundmedicine.com/medline/citation/2431983/[Inhibitory_effect_on_the_release_of_mediators_from_rat_peritoneal_exudate_cells_and_the_antagonistic_effect_against_mediators_of_MY_5116_and_other_anti_allergic_agents]_ L2 - https://www.medicalonline.jp/meteo_linkout.php?issn=0015-5691&volume=88&issue=3&spage=229 DB - PRIME DP - Unbound Medicine ER -