Fujiyoshi T, Ikeda K, Saito M, Yamaura T, Iida H, Maeda E, Kase N, Uematsu T
Nihon Yakurigaku Zasshi. 1986 Apr;87(4):379-95. doi: 10.1254/fpj.87.379.
This study was conducted to clarify the antiinflammatory profile of EB-382, comparing it with those of ibuprofen and other antiinflammatory agents. EB-382 had a more potent inhibition on the acetic acid-induced intensive mouse intraperitoneal vascular permeability and carrageenin-induced rat hind paw edema, but a less potent inhibition on the ultraviolet-induced guinea-pig erythema and the prostaglandin biosynthesis in vitro than ibuprofen. The inhibition by EB-382 was equipotent to that of indomethacin on carrageenin-induced rat pleurisy and the zymosan air pouch, and it demonstrated a strong inhibition on the kallikrein and zymosan-induced intensive guinea-pig skin vascular permeability. EB-382 had a more effective activity on paper disk-induced granuloma and adjuvant arthritis, and it had a less potent action on the gastric mucosal membrane than ibuprofen. EB-382 had a weak action on histamine-induced rat back skin vascular permeability and heat-induced protein denaturation and hemolysis in vitro, as also shown by other test agents. The above results indicate that EB-382 will be useful as an antiinflammatory agent with a new pharmacological effectiveness besides possessing properties common to other acidic non-steroidal antiinflammatory agents in clinical studies.
本研究旨在阐明EB - 382的抗炎特性，并将其与布洛芬及其他抗炎药进行比较。与布洛芬相比，EB - 382对乙酸诱导的小鼠腹腔血管通透性增强及角叉菜胶诱导的大鼠后爪水肿具有更强的抑制作用，但对紫外线诱导的豚鼠红斑及体外前列腺素生物合成的抑制作用较弱。EB - 382对角叉菜胶诱导的大鼠胸膜炎及酵母聚糖气囊的抑制作用与吲哚美辛相当，且对激肽释放酶和酵母聚糖诱导的豚鼠皮肤血管通透性增强具有强烈抑制作用。EB - 382对纸片诱导的肉芽肿和佐剂性关节炎具有更有效的作用，且对胃黏膜的作用比布洛芬弱。EB - 382对组胺诱导的大鼠背部皮肤血管通透性及体外热诱导的蛋白质变性和溶血作用较弱，其他受试药物也有此表现。上述结果表明，EB - 382除了在临床研究中具有其他酸性非甾体抗炎药的共同特性外，还将作为一种具有新药理活性的抗炎药发挥作用。
