Shirota H, Chiba K, Goto M, Hashida R, Ono H
Eisai Tsukuba Research Laboratories, Ibaraki, Japan.
Agents Actions Suppl. 1991;32:219-23. doi: 10.1007/978-3-0348-7405-2_29.
E5090 is a novel orally active inhibitor of IL-1 generation without cyclooxygenase-inhibiting activity. The effects of E5090 on several inflammatory animal models were investigated in rats. In adjuvant arthritis, E5090 suppressed both the paw swelling and the enhancements of ESR and number of peripheral blood leucocytes, like the steroidal antiinflammatory drug prednisolone. However, the thymus was not withered by E5090 though it was by prednisolone. In type II collagen-induced arthritis, E5090 inhibited paw swelling and joint destruction. E5090 was effective in acute inflammatory models such as carrageenin-induced paw edema, and adjuvant-induced local hyperthermia, and also showed analgesic effects against inflammatory pain and antipyretic effects. The results suggest that this orally active inhibitor of IL-1 generation, E5090, may be a therapeutically useful antiinflammatory drug with a novel mechanism of action.
E5090是一种新型的口服活性白细胞介素-1生成抑制剂，无环氧化酶抑制活性。在大鼠中研究了E5090对几种炎症动物模型的影响。在佐剂性关节炎中，E5090抑制爪肿胀以及血沉增速和外周血白细胞数量的增加，类似于甾体抗炎药泼尼松龙。然而，E5090并未使胸腺萎缩，而泼尼松龙会使其萎缩。在Ⅱ型胶原诱导的关节炎中，E5090抑制爪肿胀和关节破坏。E5090在急性炎症模型如角叉菜胶诱导的爪水肿和佐剂诱导的局部体温过高中有效，并且对炎性疼痛也显示出镇痛作用以及解热作用。结果表明，这种口服活性白细胞介素-1生成抑制剂E5090可能是一种具有新型作用机制的治疗用抗炎药物。
