Neuman R G, Wilson B D, Barkley M, Kimball E S, Weichman B M, Wood D D
Agents Actions. 1987 Jun;21(1-2):160-6. doi: 10.1007/BF01974936.
Etodolac is the first anti-inflammatory drug belonging to the tetrahydropyranoindole class. In contrast to several other common anti-inflammatory drugs, etodolac exhibited an unusually high potency as an inhibitor of established adjuvant arthritis relative to its activity against carrageenan paw edema in the rat. This phenomenon led us to investigate whether the ability of NSAIDs to inhibit prostaglandin biosynthesis differed between cultures of macrophages, which are present in inflammatory exudates, and cultures of synoviocytes and chondrocytes, which contribute to inflammation of the articulating joint. Although other anti-inflammatory drugs were found to be equally active in all three cell types, etodolac was found to be much more effective on the cells of the joint than on the macrophage. This differential activity may be responsible for the striking efficacy of etodolac as an anti-arthritic drug.
依托度酸是首个属于四氢吡喃吲哚类的抗炎药。与其他几种常见抗炎药不同，相对于其对大鼠角叉菜胶足爪水肿的作用，依托度酸在抑制佐剂性关节炎方面表现出异常高的效力。这一现象促使我们研究非甾体抗炎药抑制前列腺素生物合成的能力在炎症渗出液中的巨噬细胞培养物、以及导致关节炎症的滑膜细胞和软骨细胞培养物之间是否存在差异。尽管发现其他抗炎药在所有三种细胞类型中均具有同等活性，但发现依托度酸对关节细胞的作用比对巨噬细胞的作用更为有效。这种差异活性可能是依托度酸作为抗关节炎药物具有显著疗效的原因。
