Cunha F Q, Boukili M A, da Motta J I, Vargaftig B B, Ferreira S H
Departmento de Farmacologia, Faculdade de Medicina de Ribeirão Preto, Brazil.
Eur J Pharmacol. 1993 Jul 6;238(1):47-52. doi: 10.1016/0014-2999(93)90503-a.
Fenspiride, an antiinflammatory drug with low anti-cyclooxygenase activity, administered orally at 60-200 mg/kg inhibited neutrophil migration into peritoneal and air pouches cavities as well as exudation into peritoneal cavities induced by endotoxin but not induced by carrageenin. Up to 100 microM, fenspiride failed to inhibit the in vitro release of a neutrophil chemotactic activity by endotoxin-stimulated macrophages and the in vivo migration into the peritoneal cavities induced by the supernatant of those macrophages. The release of tumour necrosis factor by stimulated macrophages was inhibited by fenspiride in a dose-dependent manner. These results suggest that the antiinflammatory effects of fenspiride are associated with the inhibition of the tumour necrosis factor release by resident macrophages.
芬司匹利是一种具有低抗环氧化酶活性的抗炎药，口服剂量为60 - 200mg/kg时，可抑制中性粒细胞向腹膜腔和气囊腔的迁移，以及内毒素诱导的腹膜腔渗出，但对角叉菜胶诱导的渗出无抑制作用。在高达100微摩尔的浓度下，芬司匹利未能抑制内毒素刺激的巨噬细胞体外释放中性粒细胞趋化活性，也未能抑制这些巨噬细胞上清液诱导的体内向腹膜腔的迁移。芬司匹利以剂量依赖的方式抑制刺激的巨噬细胞释放肿瘤坏死因子。这些结果表明，芬司匹利的抗炎作用与抑制驻留巨噬细胞释放肿瘤坏死因子有关。
