Masso J M, Villar A M, Conde J R, Martorell J
Department of Pharmacology, ELMU-QUIMICA FARMACEUTICA S.L., Madrid, Spain.
Agents Actions. 1994 Oct;42(3-4):118-22. doi: 10.1007/BF01983476.
The antiinflammatory compound fepradinol has been tested in several experimental models of acute inflammation in rats. On the increased vascular permeability in the skin, fepradinol (25 mg/kg p.o.) was the only compound that inhibited the inflammatory actions induced by the three chemical mediators injected (histamine, serotonin and bradykinin). On the carrageenin-induced pleurisy, fepradinol (100 mg/kg p.o.) was more potent than indomethacin (5 mg/kg p.o.) and similar to piroxicam (5 mg/kg p.o.) in reducing the exudate volume and preventing cell migration. On the zymosan-induced peritonitis, while the activity of indomethacin (10 mg/kg p.o.) and cyproheptadine was observed only 3 h after zymosan challenge, the response of fepradinol developed within 30 min, suggesting that fepradinol inhibits both the early and late phases of the exudative response. These findings indicate that fepradinol may act on acute inflammation by reducing vascular permeability.
抗炎化合物非普拉醇已在大鼠急性炎症的多个实验模型中进行了测试。在皮肤血管通透性增加方面，非普拉醇（25毫克/千克，口服）是唯一能抑制注射的三种化学介质（组胺、5-羟色胺和缓激肽）诱导的炎症作用的化合物。在角叉菜胶诱导的胸膜炎中，非普拉醇（100毫克/千克，口服）在减少渗出液体积和防止细胞迁移方面比吲哚美辛（5毫克/千克，口服）更有效，且与吡罗昔康（5毫克/千克，口服）相似。在酵母聚糖诱导的腹膜炎中，虽然吲哚美辛（10毫克/千克，口服）和赛庚啶的活性仅在酵母聚糖攻击后3小时观察到，但非普拉醇的反应在30分钟内就出现了，这表明非普拉醇抑制渗出反应的早期和晚期阶段。这些发现表明，非普拉醇可能通过降低血管通透性作用于急性炎症。
