Tsurumi K, Kokuba S, Okada K, Yanagihara M, Fujimura H
Arzneimittelforschung. 1986 Dec;36(12):1810-7.
The preventive and therapeutic effects of 2-(10,11-dihydro-10-oxodibenzo [b,f]thiepin-2-yl)propionic acid (CN-100) on local and systemic changes of rats with adjuvant arthritis being used frequently as experimental model of rheumatoid arthritis were investigated in comparison with those of reference drugs, indometacin and pranoprofen. Preventively and therapeutically CN-100 showed potent inhibitory effects on adjuvant primary inflammation and secondary lesion. CN-100 also exerted an evident preventive effect on destruction of foot bone, improved the changes in organ weight, and stimulated weight gain. These effects were dose-dependent, and the effects at 5.0 mg/kg were almost the same as those of indometacin and pranoprofen at 1.25 and 2.5 mg/kg, respectively. The mode of action of CN-100 resembled that of reference compounds. Although CN-100 improved the change in albumin/globulin ratio, which was a parameter of systemic inflammatory reactions, the effect was more remarkable in therapeutic administration than in preventive one. This suggests that CN-100 is suitable for clinical application.
以常用的类风湿性关节炎实验模型佐剂性关节炎大鼠为对象,将2-(10,11-二氢-10-氧代二苯并[b,f]硫杂卓-2-基)丙酸(CN-100)与参比药物吲哚美辛和普拉洛芬进行比较,研究其对局部和全身变化的预防和治疗作用。CN-100在预防和治疗方面对佐剂原发性炎症和继发性病变均显示出强效抑制作用。CN-100对足骨破坏也有明显的预防作用,改善了器官重量变化,并促进体重增加。这些作用呈剂量依赖性,5.0mg/kg时的作用分别与1.25mg/kg和2.5mg/kg的吲哚美辛及普拉洛芬的作用几乎相同。CN-100的作用方式与参比化合物相似。虽然CN-100改善了作为全身炎症反应参数的白蛋白/球蛋白比值变化,但治疗给药时的效果比预防给药时更显著。这表明CN-100适合临床应用。