双氯芬酸 化学药品说明书双氯芬酸|药物应用信息双氯芬酸缓释胶囊
双氯芬酸的作用机理为抑制环氧化酶活性,从而阻断花生四烯酸向前列腺素的转化生成,因前列腺素为引起疼痛、发烧及发炎等之现象的主要因子。
Human COX-2
1.3 nM (IC 50 , in CHO cells)
Human COX-1
4 nM (IC 50 , in CHO cells)
Ovine COX-2
0.84 μM (IC 50 )
Ovine COX-1
5.1 μM (IC 50 )
Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC 50 of 7±3 nM. Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner. Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3.
Cell Viability Assay
Western Blot Analysis
Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal 51 Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days. Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats.