雙氯芬酸 化學藥品說明書雙氯芬酸|藥物應(yīng)用信息雙氯芬酸緩釋膠囊
雙氯芬酸的作用機理為抑制環(huán)氧化酶活性，從而阻斷花生四烯酸向前列腺素的轉(zhuǎn)化生成，因前列腺素為引起疼痛、發(fā)燒及發(fā)炎等之現(xiàn)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.