78213-16-8
78213-16-8 结构式
基本信息
双氯芬酸二乙胺
2-((2,6-二氯苯基)氨基)苯乙酸二乙胺盐
双氯芬酸二乙胺盐
DICLOFENAC DIETHYLAMINE
n-ethylethanamine 2-[(2,6-dichlorophenyl)amino]benzeneacetate
2-[(2,6-dichlorophenyl)amino]-benzeneacetic acid compd. with n-ethylethanamine
物理化学性质
常见问题列表
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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 diethylamine抗炎，退热，和镇痛作用的主要作用机制被认为是通过抑制环氧合酶(COX)，从而抑制前列腺素合成。它通过抑制细菌DNA合成发挥出抑菌活性。COX的抑制也会减少胃上皮细胞中的前列腺素，使其对胃酸的腐蚀更敏感。这也是diclofenac diethylamine的主要副作用。Diclofenac diethylamine阻断COX2-同工酶(大约10倍)，具有低到中度的选择性，因此，diclofenac diethylamine造成的胃肠疾病的发生率比消炎痛和阿司匹林低。
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.
| Animal Model: | Male Sprague-Dawley rats (150±200 g) |
| Dosage: | 3 mg/kg |
| Administration: | Oral administration, b.i.d., for 5 days |
| Result: | Resulted in a significant increase in faecal 51 Cr excretion. |
| Animal Model: | Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model |
| Dosage: | 10 mg/kg |
| Administration: | Administered via oral route just prior to induction of inflammation |
| Result: | Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h). |