Acemetacin 是一种非甾体抗炎类的化合物。

Acemetacin is a carboxymethyl ester of indometacin. It is a potent non-steroidal anti-inflammatory drug, derived from the indol-3-acetic acid, whose activity is thought to be mainly through its active metabolite indomethacin. In clinical trials, acemetacin exhibits a better gastric tolerability compared to its active metabolite indometacin.

在COX-2和NOS抑制剂预处理的大鼠中,尽管COX活性被显著抑制,但与吲哚美辛相比,Acemetacin能显著减少胃肠损伤.

Acemetacin通过抑制PG合成发挥抗炎作用。在发炎的滑膜组织中,Acemetacin（10 μM）阻止PGE2的释放。在体外Acemetacin对关节滑膜的前列腺素E2释放具有抑制作用。在胃黏膜孵化过程中,Acemetacin浓度依赖性抑制PGE积累的效果不如吲哚美辛,其对胃6-酮-PGF1α和血栓素B2的减少作用也比吲哚美辛低。

53164-05-9

C21H18ClNO6

415.83

TVX 1322;阿西美辛;K-708

H2O:<1 mgml
DMSO:77 mg/mL (185.2 mM)
Ethanol:54 mg/mL (129.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years