Beretta C, Garavaglia G, Cavalli M
Department of Veterinary Clinical Sciences, Faculty of Veterinary Medicine, Via Celoria 10, 20133 Milan, Italy.
Pharmacol Res. 2005 Oct;52(4):302-6. doi: 10.1016/j.phrs.2005.04.004.
We report on the inhibitory activity of the NSAIDs meloxicam, carprofen, phenylbutazone and flunixin, on blood cyclooxygenases in the horse using in vitro enzyme-linked assays. As expected, comparison of IC50 indicated that meloxicam and carprofen are more selective inhibitors of COX-2 than phenylbutazone and flunixin; meloxicam was the most advantageous for horses of four NSAIDs examined. However at IC80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC50, and meloxicam (-41.2%) and carprofen (-12.9%) had lower COX-2 selectivity than at IC50. We therefore propose that the selectivity of NSAIDs should be assessed at the 80% as well as 50% inhibition level.
我们使用体外酶联测定法报告了非甾体抗炎药美洛昔康、卡洛芬、保泰松和氟尼辛对马血液中环氧合酶的抑制活性。正如预期的那样，半数抑制浓度（IC50）的比较表明，与保泰松和氟尼辛相比，美洛昔康和卡洛芬是对环氧合酶-2（COX-2）更具选择性的抑制剂；在所检测的四种非甾体抗炎药中，美洛昔康对马最为有利。然而，在80%抑制浓度（IC80）时，保泰松（+134.4%）和氟尼辛（+29.7%）的COX-2选择性高于IC50时，而美洛昔康（-41.2%）和卡洛芬（-12.9%）的COX-2选择性低于IC50时。因此，我们建议应在80%以及50%抑制水平下评估非甾体抗炎药的选择性。
