COX-1 and COX-2 inhibition in horse blood by phenylbutazone, flunixin, carprofen and meloxicam: An in vitro analysis

被引：118

作者：

Beretta, C ^{[1
]}

Garavaglia, G ^{[1
]}

Cavalli, M ^{[1
]}

机构：

[1] Fac Med Vet, Dept Vet Clin Sci, I-20133 Milan, Italy

来源：

PHARMACOLOGICAL RESEARCH | 2005年 / 52卷 / 04期

关键词：

horse blood cyclooxygenases; NSAIDs; selectivity of inhibition;

D O I：

10.1016/j.phrs.2005.04.004

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：302 / 306

页数：5

共 18 条

[1] In vitro effects of cyclooxygenase inhibitors in whole blood of horses, dogs, and cats [J].