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

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 IC 50 indicated that meloxicam and carprofen are more selective inhibitors of COX-2 than phenylb...

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Bibliographic Details
Published in:Pharmacological research 2005-10, Vol.52 (4), p.302-306
Main Authors: Beretta, C., Garavaglia, G., Cavalli, M.
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Carbazoles - pharmacology
Clonixin - analogs & derivatives
Clonixin - pharmacology
Cyclooxygenase Inhibitors - pharmacology
Dinoprostone - blood
Female
Horse blood cyclooxygenases
Horses
In Vitro Techniques
Male
NSAIDs
Phenylbutazone - pharmacology
Selectivity of inhibition
Thiazines - pharmacology
Thiazoles - pharmacology
Thromboxane B2 - blood
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Summary: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 IC 50 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 IC 80, phenylbutazone (+134.4%) and flunixin (+29.7%) had greater COX-2 selectivity than at IC 50, and meloxicam (−41.2%) and carprofen (−12.9%) had lower COX-2 selectivity than at IC 50. We therefore propose that the selectivity of NSAIDs should be assessed at the 80% as well as 50% inhibition level.
ISSN:1043-6618
1096-1186
DOI:10.1016/j.phrs.2005.04.004