Effects of nimesulide and indometacin on COX-1 and COX-2: a comparative study.
Evidence of the existence of two forms of cyclooxygenases and the clinical relevance of COX-2 inhibition led to the development of COX-2 selective NSAIDs. In order to evaluate this selectivity, we have developed and validated an enzymatic method. The precision and reproducibility of the assay were determined and COX-2 selectivity examined using nimesulide and indometacin.
de Leval
X
X
Department of Medicinal Chemistry, C.H.U., University of Liège.
Dogné
J M
JM
Neven
P
P
Labasse
A
A
Delarge
J
J
Reginster
J Y
JY
Henrotin
Y
Y
D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D007213:Indomethacin / Q000494:pharmacology*; D007527:Isoenzymes / Q000378:metabolism*; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism*; D013379:Substrate Specificity; D013449:Sulfonamides / Q000494:pharmacology*
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D013449:Sulfonamides; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases; C012655:nimesulide; D007213:Indomethacin