A High Level of Cyclooxygenase-2 Inhibitor Selectivity is Associated with a Reduced Interference of Platelet Cyclooxygenase-1 Inactivation by Aspirin

• Published in: Proceedings of the National Academy of Sciences - PNAS Vol. 98; no. 25; pp. 14583 - 14588
• Main Authors: Ouellet, Marc, Riendeau, Denis, Percival, M. David
• Format: Journal Article
• Language: English
• Published: United States National Academy of Sciences 04.12.2001; National Acad Sciences; The National Academy of Sciences
• Subjects: Acetylation; Active sites; Animals; Anti-inflammatory agents; Anticoagulants; Aspirin; Aspirin - pharmacology; Biological Sciences; Blood Platelets - drug effects; Blood Platelets - enzymology; Calcium; Celecoxib; Cellular biology; Cyclooxygenase 1; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Cyclooxygenase inhibitors; Cyclooxygenase Inhibitors - pharmacology; Dosage; Drug therapy; Etoricoxib; Gels; Humans; Ibuprofen - pharmacology; In Vitro Techniques; Inactivation; Inhibitory concentration 50; Isoenzymes - antagonists & inhibitors; Isoenzymes - blood; Isoenzymes - chemistry; Isoxazoles - pharmacology; Lactones - pharmacology; Medical research; Membrane Proteins; Nonsteroidal anti-inflammatory drugs; Platelets; Prostaglandin-Endoperoxide Synthases - blood; Prostaglandin-Endoperoxide Synthases - chemistry; Pyrazoles; Pyridines - pharmacology; rofecoxib; Sheep; Sulfonamides - pharmacology; Sulfones - pharmacology; Titration

Both nonsteroidal anti-inflammatory drugs, such as ibuprofen, and the prototypical selective cyclooxygenase (Cox)-2 inhibitors DuP-697 and NS-398 block the inhibition of Cox-1 by aspirin in vitro. However, clinical studies have shown that the Cox-2 selective drugs (or coxibs) rofecoxib and etoricoxi...