Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX‐2 inhibitor

DFU (5,5‐dimethyl‐3‐(3‐fluorophenyl)‐4‐(4‐methylsulphonyl)phenyl‐2(5H)‐furanone) was identified as a novel orally active and highly selective cyclo‐oxygenase‐2 (COX‐2) inhibitor. In CHO cells stably transfected with human COX isozymes, DFU inhibited the arachidonic acid‐dependent production of prost...

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Veröffentlicht in:	British journal of pharmacology 1997-05, Vol.121 (1), p.105-117
Hauptverfasser:	Riendeau, D, Percival, M D, Boyce, S, Brideau, C, Charleson, S, Cromlish, W, Ethier, D, Evans, J, Falgueyret, J ‐P, Ford‐Hutchinson, A W, Gordon, R, Greig, G, Gresser, M, Guay, J, Kargman, S, Léger, S, Mancini, J A, O'Neill, G, Ouellet, M, Rodger, I W, Thérien, M, Wang, Z, Webb, J K, Wong, E, Xu, L, Young, R N, Zamboni, R, Prasit, P, Chan, C ‐C
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - pharmacology Anti-Inflammatory Agents, Non-Steroidal - therapeutic use Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents CHO Cells - cytology CHO Cells - drug effects COX‐1 COX‐2 Cricetinae Cyclooxygenase 1 Cyclooxygenase 2 Cyclooxygenase 2 Inhibitors Cyclooxygenase Inhibitors - administration & dosage Cyclooxygenase Inhibitors - pharmacology Cyclooxygenase Inhibitors - therapeutic use cyclo‐oxygenase Digestive System - drug effects Dinoprostone - biosynthesis Dose-Response Relationship, Drug Edema - drug therapy Fever - drug therapy Furans - administration & dosage Furans - pharmacology Furans - therapeutic use Humans Hyperalgesia - drug therapy Indomethacin - toxicity inflammation Isoenzymes - blood Isoenzymes - drug effects Isoenzymes - metabolism Lipopolysaccharides - toxicity Male Medical sciences Membrane Proteins nonsteroidal anti‐inflammatory drugs Peroxidases - antagonists & inhibitors Peroxidases - metabolism Pharmacology. Drug treatments Prostaglandin-Endoperoxide Synthases - blood Prostaglandin-Endoperoxide Synthases - drug effects Prostaglandin-Endoperoxide Synthases - metabolism Prostaglandins Rats Rats, Sprague-Dawley Recombinant Proteins - metabolism Saimiri Structure-Activity Relationship Thromboxane B2 - biosynthesis Transfection
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