Valdecoxib
Valdecoxib is a COX inhibitor specific for COX-2; it also inhibits carbonic anhydrase. Valdecoxib is a non-steroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory and analgesic activities. In addition to its mediation of inflammatory signaling, valdecoxib also activates cannabinoid 1 (CB1) receptors in vivo, modulating glutamate signaling and GABA release. Valdecoxib has been removed from clinical use due to increased risk of thrombotic effects.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18978700
| Cas No. |
181695-72-7 |
|---|---|
| Purity |
≥98% |
| Formula |
C16H14N2O3S |
| Formula Wt. |
314.36 |
| IUPAC Name |
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzenesulfonamide |
| Melting Point |
162-164℃ |
| Solubility |
Water 0.5 mg/ml |
| Appearance |
White Crystal Powder |
Atukorala I, Hunter DJ. Valdecoxib : the rise and fall of a COX-2 inhibitor. Expert Opin Pharmacother. 2013 Jun;14(8):1077-86. PMID: 23517091.
Schröder H, Höllt V, Becker A. Parecoxib and its metabolite valdecoxib directly interact with cannabinoid binding sites in CB1-expressing HEK 293 cells and rat brain tissue. Neurochem Int. 2011 Jan;58(1):9-13. PMID: 21073910.
Roumie CL, Choma NN, Kaltenbach L, et al. Non-aspirin NSAIDs, cyclooxygenase-2 inhibitors and risk for cardiovascular events-stroke, acute myocardial infarction, and death from coronary heart disease. Pharmacoepidemiol Drug Saf. 2009 Nov;18(11):1053-63. PMID: 19637402.
Benetello V, Sakamoto FC, Giglio FP, et al. The selective and non-selective cyclooxygenase inhibitors valdecoxib and piroxicam induce the same postoperative analgesia and control of trismus and swelling after lower third molar removal. Braz J Med Biol Res. 2007 Aug;40(8):1133-40. PMID: 17665051.
Dogné JM, Thiry A, Pratico D, et al. Dual carbonic anhydrase–cyclooxygenase-2 inhibitors. Curr Top Med Chem. 2007;7(9):885-91. PMID: 17504133.
Walker MC, Kurumbail RG, Kiefer JR, et al. A three-step kinetic mechanism for selective inhibition of cyclo-oxygenase-2 by diarylheterocyclic inhibitors. Biochem J. 2001 Aug 1;357(Pt 3):709-18. PMID: 11463341.
