An internal standard for the quantification of nimesulide
Nimesulide-d5 is intended for use as an internal standard for the quantification of nimesulide by GC- or LC-MS. Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) and COX-2 inhibitor (IC50s = 1.27 and 0.03 ?M for the human and ovine enzymes, respectively).1,2 It is selective for COX-2 over COX-1 (IC50s = 70 and 22 ?M for the human and ovine enzymes, respectively). Nimesulide also inhibits sodium-dependent neutral amino acid transporter (B0AT1) with an IC50 value of 23 ?M for the rat kidney transporter.3 It inhibits infection-induced increases in brain prostaglandin E2 levels, as well as reduces pyresis (ED50 = 0.3 mg/kg), in yeast-infected rats.4 Nimesulide (2.9 mg/kg) inhibits formalin-induced hindpaw thermal hyperalgesia in rats.5
1.Johnson, J.L., Wimsatt, J., Buckel, S.D., et al.Purification and characterization of prostaglandin H synthase-2 from sheep placental cotyledonsArch. Biochem. Biophys.324(1)26-34(1995) 2.Barnett, J., Chow, J., Ives, D., et al.Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus systemBiochim. Biophys. Acta1209(1)130-139(1994) 3.Pochini, L., Seidita, A., Sensi, C., et al.Nimesulide binding site in the B0AT1 (SLC6A19) amino acid transporter. Mechanism of inhibition revealed by proteoliposome transport assay and molecular modellingBiochem. Pharmacol.89(3)422-430(2014) 4.Taniguchi, Y., Yokoyama, K., Inui, K., et al.Inhibition of brain cyclooxygenase-2 activity and the antipyretic action of nimesulideEur. J. Pharmacol.330221-229(1997) 5.Bianchi, M., and Broggini, M.Anti-hyperalgesic effects of nimesulide: Studies in rats and humansInt. J. Clin. Pract. Suppl.57(128)11-19(2002)
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