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Chemical Compound Review

Flosulida     N-[6-(2,4-difluorophenoxy)-1- oxo-2,3...

Synonyms: Flosulide, Flosulidum, CHEMBL147580, SureCN195509, CGP-28238, ...
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Disease relevance of Cgp 28238


High impact information on Cgp 28238

  • Available experimental and clinical data of selective COX-2 inhibitors, including flosulide, celecoxib or rofecoxib, suggest improved gastric tolerance as compared to conventional, non-selective NSAIDs [5].
  • There was concentration-dependent (IC50 = 107 +/- 55 nM) and ultimately complete inhibition of PGE2 generation by flosulide [6].
  • High-dose flosulide induced a decrease in glomerular prostanoid production possibly because of COX-1 inhibition [1].
  • High-dose flosulide treatment reduced renal prostaglandin production and caused a marked decline in COX-1 and COX-2 protein expression [1].
  • However, a 250-fold molar excess of flosulide could not displace labeled FMLP from the receptor [7].

Biological context of Cgp 28238


Anatomical context of Cgp 28238


Associations of Cgp 28238 with other chemical compounds

  • HN-56249 surpassed the COX-2 selectivities of the COX-2 selective inhibitors 3-cyclohexyloxy-4-methylsulfonylamino-nitrobenzene (NS-398) and 6-(2,4-difluorophenoxy)-5-methyl-sulfonylamino-1-indanone (flosulide) in the intact cell assays by eight- and threefold, respectively, and in the whole blood assays by approximately 40-fold [11].
  • The TPA-induced increase in 6-keto-PGF1 alpha was greatly inhibited by all COX-2 inhibitors while LTB4 was potentiated by both flosulide and L-745,337 [12].
  • The selective COX-2 inhibitor, flosulide, is significantly better tolerated and causes less gastric mucosal damage than naproxen when given for two weeks [13].
  • Fourteen days after inoculation, AA rats were selected and treated orally every day for two weeks with the selective COX-2 inhibitor, flosulide, or the COX-1-COX-2 inhibitor, indomethacin [10].

Gene context of Cgp 28238

  • CONCLUSIONS: Under the influence of flosulide, a highly COX-2-selective inhibitor, we observed an antiproteinuric drug effect [1].
  • Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class [14].
  • The topical effects of cyclooxygenase-2 (COX-2)-selective inhibitors, flosulide (CGP 28238), L-745,337 and SC-57,666 were examined in AA- and TPA-induced ear dermal inflammation in the mouse [12].
  • Myeloperoxidase (MPO) levels were lowered by flosulide and L-745,337 but not by SC-57,666 [12].

Analytical, diagnostic and therapeutic context of Cgp 28238


  1. Effect of flosulide, a selective cyclooxygenase 2 inhibitor, on passive heymann nephritis in the rat. Blume, C., Heise, G., Mühlfeld, A., Bach, D., Schrör, K., Gerhardz, C.D., Grabensee, B., Heering, P. Kidney Int. (1999) [Pubmed]
  2. Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives. Li, C.S., Black, W.C., Chan, C.C., Ford-Hutchinson, A.W., Gauthier, J.Y., Gordon, R., Guay, D., Kargman, S., Lau, C.K., Mancini, J. J. Med. Chem. (1995) [Pubmed]
  3. The potential role of spinal cord cyclooxygenase-2 in the development of Freund's complete adjuvant-induced changes in hyperalgesia and allodynia. Hay, C.H., Trevethick, M.A., Wheeldon, A., Bowers, J.S., de Belleroche, J.S. Neuroscience (1997) [Pubmed]
  4. A randomized, double-blind, crossover comparative endoscopy study on the gastroduodenal tolerability of a highly specific cyclooxygenase-2 inhibitor, flosulide, and naproxen. Bjarnason, I., Macpherson, A., Rotman, H., Schupp, J., Hayllar, J. Scand. J. Gastroenterol. (1997) [Pubmed]
  5. Cyclooxygenase-2 inhibition and side-effects of non-steroidal anti-inflammatory drugs in the gastrointestinal tract. Meyer-Kirchrath, J., Schrör, K. Current medicinal chemistry. (2000) [Pubmed]
  6. Constitutive cyclooxygenase-2 expression in healthy human and rabbit gastric mucosa. Zimmermann, K.C., Sarbia, M., Schrör, K., Weber, A.A. Mol. Pharmacol. (1998) [Pubmed]
  7. Influence of the anti-inflammatory compound flosulide on granulocyte function. Zimmerli, W., Sansano, S., Wiesenberg-Böttcher, I. Biochem. Pharmacol. (1991) [Pubmed]
  8. Acute effects of the anti-inflammatory cyclooxygenase-2 selective inhibitor, flosulide, on renal plasma flow and glomerular filtration rate in rats. Turull, A., Piera, C., Queralt, J. Inflammation (2001) [Pubmed]
  9. Renal and endocrine effects of flosulide, after single and repeated administration to healthy volunteers. Brunel, P., Hornych, A., Guyene, T.T., Sioufi, A., Turri, M., Ménard, J. Eur. J. Clin. Pharmacol. (1995) [Pubmed]
  10. Changes in prostaglandin E2 (PGE2) levels in paw exudate, stomach and kidney of arthritic rats: effects of flosulide. Turull, A., Queralt, J. Prostaglandins Other Lipid Mediat. (2001) [Pubmed]
  11. Pharmacology of a selective cyclooxygenase-2 inhibitor, HN-56249: a novel compound exhibiting a marked preference for the human enzyme in intact cells. Berg, J., Fellier, H., Christoph, T., Kremminger, P., Hartmann, M., Blaschke, H., Rovensky, F., Towart, R., Stimmeder, D. Naunyn Schmiedebergs Arch. Pharmacol. (2000) [Pubmed]
  12. Effect of topically applied cyclooxygenase-2-selective inhibitors on arachidonic acid- and tetradecanoylphorbol acetate-induced dermal inflammation in the mouse. Puigneró, V., Queralt, J. Inflammation (1997) [Pubmed]
  13. Gastroduodenal tolerability of highly specific cyclo-oxygenase-2 inhibitor. Hayllar, J., Bjarnason, I. The Italian journal of gastroenterology. (1996) [Pubmed]
  14. Substituted heterocyclic analogs as selective COX-2 inhibitors in the flosulide class. Ouimet, N., Chan, C.C., Charleson, S., Claveau, D., Gordon, R., Guay, D., Li, C.S., Ouellet, M., Percival, D.M., Riendeau, D., Wong, E., Zamboni, R., Prasit, P. Bioorg. Med. Chem. Lett. (1999) [Pubmed]
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