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Chemical Compound Review

AC1LD8JN     5-hydroxy-4-(4- methylsulfonylphenyl)-3...

Synonyms: 5-OH-rofecoxib
 
 
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High impact information on 5-OH-rofecoxib

 

Anatomical context of 5-OH-rofecoxib

  • In contrast to microsomes, the oxidation of rofecoxib to 5-hydroxyrofecoxib by S9 fractions followed two pathways, one NADPH-dependent and one NAD+-dependent (non-cytochrome P450), with the latter accounting for about 40% of total activity [2].
 

Gene context of 5-OH-rofecoxib

  • Eight individual cDNA-expressed human UGT isozymes (1A1, 1A3, 1A4, 1A6, 1A8, 1A9, 2B7, and 2B15) were evaluated for glucuronidation of 5-hydroxyrofecoxib [1].

References

  1. Involvement of human UGT2B7 and 2B15 in rofecoxib metabolism. Zhang, J.Y., Zhan, J., Cook, C.S., Ings, R.M., Breau, A.P. Drug Metab. Dispos. (2003) [Pubmed]
  2. Metabolism of rofecoxib in vitro using human liver subcellular fractions. Slaughter, D., Takenaga, N., Lu, P., Assang, C., Walsh, D.J., Arison, B.H., Cui, D., Halpin, R.A., Geer, L.A., Vyas, K.P., Baillie, T.A. Drug Metab. Dispos. (2003) [Pubmed]
  3. Mechanistic studies on the reversible metabolism of rofecoxib to 5-hydroxyrofecoxib in the rat: evidence for transient ring opening of a substituted 2-furanone derivative using stable isotope-labeling techniques. Baillie, T.A., Halpin, R.A., Matuszewski, B.K., Geer, L.A., Chavez-Eng, C.M., Dean, D., Braun, M., Doss, G., Jones, A., Marks, T., Melillo, D., Vyas, K.P. Drug Metab. Dispos. (2001) [Pubmed]
 
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