Reaction: Diclofenac to 1 product

Reaction
Reaction type
3'-hydroxylation
Direction
Major circulating metabolite?
No
Spontaneous?
No
Activity
unknown
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
  2. Davies NM, Anderson KE: Clinical pharmacokinetics of diclofenac. Therapeutic insights and pitfalls. Clin Pharmacokinet. 1997 Sep;33(3):184-213. doi: 10.2165/00003088-199733030-00003. [Article]
  3. Bort R, Mace K, Boobis A, Gomez-Lechon MJ, Pfeifer A, Castell J: Hepatic metabolism of diclofenac: role of human CYP in the minor oxidative pathways. Biochem Pharmacol. 1999 Sep 1;58(5):787-96. [Article]
  4. Yan Z, Li J, Huebert N, Caldwell GW, Du Y, Zhong H: Detection of a novel reactive metabolite of diclofenac: evidence for CYP2C9-mediated bioactivation via arene oxides. Drug Metab Dispos. 2005 Jun;33(6):706-13. doi: 10.1124/dmd.104.003095. Epub 2005 Mar 11. [Article]
  5. Boerma JS, Vermeulen NP, Commandeur JN: One-electron oxidation of diclofenac by human cytochrome P450s as a potential bioactivation mechanism for formation of 2'-(glutathion-S-yl)-deschloro-diclofenac. Chem Biol Interact. 2014 Jan 25;207:32-40. doi: 10.1016/j.cbi.2013.11.001. Epub 2013 Nov 15. [Article]
  6. Kamimura H, Ito S, Nozawa K, Nakamura S, Chijiwa H, Nagatsuka S, Kuronuma M, Ohnishi Y, Suemizu H, Ninomiya S: Formation of the accumulative human metabolite and human-specific glutathione conjugate of diclofenac in TK-NOG chimeric mice with humanized livers. Drug Metab Dispos. 2015 Mar;43(3):309-16. doi: 10.1124/dmd.114.061689. Epub 2014 Dec 11. [Article]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
Cytochrome P450 2C9Not AvailableNot Availableimplied