Protein Information

Name CYP1A2
Synonyms CP12; CYP1A2; CYPIA 2; CYPIA2; Cytochrome P450 1A2; Dioxin inducible P3 450; P(3)450; P3 450…

Compound Information

Name sulfoxide
CAS 5-[2-(octylsulfinyl)propyl]-1,3-benzodioxole

Reference List

PubMed Abstract RScore(About this table)
18813404 Cengiz Ustuner M, Degirmenci I, Kiran I, Ozden H, Civi K, Ustuner D, Gunes HV: The protective effects of demethoxyviridine and 1-alpha-hydroxy-demethoxyviridine in the livers of male rats treated with diethylnitrosamine and 2-acetylaminflourene. Saudi Med J. 2008 Sep;29(9):1241-6.


The liver microsomes were prepared from rats and the levels of expression of cytochrome P450 1A2 (CYP1A2) enzymes were determined with western blot technique.
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18385292 Kanebratt KP, Andersson TB: Evaluation of HepaRG cells as an in vitro model for human drug metabolism studies. Drug Metab Dispos. 2008 Jul;36(7):1444-52. Epub 2008 Apr 2.


The metabolism of midazolam, naloxone, and clozapine in HepaRG cells was similar to human hepatocytes, indicating the function of CYP3A4, CYP1A2, and UDP-glucuronosyltransferase enzymes.
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18617602 Grondin M, Hamel F, Sarhan F, Averill-Bates DA: Metabolic activity of cytochrome p450 isoforms in hepatocytes cryopreserved with wheat protein extract. Drug Metab Dispos. 2008 Oct;36(10):2121-9. Epub 2008 Jul 10.


This was achieved by comparing basal and inducible or metabolic activities of isoforms CYP1A1, CYP1A2, CYP2C6, CYP2D2, and CYP3A in rat hepatocytes that were cryopreserved with WPE, relative to fresh cells and those cryopreserved with DMSO.
1(0,0,0,1) Details
20019244 Antherieu S, Chesne C, Li R, Camus S, Lahoz A, Picazo L, Turpeinen M, Tolonen A, Uusitalo J, Guguen-Guillouzo C, Guillouzo A: Stable expression, activity, and inducibility of cytochromes P450 in differentiated HepaRG cells. Drug Metab Dispos. 2010 Mar;38(3):516-25. Epub 2009 Dec 17.


Thus, CYP1A2, CYP2B6, and CYP3A4 were found to accurately respond to their respective prototypical inducers, i.e., omeprazole, phenobarbital, and rifampicin.
1(0,0,0,1) Details
17344341 Kammerer B, Scheible H, Albrecht W, Gleiter CH, Laufer S: Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-( 1-phenylethyl)-amine), a 4-Pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor. Drug Metab Dispos. 2007 Jun;35(6):875-83. Epub 2007 Mar 7.

In addition, pharmacokinetics of ML3403 were evaluated in male and female Wistar rats after oral gavage, showing a fast and high conversion to its active sulfoxide metabolite ML3603.
Incubations were carried out with hepatic microsomes from various species and with recombinant human cytochrome P450 isoenzymes, showing that CYP1A2, CYP2C19, CYP2D6, and CYP3A4 are the prominent enzymes in the metabolism of ML3403.
1(0,0,0,1) Details