Beside using the knockout models, I need the most commonly used CYP2E1 agonist and antagonist that used for mimic and block CYP2E1 activity, respectively, especially in rat models. Suggestions with published references are highly appreciated.
Inducer - ethanol, isoniazid
Inhibitor - 4-methylpyrazole, disulfuram
(Katzung)
If you mean substrate and inhibitor (enzymes have 'substrates' and 'inhibitors', while receptors have 'agonists' and 'antagonists'), then the 3-hydroxylation of p-nitrophenol, the 6-hydroxylation of chlorzoxazone and the 4-hydroxylation of aniline are all good CYP2E1-selective reactions. By virtue of this fact, each of these substrates is also a good competitive inhibitor of any other CYP2E1-catalyzed reaction. Other CYP2E1-selective inhibitors include diethyldithiocarbamate, clomethiazole and diallyldisulfide.
Please loook at my publications for human models published in Drug Metabolism Reviews 1997 and. 2oo2. I would ruther talko about indicers, inhibitors, and/or activators and not about agonists or antagonists of the enzyme activities.
Thanks alot @ Denis M Grant & Slobodan Peter Rendic, I'm appreciated
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