SCHOOL OF MEDICINE

Department of Medicine

Clinical Pharmacology

2E1 REFERENCES

 2E1 SUBSTRATES: 

ACETAMINOPHEN=>NAPQI
Acetaminophen activation by human liver cytochrome P450 2E1 and 1A2. [ PMID 2729995 ]
Raucy JE, Lasker JM, Lieber CS, Black M.
Arch Biochem Biophys 1989;271(2):270-283.

ANILINE
Requirements for cytochrome b5 in the oxidation of 7-ethoxycoumarin, chlorzoxazone, aniline, and N-nitrosodimethylamine by recombinant cytochrome P450 2E1 and by human liver microsomes. [ PMID 8694855 ]
Yamazaki H, Nakano M, Gillam EM, Bell LC, Guengerich FP, Shimada T.
Biochem Pharmacol 1996 Jul 26;52(2):301-309.

BENZENE
Benzene poisoning, a risk factor for hematological malignancy, is associated with the NQO1 609C-->T mutation and rapid fractional excretion of chlorzoxazone. [ PMID 9230185 ]
Rothman N, Smith MT, Hayes RB, Traver RD, Hoener B, Campleman S, Li GL, Dosemeci M, Linet M, Zhang L, Xi L, Wacholder S, Lu W, Meyer KB, Titenko-Holland N, Stewart JT, Yin S, Ross D.
Cancer Res 1997 Jul 15;57(14):2839-2842.

CHLORZOXAZONE
Hydroxylation of chlorzoxazone as a specific probe for human liver cytochrome P4502E1. [ PMID 2103328 ]
Peter R, Böcker R, Beaune PH, Iwasaki PH,Guengerich FP, Yang CS.
Chem Res Toxicol 1990;3:566-573.

ENFLURANE
Stereoselective metabolism of enflurane by human liver cytochrome P450 2E1. [ PMID 8689955 ]
Garton KJ, Yuen P, Meinwald J, Thummel KE, Kharasch ED.
Drug Metab Dispos 1995 Dec;23(12):1426-1430.

Clinical enflurane metabolism by cytochrome P450 2E1. [ PMID 8162670 ]
Kharasch ED, Thummel KE, Mautz D, Bosse S.
Clin Pharmacol Ther 1994 Apr;55(4):434-440.

ETHANOL

HALOTHANE

Cytochrome P450 2E1 is the principal catalyst of human oxidative halothane metabolism in vitro. [ PMID 9103523 ]
Spracklin DK, Hankins DC, Fisher JM, Thummel KE, Kharasch ED.
J Pharmacol Exp Ther 1997 Apr;281(1):400-11.

Interindividual variability in P450-dependent generation of neoantigens in halothane hepatitis. [ PMID 9877205 ]
Eliasson E, Gardner I, Hume-Smith H, de Waziers I, Beaune P, Kenna JG.
Chem Biol Interact 1998 Nov 6;116(1-2):123-41.

ISOFLURANE

METHOXYFLURANE

N,N-DIMETHYLFORMAMIDE
Investigation of the mechanistic basis of N,N-dimethylformamide toxicity. Metabolism of N,N-dimethylformamide and its deuterated isotopomers by cytochrome P450 2E1. [ PMID 8477011 ]
Mraz J, Jheeta P, Gescher A, Hyland R, Thummel K, Threadgill MD.
Chem Res Toxicol 1993 Mar;6(2):197-207.

SEVOFLURANE

THEOPHYLLINE

Dose-dependent inhibition of theophylline metabolism by disulfiram in recovering alcoholics. [ PMID 2721103 ]
Loi CM, Day JD, Jue SG, Bush ED, Costello P, Dewey LV, Vestal RE.
Clin Pharmacol Ther 1989:45(5):476-486.

 


 2E1 INHIBITORS: 

DIETHYL-DITHIOCARBAMATE
Role of human cytochrome P450 2E1 in the oxidation of many low molecular weight cancer suspects. [ PMID 1664256 ]
Guengerich FP, Kim DH, Iwasaki M.
Chem Res Toxicol 1991; 4:168-179.

DISULFIRAM
Single dose disulfiram inhibition of chlorzoxazone metabolism: A clinical probe for P450 2E1. [ PMID 8513656 ]
Kharasch ED, Thummel KE, Mhyre J, Lillibridge JH.
Clin Pharmacol Ther 1993;53:643-650.


 2E1 INDUCERS: 

ETHANOL

ISONIAZID
Inhibition and induction of cytochrome P4502E1-catalyzed oxidation by isoniazid in humans. [ PMID 8354023 ]
Zand R, Nelson SD, Slattery JT, Thummel KE, Kalhorn TF, Adams SP, Wright JM Clin Pharmacol Ther 1993;54(2):142-149