TABLE 1

Inhibition of CYP2B6-catalyzed bupropion hydroxylation by various substances in human liver microsomes


Inhibitor

IC50

Inhibition (% of Control) at the Highest Concentration Used
μM
Ticlopidine 0.32 100 (1)
ThioTEPA 1.75 100 (100)
Tranylcypromine 3.1 90 (100)
Ketoconazole 3.5 70 (100)
Metyrapone 4.14 100(1000)
Xanthate C8 6.93 100(1000)
Benzyl-isothiocyanate 8.59 100 (100)
Retinol 17.0 70 (100)
Deramciclane 63.5 58 (100)
Troglitazone 88.2 55 (100)
Ethinylestradiol
100
50 (100)