Inactivation Assay Components | Activity |
---|---|
% of Control3-a | |
HL microsomes (4 mg/ml) + NADPH (1 mM) (control) | 100 (3.0) |
HL microsomes + NADPH+ SCH 66712 (16 μM) | 19 (1.3) |
HL microsomes + NADPH + SCH 66712 (16 μM) + Quinidine (200 nM) | 40 (3.0) |
Supersomes (20 pmol of CYP2D6) + NADPH (control) | 100 (4.0) |
Supersomes + NADPH+ SCH 66712 (4 μM) | 8 (4.0) |
Supersomes + NADPH + SCH 66712 (4 μM) + Quinidine (200 nM) | 40 (31) |
Human liver microsomes or Supersomes were preincubated for 10 min at 37°C (inactivation assay). The reaction mixtures were diluted 10-fold, and the dextromethorphan O-demethylase activity was determined.
↵3-a Data are means (%CV) of three separate determinations.