TABLE 1

Inhibition of dextromethorphan O-demethylation by cimetidine and quinidine Pooled human liver microsomes (HLM; 0.5 mg of protein/ml) or recombinant CYP2D6 (rCYP2D6; 2.5 pmol/ml) were incubated with NADPH (1 mM) and various concentrations of DEX and cimetidine or quinidine, and Ki values were determined as described under Materials and Methods. Data are expressed as the mean ± S.D. of three independent determinations.


Inhibitor

Ki

Mode of Inhibition
μM
Cimetidine
   HLM 38 ± 5 competitive
   rCYP2D6 103 ± 17 mixed
nM
Quinidine
   HLM 53 ± 28 competitive
   rCYP2D6
1.3 ± 0.4
competitive