Table 4

Ki values for fluoxetine, ezlopitant, imipramine, and quinidine on CYP2D6 catalyzed bufuralol 1′-hydroxylase activity based on total (nominal) and free inhibitor and substrate concentrations

Microsomal Protein ConcentrationFluoxetineEzlopitantImipramineQuinidine
NominalFreeNominalFreeNominalFreeNominalFree
μM
Control (0.0088 mg/ml)0.0480.0330.0340.00160.390.300.00100.00078
 0.2 mg/ml0.160.0250.220.00930.710.330.00160.0012
 2.0 mg/ml1.70.0431.30.00394.10.950.00380.0017