Table 1

Derivation of RAFs and relative liver abundance of cDNA-expressed CYP

RAFs Determined on Site1-aManufacturer's RAFs1-bImmunoquantified CYP Liver Content
MethodRAFMethodRAFReferenceFactor1-c
CYP1A2Phenacetin-O-deethylation (100 μM)346  (232)Phenacetin-O-deethylation (200 μM)513 Shimada et al., 1994 42
CYP2C8Paclitaxel-6α-hydroxylation (10 μM)45  (22)Paclitaxel-6α-hydroxylation (10 μM)115 Shimada et al., 1994 (total CYP2C)/Lasker et al., 1998 (ratio 2C8:2C9:2C19)6
CYP2C9Tolbutamide-methylhydroxylation (600 μM)30  (12)Diclofenac-4′-hydroxylation (200 μM)71 Shimada et al., 1994 (total CYP2C)/Lasker et al., 1998 (ratio 2C8:2C9:2C19)45
CYP2D6Dextromethorphan-O-demethylation (10 μM)34  (11)Bufuralol-1′-hydroxylation (25 μM)28 Shimada et al., 1994 5
CYP3A4Triazolam-4-hydroxylation (750 μM)125  (61)Testosterone-6β-hydroxylation (200 μM)311 Shimada et al., 1994 (CYP3A)96
  • 1-a  RAFs determined for the same 10 human liver microsomal preparations used for mirtazapine biotransformation studies [mean (S.D.), pmol of CYP/mg of protein].

  • 1-b  RAFs derived from activity data provided by Gentest Corp. (activity of pooled HLM from manufacturer of the rCYP/activity of the lot of recombinant CYP actually used) (pmol of CYP/mg of protein).

  • 1-c  Human liver content of the respective CYP according to the references (pmol of CYP/mg of protein).