Interdonor variability in induction of CYP2B6 activity in primary human hepatocyte cultures Rates of bupropion hydroxylation were determined in duplicate in microsomes isolated from three human hepatocyte preparations (HL-N95, HL-N98, HL-N100) treated daily for 3 days with the indicated concentrations of tests compounds. Bupropion hydroxylase activities in control samples were 23, 16, and 45 pmol/min/mg protein for HL-N95, HL-N98, and HL-N100, respectively. Values in the table represent fold induction over control activities.
Compound | HL-N95 | HL-N98 | HL-N100 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 2 μM | 10 μM | 20 μM | 2 μM | 10 μM | 20 μM | 2 μM | 10 μM | 20 μM | |||||||
| CMZ | N.A. | 2.7 | 3.7 | 1.3 | 2.5 | 4.4 | 1.4 | 2.5 | 4.4 | ||||||
| CLZ | 2.1 | 12.8 | 20.4 | 1.6 | 4.0 | 7.1 | 2.3 | 7.7 | 18.3 | ||||||
| DEX | 1.7 | 1.3 | 1.4 | 0.9 | 1.2 | 1.3 | 1.3 | 1.5 | 1.8 | ||||||
| DTBA | 1.2 | 1.5 | 1.7 | 1.3 | 1.6 | 2.3 | 1.4 | 1.8 | 2.2 | ||||||
| MTX | 0.9 | 0.8 | 0.9 | 0.8 | 0.9 | 0.9 | 1.0 | 0.9 | 1.0 | ||||||
| PAX | 0.9 | 0.8 | 0.8 | 0.9 | 1.6 | 1.5 | 1.2 | 1.3 | 1.0 | ||||||
| PBa | 2.0 | 4.0 | 5.9 | 3.2 | 5.9 | 6.9 | 3.0 | 4.3 | 6.2 | ||||||
| PHN | 2.9 | 4.3 | 5.6 | 3.5 | 7.1 | 9.5 | 2.6 | 8.0 | 9.1 | ||||||
| PROB | 0.8 | 1.0 | 1.1 | 1.1 | 0.9 | 1.0 | 1.0 | 1.1 | 1.1 | ||||||
| RIF | 4.3 | 5.7 | 9.1 | 3.3 | 4.9 | 7.2 | 4.1 | 5.6 | 9.8 | ||||||
| RIT | 4.0 | 6.6 | 7.1 | 2.3 | 4.1 | 3.7 | 1.9 | 6.4 | 5.3 | ||||||
| SDM | 1.0 | 1.1 | 1.1 | 1.0 | 1.2 | 1.3 | 1.0 | 1.0 | 0.9 | ||||||
| SPZ | 0.7 | 0.8 | 1.4 | 1.1 | 1.5 | 2.2 | 1.0 | 1.1 | 1.6 | ||||||
| TAO | 0.9 | 1.4 | 1.5 | 0.9 | 1.0 | 1.4 | 1.0 | 1.1 | 1.1 | ||||||
N.A., microsomal sample not available for analysis.
↵ a Treatment concentrations for PB were 50, 150, and 250 μM