F2 values and -fold induction at highest concentration tested (given in parenthesis) for induction of CYP1A1 and CYP1A2 mRNA in HepaRG cells treated with rifampicin, omeprazole, troglitazone, phenytoin, primaquine, or phenobarbital F2 is the concentration resulting in a 2-fold increase of baseline mRNA levels. EC50 values are presented when achieved. Values are mean ± S.D. of three separate batches of differentiated HepaRG cells.
CYP1A1 mRNA | CYP1A2 mRNA | |||||
|---|---|---|---|---|---|---|
| F2 | -Fold Induction at Highest Concentration | F2 | -Fold Induction at Highest Concentration | |||
| Rifampicin | N.I.a | N.I. | N.I. | N.I. | ||
| Omeprazole | 1.4 ± 0.14b (EC50 = 5.9 ± 1.5b) | 62 ± 13 (40 μM) | 1.0 ± 0.2 | 38 ± 19 (40 μM) | ||
| Troglitazone | N.I. | N.I. | N.I. | N.I. | ||
| Phenytoin | N.I. | N.I. | N.I. | N.I. | ||
| Primaquine | 4.6 ± 3.3 | 7.4 ± 2.2 (40 μM) | 1.7 ± 1.0 | 20 ± 16 (40 μM) | ||
| Phenobarbital | N.I. | N.I. | N.I. | N.I. | ||