Kinetic values for induction of the CYP3A4 reporter gene by classical CYP3A4 inducers
| Compound | hGR/hPXR Co-Transfected | Imax(SCE) | EC50 | IA |
|---|---|---|---|---|
| μM | SCE/μM | |||
| Carbemazepine | − | 8.1 ± 0.5 | 1.6 ± 0.6 | 5.0 |
| Carbemazepine | + | 14.1 ± 0.5 | 0.9 ± 0.2 | 16.4 |
| Metyrapone | − | 12.8 ± 1.3 | 6.4 ± 2.8 | 2 |
| Metyrapone | + | 20.9 ± 3.0 | 6.6 ± 4.0 | 3.2 |
| Phenytoin | − | 15.8 ± 1.1 | 17.6 ± 3.3 | 0.9 |
| Phenytoin | + | 27.5 ± 8.7 | 25.1 ± 18.4 | 1.1 |
| Phenobarbital | − | 16.9 ± 2.6 | 17.2 ± 7.3 | 1.0 |
| Phenobarbital | + | 41.3 ± 15.3 | 9.7 ± 12.7 | 4.3 |
| Spironolactone | − | 9.0 ± 0.9 | 9.1 ± 3.4 | 1.0 |
| Spironolactone | + | 13.2 ± 0.7 | 1.1 ± 0.4 | 11.7 |
Imax, EC50, and IA values were derived from concentration response curves for each compound. Four xenobiotic concentrations (1, 10, 30, and 50 μM) were used in the construction of each curve, and each data point was derived from eight replicates in a representative experiment. Imax, EC50, and IA values were only derived if the curve fitting passed strict criteria, as described under Materials and Methods.