Table 1. Compounds Activating One or More Nuclear Receptors.
| Agent | Concentration | Nuclear Receptor (Fold Activationa) | |||
|---|---|---|---|---|---|
| μM | Canine PXR | Canine CAR3 | Rat PXR | Rat CAR3 | |
| Dexamethasone | 10 | -b | - | 60.9 ± 8.4 | - |
| 100 | - | - | 59.9 ± 12.7 | - | |
| ANF | 10 | - | - | - | 3.4 ± 0.8c |
| Forskolin | 10 | 5.6 ± 1.4 | - | 5.8 ± 0.5 | - |
| Troleandomycin | 100 | 26.8± 3.7 | - | - | - |
| Rifampicin | 10 | 11.3 ± 1.4 | - | - | - |
| Felodipine | 30 | 8.0 ± 1.5 | - | 11.5 ± 1.3 | - |
| Omeprazole | 100 | 9.6 ± 1.3 | - | 9.8 ± 0.9 | - |
| CITCO | 10 | 5.4 ± 2.1 | - | - | - |
| Ritanovir | 10 | 9.8 ± 0.8 | - | 5.1 ± 1.1 | - |
| Efavirenz | 10 | - | - | 7.5 ± 2.3 | 3.9 ± 0.6c 7.4 ± 3.3d |
| Artemisinin | 50 | - | 10.5 ± 0.5c 7.3 ± 1.8d | - | 7.1 ± 0.4c 10.5 ± 2.2d |
| Pregnenolone 16α carbonitrile | 1 | - | - | 11.7 ± 0.6 | - |
| 10 | - | - | 10.4 ± 0.7 | - | |
| DEHP | 10 | - | 4.3 ± 0.8c | - | - |
| Clotrimazole | 10 | 15.6 ± 0.07 | 3.1 ± 0.4c 3.1 ± 0.4d | 12.5 ± 0.9 | 13.7 ± 0.8c 26.9 ± 1.3d |
| Miconazole | 10 | - | - | 9.1 ± 1.2 | 5.1 ± 1.0c 5.9 ± 1.9d |
| SR12813 | 10 | 60.1 ± 3.1 | 3.1 ± 0.7d | 6.1 ± 0.6 | - |
a Values represent the fold activation above DMSO treated cells normalized to the cell number in each well. Each value is the mean of 3 or more determinations and is expressed as fold increase ± SE at p < 0.01.
b Indicates that there was no statistically significant difference from control (DMSO treated cells) at p < 0.01.
c Fold activation of CAR3 in the presence of the CYP2B6 promoter and enhancer
d Fold activation of CAR3 in the presence of the CYP3A4 promoter and enhancer