Compounds that activate the PXR: a comparison of species and cultured cells
| Cell Type | PXR Species | Compounds That Activate: | Response Element | Reference | ||
|---|---|---|---|---|---|---|
| Most Efficacious | Moderate | Weak/None | ||||
| CV-1 | Mouse | Cyproterone-acetate | Dexamethasone | Clotrimazole | CYP3A1 (DR3)2-tk-CAT | Blumberg et al., 1998 |
| PCN | Spironolactone | Lovastatin | GAL4 constructs | Kliewer et al., 1998 | ||
| RU486 | Pregnenolone | Phenobarbital | (ER6)3-tkCAT | Lehmann et al., 1998 | ||
| 5β-Pregnane-3,20-dione | Progesterone | Rifampicin | Jones et al., 2000 | |||
| 17-OH-Pregnenolone | 17-OH-progesterone | Trans-nonachlor | ||||
| Troglitazone | ||||||
| Corticosterone | ||||||
| Cortisone | ||||||
| 17β-Estradiol | ||||||
| LLC-PK1 pig kidney | Mouse | Cyproterone-acetate | Chlordane | Trans-nonachlor | (CYP3A23)2-tk-CAT | Schuetz et al., 1998 |
| epithelial cells | RU486 | nonplanar PCBs | ||||
| 5β-Pregnane-3,20-dione | Spironolactone | |||||
| Pregnenolone | ||||||
| Progesterone | ||||||
| CV-1 | Rat | Cyproterone-acetate | Dexamethasone | Rifampicin | (ER6)3-tkCAT | Jones et al., 2000 |
| PCN | trans-nonachlor | Troglitazone | (DR3)3-tk CAT | Savas et al., 2000 | ||
| RU486 | Spironolactone | Phenobarbital | ||||
| 5β-Pregnane-3,20-dione | Progesterone | Clotrimazole | ||||
| 17-OH-progesterone | Corticosterone | |||||
| Cortisone | ||||||
| 17β-Estradiol | ||||||
| Pregnenolone | ||||||
| 17-OH-pregnenolone | ||||||
| Primary rat hepatocytes | Rat | Nifedipine | Clotrimazole | CYP3A23 or CYP3A4 | Xie et al., 2000a | |
| PCN | Phenobarbital | promoters—luciferase | ||||
| RU486 | Rifampicin | |||||
| Cortisol | ||||||
| Corticosterone | ||||||
| 17β-Estradiol | ||||||
| CV-1 | Rabbit | Dexamethasone | Clotrimazole | Pregnenolone | CYP3A1 (DR3)2-tk-CAT | Jones et al., 2000 |
| Rifampicin | Cyproterone-acetate | 17-OH-pregnenolone | CYP3A23-(DR3)2-TK Luc | Savas et al., 2000 | ||
| 17-OH-progesterone | PCN | Corticosterone | ||||
| Phenobarbital | Cortisone | |||||
| RU486 | 17β-Estradiol | |||||
| Spironolactone | ||||||
| Trans-nonachlor | ||||||
| Troglitazone | ||||||
| 5β-Pregnane-3,20-dione | ||||||
| Progesterone | ||||||
| CV-1 | Human | Clotrimazole | Lovastatin | Dexamethasone | (ER6)3 tk-CAT | Blumberg et al., 1998 |
| Rifampicin | Nifedipine | Cyproterone-acetate | CYP3A1 (DR3)2-tk-CAT | Lehmann et al., 1998 | ||
| 5β-Pregnane-3,20-dione | Phenobarbital | PCN | Jones et al., 2000 | |||
| RU486 | Spironolactone | |||||
| Trans-nonachlor | Aldosterone | |||||
| Troglitazone | Cortisone | |||||
| Corticosterone | 17-OH-pregnenolone | |||||
| 17β-Estradiol | 17-OH-progesterone | |||||
| Pregnenolone | ||||||
| Progesterone | ||||||
| Caco-2 | Human | Clotrimazole | RU486 | Dexamethasone | GAL4 constructs or CYP3A4 | Bertilsson et al., 1998 |
| Nifedipine | Cortisol | PCN | IR-6 luciferase | |||
| Rifampicin | 17β-Estradiol | Aldosterone | ||||
| 5β-Pregnane-3,20-dione | Pregnenolone | |||||
| Progesterone | ||||||
| 17-OH-pregnenolone | ||||||
| 17-OH-progesterone | ||||||
| Primary rat hepatocytes | Human | Rifampicin | Nifedipine | PCN | CYP3A23 or CYP3A4 | Xie et al., 2000a |
| Clotrimazole | Phenobarbital | Progesterone | promoters—luciferase | |||
| RU486 | ||||||
| 17β-Estradiol | ||||||
| Pregnenolone | ||||||
Activation profiles were generated by transient cotransfections of the PXR and various response elements. Information listed in the table is intended as a general guide to compounds that activate the PXR, and should not be considered quantitative.