Comparison of uptake rates (CLint,uptake) for plated rat hepatocytes and suspended cells.
| Substrate | BDDCS Classa | Uptake Transporterb | CLint,uptake (μl/min × 106 cells) | |
|---|---|---|---|---|
| Plated Cells | Suspended Cells | |||
| Atenololc | III | None | 1.2 ± 0.2*** | 3.9 ± 0.4 |
| Metoprololc | I | None | 10 ± 2** | 27 ± 3 |
| Atorvastatin | II | OATPs | 30 ± 3 | 30 ± 4 |
| Bosentan | II | OATPs | 11.5 ± 3 | 18 ± 3 |
| Estrone-3-sulfated | III | NTCP/OATs/OATPs | 75 ± 9** | 210 ± 32 |
| Fexofenadine | III | OATPs | 3 ± 0.5** | 6 ± 1 |
| Terfenadinec | II | None | 153 ± 19** | 324 ± 53 |
| Montelukast | II | OATPs | 145 ± 20 | 143 ± 14 |
Mean 6 S.D. is shown, n = 3. Statistical significance was tested with the two-tailed Student's t test. ** P < 0.01, *** P < 0.001.
↵a BDDCS class as described by Benet et al. (2011).
↵b Transporter data are from the University of Tokyo and University of California–San Francisco and U.S. Food and Drug Administration (UCSF-FDA) online transporter databases (Ozawa et al., 2004; Morrissey et al., 2012); http://bts.ucsf.edu/fdatransportal.
↵c Compounds with predominantly passive uptake.
↵d As no dose value can be assigned to estrone-3-sulfate, no true BDDCS class assignation can be given, except to note that it is a highly soluble compound with little passive permeability.