Permeability data for So324 (H), Cf1525 (p-Me), and Cf1572 (p-I) derivatives at C0 0.5 mM through MDCKII and MDR1-MDCKII monolayers measured in a 120-min transport experiment
Results are mean ± S.D. of four monolayers.
Compound | Permeability Coefficients (×10-6 cm/s) | ||||||
|---|---|---|---|---|---|---|---|
| MDCKII | MDR1-MDCKII | ||||||
| FE | SE | FE | SE | ||||
| So324 (H) | |||||||
| A-B | 1.1 ± 0.1 | 1.0 ± 0.1 | 0.6 ± 0.1 | 0.6 ± 0.1 | |||
| B-A | 3.5 ± 0.5 | 3.5 ± 0.1 | 7.4 ± 1.9 | 7.1 ± 2.1 | |||
| Cf1525 (p-Me) | |||||||
| A-B | <0.1a | <0.1a | <0.1a | <0.1a | |||
| B-A | 3.5 ± 1.0 | 3.0 ± 0.9 | 13.4 ± 2.3 | 14.5 ± 2.0 | |||
| Cf1572 (p-I) | |||||||
| A-B | 1.6 ± 0.3 | 3.5 ± 1* | <0.1a | <0.1a | |||
| B-A | 5.3 ± 0.8 | 8.0 ± 1.2* | 16.8 ± 2.0 | 19.9 ± 2.4 | |||
>* Statistical difference of the SE to the respective FE diastereoisomer (p < 0.05).
↵ a Concentrations in the receiver chambers were below the limit of detection of the HPLC assay and only upper limits of permeability could be calculated.