Kinetic parameters for the penetration across the monolayers of polarized cell lines expressing mouse Mdr1a and their corresponding control cells
Permeabilities across LLC-PK1/L-mdr1a were determined by the slops from 1 to 3 h in the transcellular transport. Transport of apical-to-basal (A to B) and basal-to-apical (B to A) direction represent the mean ± S.E.M. (n = 3).
| Compound | Transport | |||
|---|---|---|---|---|
| LLC–PK1 | L–mdr1a | |||
| A to B | B to A | A to B | B to A | |
| μl/h/well | ||||
| Antipyrine | 31.2 ± 1.9 | 29.6 ± 3.0 | 28.7 ± 3.3 | 25.6 ± 1.3 |
| Benzylpenicillin | 5.2 ± 0.7 | 3.7 ± 0.3 | 7.5 ± 1.4 | 4.7 ± 0.3 |
| Buspirone | 40.7 ± 3.1 | 39.9 ± 1.0 | 38.6 ± 0.6 | 38.4 ± 1.4 |
| Caffeine | 32.1 ± 1.2 | 34.5 ± 2.2 | 29.7 ± 1.7 | 35.4 ± 2.7 |
| Carbamazepine | 41.0 ± 0.9 | 46.5 ± 1.2 | 40.6 ± 2.6 | 45.2 ± 1.9 |
| Cephalexin | 4.0 ± 0.2 | 3.7 ± 0.4 | 4.8 ± 0.3 | 3.7 ± 0.1 |
| Citalopram | 32.0 ± 5.3 | 35.5 ± 5.4 | 25.9 ± 3.3 | 39.2 ± 4.1 |
| Cimetidine | 3.6 ± 0.0 | 20.2 ± 1.2 | 3.2 ± 0.8 | 15.0 ± 2.6 |
| Daidzein | 16.5 ± 0.7 | 39.1 ± 0.9 | 17.3 ± 1.3 | 41.0 ± 1.2 |
| Dantrolene | 22.5 ± 1.3 | 38.6 ± 1.2 | 24.3 ± 0.4 | 39.2 ± 3.3 |
| Diazepam | 44.4 ± 1.8 | 43.7 ± 1.9 | 46.5 ± 1.4 | 42.2 ± 1.1 |
| Flavopiridol | 26.6 ± 1.1 | 39.6 ± 1.7 | 9.6 ± 2.2*** | 67.3 ± 9.8** |
| Fleroxacin | 5.0 ± 0.2 | 6.1 ± 0.3 | 5.4 ± 0.2 | 7.5 ± 0.6 |
| Genistein | 17.8 ± 1.0 | 33.1 ± 4.1 | 14.7 ± 1.6 | 28.1 ± 0.8 |
| Loperamide | 22.1 ± 0.6 | 15.0 ± 1.2 | 12.9 ± 0.7** | 54.7 ± 2.3*** |
| Midazolam | 41.4 ± 3.1 | 42.2 ± 1.2 | 38.1 ± 0.5 | 44.5 ± 3.0 |
| Pefloxacin | 5.4 ± 1.7 | 8.5 ± 0.1 | 5.1 ± 1.5 | 12.3 ± 0.7** |
| Phenytoin | 31.0 ± 2.2 | 37.7 ± 1.5 | 29.6 ± 1.6 | 37.1 ± 1.7 |
| Quinidine | 22.3 ± 0.8 | 22.9 ± 1.1 | 6.6 ± 0.6*** | 42.2 ± 2.2** |
| Risperidone | 41.8 ± 0.1 | 45.9 ± 1.5 | 21.3 ± 4.9* | 63.0 ± 2.6** |
| Sertraline | 2.7 ± 0.2 | 1.9 ± 0.2 | 2.8 ± 0.2 | 2.4 ± 0.3 |
| Sulpiride | 1.9 ± 0.2 | 2.4 ± 0.1 | 2.0 ± 0.7 | 2.7 ± 0.3 |
| Thiopental | 37.1 ± 1.4 | 36.4 ± 1.7 | 39.6 ± 2.0 | 37.7 ± 1.1 |
| Verapamil | 24.9 ± 0.5 | 23.4 ± 1.3 | 15.4 ± 1.1** | 49.0 ± 1.9*** |
| Zolpidem | 42.4 ± 1.8 | 41.6 ± 1.9 | 40.3 ± 0.7 | 45.8 ± 4.6 |
↵Statistically significant differences in the permeability between transporter-expressing cells and the corresponding control cells: *, P < 0.05; **, P < 0.01; and ***, P < 0.001.