1′-OH-MDZ/4-hydroxymidazolam formation ratios from incubations of MDZ with cultured Caco-2 cells
Cell | Duration of 1α,25-(OH)2-D3 treatment | Extracellular matrix | Duration of MDZ incubation | 1′-OH-MDZ/4-OH-MDZ | |
---|---|---|---|---|---|
Apical | Basolateral | ||||
hr | hr | ||||
Clone 5 | |||||
336 | Matrigel | 7.5 | 5.4 | 5.2 | |
Untreated | Matrigel | 7.5 | 4.5 | 3.6 | |
Clone 7 | |||||
12 | Matrigel | 6 | 3.8 | N.D. | |
120 | Matrigel | 6 | 5.1 | N.D. | |
336 | Matrigel | 6 | 5.3 | N.D. | |
336 | laminin | 7 | 5.4 | 5.2 | |
336 | Matrigel | 7 | 5.3 | 5.2 |
Clone 5 is the clone that maximally expresses CYP3A immunoreactive protein, whether treated or untreated with 1α,25-(OH)2-D3. Clone 7 is the clone that was used for all of the other experiments described.
N.D., not done.