CLint values of inhibitors determined in five human hepatocyte donors
Assays were carried out 12 to 16 h after plating and CLint values were determined by the rate of parent disappearance over 90 min as described under Materials and Methods. Final concentration of compounds was 1 μM. Due to limited numbers of hepatocytes, all compounds were not incubated in all donors.
Compound | CLint | ||||||||
---|---|---|---|---|---|---|---|---|---|
Donor 1 | Donor 2 | Donor 3 | Donor 4 | Donor 5 | |||||
μl/min/106 cells | |||||||||
Tienilic acid | 5 | 7 | 6 | 7 | 9 | ||||
Erythromycin | 15 | 7 | N.D. | N.D. | 5 | ||||
Troleandomycin | 49 | 51 | N.D. | N.D. | 37 | ||||
Fluoxetine | 13 | N.D. | 35 | 10 | 9 | ||||
AZ1 | 0.3 | N.D. | 0.3 | N.D. | 0.2 |
N.D., not determined.