TABLE 1

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.