Table 5

Binding of the model compounds to hepatic microsomes and their effects on predicting human CLint, in vivo

CompoundsMicrosomal Protein Concentrationfu, microsomeHuman CLuint, in vitroHuman Scaling Factor
RatDogHumanWell StirredParallel-TubeDispersion
mg/ml ml/min/kg
FK10520.50.3470.3340.323182.358.65.25.9
FK4801.00.1190.1200.112662.590.50.50.5
Zolpidem0.50.9380.9400.93930.885.14.24.4
Omeprazole0.50.9290.9720.975100.595.33.13.5
Nicardipine0.20.1750.1830.129134600.10.050.06
Nilvadipine0.20.4690.4700.4433866.552.10.70.8
Diazepam0.50.7810.7520.74520.131.11.11.1
Diltiazem0.2N.D.0.9070.863136.912.11.01.2
  • N.D., not determined.