TABLE 2

The parameters of eight model compounds in rats


Compound

Class

In Vivo Kp

fu,plasma

fu,homogenate

fu,slice

Cslice/Cplasma

fu,plasma/fu,slice

fu,plasma/fu,homogenate
Caffeine Neutral 0.70a 0.96 ± 0.03 1.1 ± 0.2 0.71 0.36 1.3 0.87
CP-141938 Base 0.31a 0.56 ± 0.01 0.22 ± 0.03 0.11 2.8 5.0 2.5
Fluoxetine Base 25a 0.060 ± 0.001 0.00094 ± 0.00050 0.0027 20 22 60
NFPS Zwitterion 0.90a 0.041 ± 0.005 0.0017 ± 0.0002 0.011 2.7 3.7 24
Propranolol Base 15a 0.15 ± 0.02 0.036 ± 0.009 0.019 8.4 7.9 4.2
Quinidine Base 0.5b 0.184 ± 0.023 0.0392 ± 0.0035 0.032 6.1 5.8 4.7
Theobromine Neutral 0.50a 0.92 ± 0.06 0.61 ± 0.09 0.62 1.6 1.5 1.5
Theophylline
Neutral
0.31a
0.29 ± 0.01
0.39 ± 0.06
0.31
0.60
0.94
0.74