TABLE 1

Molecular weight (MW), mean rat plasma (fu,p) and brain homogenate (fu,b) unbound fractions, and single-dose-derived neuromatrix AUC values for the nine commercial and two proprietary compounds evaluated in rats

CompoundMWfu,pafu,baPlasmaCSFBrain
AUC0-TlastAUC0-∞AUC0-TlastAUC0-∞AUC0-TlastAUC0-∞
ng · h/mlng · h/mlng · h/ml
Carbamazepineb2360.2220.09002270228045645825402550
Citalopramb3240.3550.028593095840142112,50012,900
Ganciclovirb2550.9720.8551700172078.482.5170182
Metoclopramideb3000.6350.329365367418420629635
Norclozapinec3130.06250.005693465704.808.91221699
Quinidineb3240.2650.03644920531030230418501880
Risperidonec4110.07980.069940944111.311.9108130
9-Hydroxyrisperidonec4270.1290.07551843423.2812.213.569.0
Thiopentalb2420.1110.098621624416.416.6209215
PF-4778574c3910.04760.01951221313.465.40131150
CE-157119c3100.01450.005063024796.428.1233605570
  • a For commercial compounds, mean values were reported by Liu et al. (2009a).

  • b Tlast is 7 h postdose.

  • c Tlast is 2 h postdose.