Compartmental PK parameter estimates based on simultaneous fitting of concentrations in brain ECF and unbound concentrations in plasma
The mean (% CV) calculated from the estimates obtained from fitting of individual animal data are presented; n = 4 rats for each compound.
| Drug | Vc | Cl | ka | Vp | Qd | Vb,u* | Clin | Clout |
|---|---|---|---|---|---|---|---|---|
| l/kg | ml · min−1 · kg−1 | min−1 | l/kg | ml · min−1 · kg−1 | ml/g brain | ml · min−1 · g−1 | ml · min−1 · g−1 | |
| Escitalopram | 4.1 (34) | 277 (32) | 0.02 (43) | 17 (39) | 117 (58) | 18 | 0.19 (39) | 0.16 (52) |
| Clozapine | 275 (12) | 2006 (49) | 0.04 (97) | 70 | 0.07 (50) | 0.44 (38) | ||
| N-desmethylclozapine | 607 (83) | 1597 (83) | 0.50 (68) | 82 | 0.02 (59) | 0.38 (68) | ||
| Risperidone | 21 (50) | 307 (21) | 0.03 (53) | 10 | 0.05 (25) | 0.32 (12) |
↵* Vb,u estimates = 1/fu,b and were fixed during the modeling. For escitalopram, fu,b was 3.1% and taken from Bundgaard et al. (2007a). For clozapine, N-desmethylclozapine, and risperidone, fu,b estimates were 0.8 (2), 0.7 (10), and 6.5% (8), respectively [mean (% CV)].