Table 5.
Pharmacokinetic parameters after oral administration for BIA 10‐2474 (0.1 and 0.3 mg·kg−1 p.o.) and PF‐04457845 (0.03 and 0.1 mg·kg−1 p.o.) in mouse plasma and brain (n = 4)
| Treatment (mg·kg−1) | Plasma | Brain | ||||||
|---|---|---|---|---|---|---|---|---|
| t ½ | t max | C max | AUClast | t ½ | t max | C max | AUClast | |
| (hr) | (hr) | (ng·ml−1) | (hr·ng·ml−1) | (hr) | (hr) | (ng·g−1) | (hr·ng·g−1) | |
| BIA 10‐2474 | ||||||||
| 0.1 | 2.2 | 1 | 33.0 | 109.7 | NR | 1 | 5.3 | 11.3 |
| 0.3 | 1.9 | 1 | 104.5 | 337.5 | 1.75 | 1 | 21.6 | 60.8 |
| PF‐04457845 | ||||||||
| 0.03 | NR | 2 | 1.3 | 4.3 | NR | NR | NR | NR |
| 0.1 | NR | 2 | 38.3 | 238.3 | NR | 2 | 3.7 | 22.9 |
Note. Concentrations of test substances were measured at 1, 2, 4, and 8 hr after administration. The limits of quantification were 0.1 ng·ml−1 for plasma and 1 ng·g−1 for the brain.
Abbreviation: NR, not reliable (insufficient data to calculate reliable values).