TABLE 3.
Pharmacokinetic and blood-brain barrier parameters of subcutaneous administration of a 10-mg/kg dose of compound 56, GSK-1059865, SB-334867, and SB-408124 in rats
| Compound 56 | GSK-1059865 | SB-334867 | SB-408124 | |
|---|---|---|---|---|
| Plasma | ||||
| Tmax (h) | 0.25 | 2.00 | 0.50 | 0.50 |
| T1/2 (h) | 0.62 | 2.95 | 1.11 | 2.31 |
| Cmax (ng/ml) | 1871 | 756 | 5407 | 37,028 |
| AUCinf (h*ng/ml) | 3350 | 9142 | 18,068 | 153,418 |
| Brain | ||||
| Tmax (h) | 0.25 | 1.00 | 0.50 | 0.50 |
| Cmax (ng/ml) | 903 | 254 | 1563 | 896 |
| AUCinf (h*ng/ml) | 1515 | 1520 | 5586 | 4081 |
| Brain/plasma ratio | 0.48 | 0.34 | 0.29 | 0.02 |
AUCinf, area under the curve extrapolated to infinity.