Table 4. Total Brain Level Comparison between 6, 9–12, and 18a,b.
cmpd | 6 | 9 | 10 | 11 | 12 | 18 |
---|---|---|---|---|---|---|
fu, brain (rat)c | >0.30 | 0.026 | 0.17 | 0.10 | 0.10 | >0.30 |
brain 1 h (ng/g) | 2730 | 807 | 801 | 895 | 370 | 789 |
B/P 1 h | 0.65 | 0.69 | 0.44 | 0.98 | 1.1 | 0.61 |
Male Sprague–Dawley rat fed (n = 2 per time point) 10 mg/kg s.c.
Compounds were formulated with 20% HPβCD at pH 3.5–4.
Estimated unbound drug fraction to rat brain homogenates after 5 h incubation at 37 °C using a Rapid Equilibrium Dialysis device.