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. 2015 Jan 15;6(3):282–286. doi: 10.1021/ml500463t

Table 4. Total Brain Level Comparison between 6, 912, 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
a

Male Sprague–Dawley rat fed (n = 2 per time point) 10 mg/kg s.c.

b

Compounds were formulated with 20% HPβCD at pH 3.5–4.

c

Estimated unbound drug fraction to rat brain homogenates after 5 h incubation at 37 °C using a Rapid Equilibrium Dialysis device.