TABLE 3

Calculated Fraction of I2BS Occupied by BU224 Using 11C-BU99008

Percentage occupancy
BU224 dose (mg/kg)Whole brainGlobus pallidusFrontal cortexCerebellum
0.0135 (1)25 (2)38 (1)32 (2)32 (1)24 (2)30 (1)27 (2)
0.0354 (1)*66 (2)50 (1)*61 (2)48 (1)*65 (2)47 (1)*54 (2)
0.181 (2)74 (2)73 (2)64 (2)
0.393 (1)85 (1)75 (1)72 (1)
ED500.0220.0170.0170.016
  • * Percentage occupancies generated from averaged composite of baseline scans for monkey 1 due to failure to obtain baseline scan on this study day.

  • Number in parentheses indicates animal used to derive value: monkey 1 (1) and monkey 2 (2). Whole-brain occupancy was calculated using occupancy plot (17) and is derived from slope for all reported brain regions. Values calculated from VT determined using MA1 model.