Table 1.
GABAA/benzodiazepine receptor occupancy after intravenous administration of TPA023 in baboons
Specific binding was estimated 20 min after TPA023 administration and 60 min after [11C]flumazenil injection.
Baboon | TPA023 Dose | Frontal Cortex | Parietal Cortex | Temporal Cortex | Occipital Cortex | Cerebellum | Avg. ± S.D. |
---|---|---|---|---|---|---|---|
mg/kg | % | ||||||
1 | 0.0032 | 11 | 10 | 16 | 13 | 19 | 14 ± 4 |
0.032 | 63 | 68 | 70 | 69 | 76 | 69 ± 5 | |
0.32 | 99 | 98 | 98 | 97 | 99 | 98 ± 1 | |
2 | 0.0032 | 5 | 5 | 4 | 6 | 12 | 6 ± 3 |
0.032 | 58 | 64 | 65 | 62 | 70 | 64 ± 5 | |
0.32 | 98 | 99 | 99 | 97 | 99 | 98 ± 1 | |
3 | 0.0032 | 8 | 8 | 5 | 10 | 16 | 9 ± 4 |
0.032 | 44 | 46 | 50 | 51 | 64 | 51 ± 8 | |
0.32 | 95 | 95 | 95 | 94 | 96 | 95 ± 1 |