Comparison of ALLO to GNX:PK parameters
Alloprenanolone and GNX were administered via i.v. tail vein injection. Blood was collected between 5 minutes and 6 hours after administration, and plasma was prepared. Brains were collected between 30 minutes and 3 hours after injection. Samples were analyzed as described in Materials and Methods. There were four animals per time point.
| Parameter | GNX (6 mg/kg) | GNX (9 mg/kg) | GNX (12 mg/kg) | GNX (15 mg/kg) | ALLO (15 mg/kg) |
|---|---|---|---|---|---|
| Plasma exposure (ng × h/ml; 0–6 h) | 1548 ± 564 | 2224 ± 67 | 3642 ± 346 | 6545 ± 324*** | 3010 ± 406 |
| Half life (min) | 22 ± 1 | 16 ± 1 | 17 ± 0.5 | 21 ± 1 | 16 ± 1 |
| Clearance (l/h per kilogram) | NC | 4.1 ± 0.1 | 3.4 ± 0.3 | 2.3 ± 0.1* | 5.3 ± 0.7 |
| Vd (l/kg) | NC | 1.2 ± 0.1 | 0.7 ± 1.0 | 0.87 ± 0.03 | 1.32 ± 0.21 |
| Brain exposure (ng × h/g; 0–3 h) | 8167 ± 88*** | 3789 ± 113 |
↵* P < 0.05; ***P < 0.001.