Ex vivo binding analysis after a single oral administration of Lu AA33810 in rats
All tissues were collected 1 h postdose. Plasma and brain samples were analyzed for exposure levels of Lu AA33810. Brain sections through the caudate putamen were analyzed for specific binding using the Y5 receptor-selective radioligand [35S]Lu AE66516. The reduction in specific binding of [35S]Lu AE66516 (relative to maximal values in vehicle-treated controls) was used to determine percentage receptor occupancy of Lu AA33810. Data represent mean ± S.E.M. of n = 3 experiments.
Lu AA33810 | Plasma Levels | Brain Levels | Occupancy |
|---|---|---|---|
| ng/ml | ng/g | % Maximal | |
| 1 mg/kg p.o. | 22 ± 10 | 29 ± 12 | 22 ± 12 |
| 3 mg/kg p.o. | 44 ± 14 | 69 ± 19 | 28 ± 3 |
| 10 mg/kg p.o. | 64 ± 24 | 103 ± 21 | 54 ± 6 |
| 30 mg/kg p.o. | 156 ± 6 | 285 ± 4 | 95 ± 2 |