Table 3.
FI, receptor occupancy, plasma exposure in S-D rats administered CE-178253
| Dose (mg/kg, p.o.) | Food Intake % decrease (mean ± SEM) | % Receptor Occupancy (mean ± S-D) | Unbound Plasma Concentration (nM ± S-D ) | Unbound plasma/rat brain Ki |
|---|---|---|---|---|
| 0.3 | 6 ± 3 | 27 ± 12 | 0.17 ± 0.02 | 0.4 |
| 1 | 25 ± 11 | 64 ± 2 | 1.0 ± 0.3 | 2.3 |
| 3 | 62 ± 5.2* | 78 ± 6 | 2.7 ± 1.0 | 6.2 |
| 10 | 75 ± 6.2* | 82 ± 2 | 15.6 ± 1.6 | 36 |
*significantly different from veh. p < 0.05
Overnight fasted S-D rats were administered veh. (0.5% MC), or CE-178253-01 p.o. Food was returned 30 min later. Cumulative food consumption was measured 2 hr after the return of food.