In vivo rat dopamine D2 receptor occupancy using LC/MS/MS for LY379268, LY317206, aripiprazole, and haloperidol
LY379268 (1–10 mg/kg), LY354740 (10–60 mg/kg), or aripiprazole (10–60 mg/kg) was administered 60 min or 90 min before the intravenous injection of the occupancy tracer raclopride (3 μg/kg). Animals (n = 4–5 animals per group) were sacrificed 15 min after the intravenous administration of the raclopride tracer. Haloperidol data are taken from a previously published report by Barth et al. (2006).
| Compound (Route) | Dose | %D2 RO ± S.E.M. |
|---|---|---|
| mg/kg | ||
| LY379268 (i.p.) | 1 | −11 ± 22 |
| 3 | 2.7 ± 6.6 | |
| 10 | −25.6 ± 4.3 | |
| LY354740 monohydrate (i.p.) | 3 | 13.2 ± 6.7 |
| 10 | 5.1 ± 11.7 | |
| 30 | 15.0 ± 8.3 | |
| Aripiprazole (p.o.) | 10 | 55.5 ± 6.1 |
| 30 | 88.7 ± 1.7 | |
| 60 | 93.1 ± 2.2 | |
| Haloperidol (p.o.) | 0.01 | −2.54. ± 4.4 |
| 0.03 | 12.9 ± 7.2 | |
| 0.1 | 29.9 ± 1.6 | |
| 0.3 | 52.1 ± 4.4 | |
| 1 | 71.4 ± 1.9 | |
| 3 | 86.9 ± 2.0 |
RO, receptor occupancy.