Dose dependency of MAGL occupancy measured in mouse hippocampus after intraperitoneal administration of JNJ-42226314
Corresponding plasma and brain compound exposure and brain 2-AG at 30 min are also shown. Results are mean ± S.E.M. (N = 3). Values reported without S.E.M. indicate JNJ-42226314 levels were below the lowest level of quantification for at least one animal in that group.
| Dose (i.p.) | Brain (ng/g) | Plasma (ng/ml) | Brain 2-AG (ng/g) | MAGL Occupancy % |
|---|---|---|---|---|
| 0.1 | 43 ± 38 | 10 ± 2 | 456 ± 40 | 0 ± 0 |
| 0.3 | 16 | 26 | 535 ± 93 | 12 ± 12 |
| 1 | 82 | 131 ± 67 | 1164 ± 379 | 58 ± 29 |
| 3 | 131 ± 41 | 347 ± 168 | 2401 ± 509 | 95 ± 3 |
| 10 | 925 ± 54 | 2811 ± 164 | 8425 ± 520 | 98 ± 1 |
| 30 | 2180 ± 968 | 5360 ± 2407 | 8363 ± 2460 | 98 ± 2 |