Table 1.
| ||||
---|---|---|---|---|
Compound | R | IC50 (nM)a | FAAH Inhibition in liver (%)b | FAAH Inhibition in brain (%)b |
1a (URB597) | H | 7.7 ± 1.5 | Not determined | 96.2 ± 0.4 |
1b (URB937) | OH | 26.8 ± 4.9 | 91.7 ± 0.7 | −3.0 ± 8.0 |
1c | OCH3 | 45.3 ± 14.1 | 94.6 ± 0.7 | 86.4 ± 2.1 |
1d | CH3 | 20.5 ± 0.6 | 93.0 ± 1.1 | 91.9 ± 1.5 |
1e | F | 49.7 ± 5.8 | 90.7 ± 1.2 | 89.7 ± 1.3 |
1f | NH2 | 42.5 ± 4.2 | 92.2 ± 0.6 | 23.2 ± 2.1 |
IC50 measured in membrane preparations of Wistar rat brain
FAAH inhibition measured ex vivo 1 h after injection in Swiss Webster mice (1 mg-kg−1, i.p., n = 3)