Table 5.
Characterization of selected compounds
| Cp d |
Structure |
r- FAA H IC50 [nM]a |
h
-FAA H IC50 [nM]a |
Plasm a Stab. (% at 7 h)b |
MLM Stab. half- life (min.) c |
Kineti c sol. (μM)d |
|---|---|---|---|---|---|---|
| 1a |
|
5.7 ± 1.2 |
3.1 ± 1.3 |
0 | <5 | 6 |
| 27 |
|
10.5 ± 2.9 |
3.6 ± 0.9 |
91 ± 3 | 5 | 18 |
| 34b |
|
3.9 ± 0.7 |
4.2 ± 1.0 |
88 ± 11 |
6 | 174 |
| 40 |
|
5.8 ± 0.6 |
9.4 ± 2.0 |
89 ± 9 | 8 | 152 |
IC50 values for FAAH inhibition are reported as the mean ± SEM (n= 3);
Data are the mean ± SEM of three determinations;
Data are the mean of three determinations;
Phosphate buffered saline, pH 7.4, single determination.