Table 1.
Compound | R | Ke CB1 (nM) | Ki CB1a (nM) | Ki CB2a (nM) | Selectivity (CB1/CB2) |
---|---|---|---|---|---|
5 | Me | 17 | |||
6 | Et | 2.3 | 3.57 | 426 | 119 |
7 | Ph | 4 | 2.55 | 10649 | 4176 |
8 | Cyclohexyl | 3.3 | 3.35 | 835 | 249 |
9 | n-Bu | 4.9 | 19.47 | 1046 | 54 |
10 | Cyclohexylmethyl | 2.1 | 1.93 | 2360 | 1223 |
11 | i-Bu | 5.4 | 4.01 | 89.5 | 22 |
12 | Cyclopentyl | 0.89 | 1.54 | 60.2 | 39 |
13 | 3-Methylbutyl | 7.4 | 2.67 | 215 | 81 |
14 | Cyclopentylmethyl | 2.9 | 2.02 | 569 | 282 |
15 | (Piperidin-1-yl)ethyl | 789 | |||
16 | Me2NCH2 | 140 | |||
17 | NH2 | 2768 | |||
18 | CF3 | 1.05 | 6.1 | 4501 | 738 |
Displacement was measured using [3H]CP55940