Table 1.
Compound | IC50 ± SEM (μM) | Ki ± SEM (μM) | ||
---|---|---|---|---|
CB1 | CB2 | CB1 | CB2 | |
2 a | 3.2 ± 1.0 | 3.25 ± 0.5 | 1.62 ± 0.5 | 1.62 ± 0.51 |
12 ab | >5.3 ± 1.4 | >5.93 ± 0.8 | >2.6 ± 0.7 | >2.97 ± 0.4 |
16 | 20.8 ± 4.9 | ND c | 10.4 ± 2.5 | ND c |
16 a | 0.242 ± 0.07 d | ND c | 0.121 ± 0.04 d | ND c |
18 e | 24.6 ± 2.6 | 0.101 ± 0.035 | 12.3 ± 1.3 | 0.051 ± 0.01 |
CP55,940 | 9.84 nM | 8.62 nM | 4.9 nM | 4.31 nM |
a Represents compound’s affinity up to its solubility limit; b racemic compounds; c ND = not determined because the percent displacement at 10 μM was low; d data from Figure 4, for which CP55,940 Ki = 1.267 ± 0.13 nM; e the chromophore nature of the compound may have interfered with the radioligand detection (cf. main text).