Table 3.
Allosteric Modulating Activities of Representative CB1 Allosteric Modulators in the human CB1 Calcium Mobilization, [35S]GTPγS Binding, and cAMP Assays.
| Compound | hCB1 Calcium pIC50a |
hCB1 [35S]GTPγS pIC50a |
hCB1 cAMP pIC50a |
|---|---|---|---|
| Org27569 | 6.1 ± 0.07 | 6.0 ± 0.05 | 6.8 ± 0.0654 |
| PSNCBAM-1 | 7.5 ± 0.1 | 7.0 ± 0.1 | 6.4 ± 0.1 |
| 8 | 6.7 ± 0.09 | 5.2 ± 0.05 | 5.5 ± 0.03 |
| 9 | 6.1 ± 0.05 | 5.9 ± 0.3 | N.D. b |
| 10 | 6.1 ± 0.05 | 4.4 ± 0.3 | N.D. b |
| 12 | 6.6 ± 0.1 | 4.8 ± 0.2 | 5.6 ± 0.07 |
| 24 | 5.8 ± 0.03 | 5.1 ± 0.2 | N.D. b |
| 25 | 6.1 ± 0.01 | 5.1 ± 0.09 | N.D. b |
| 26 | 6.6 ± 0.06 | 4.9 ± 0.1 | 5.4 ± 0.05 |
a
Compounds tested against EC80 (100 nM) of CP55,940. Values are the mean ± SEM of at least three independent experiments in duplicate.
b
N.D.: Not determined.