Table 1.
Allosteric Antagonist Potencies of Org27569, PSNCBAM-1, and 8-20 in the hCB1 Calcium Mobilization.
| Compound | Structure | pIC50a |
|---|---|---|
| Org27569 |
|
6.1 ± 0.07 |
| PSNCBAM-1 |
|
7.5 ± 0.1 |
| 8 |
|
6.7 ± 0.09 |
| 9 |
|
6.1 ± 0.05 |
| 10 |
|
6.1 ± 0.05 |
| 11 |
|
5.5 ± 0.03 |
| 12 |
|
6.6 ± 0.14 |
| 13 |
|
< 5 |
| 14 |
|
5.4 ± 0.06 |
| 15 |
|
< 5 |
| 16 |
|
< 5 |
| 17 |
|
5.8 ± 0.08 |
| 18 |
|
5.3 ± 0.09 |
| 19 |
|
< 5 |
|
20 (trans mixture) |
|
5.6 ± 0.09 |
a
Compounds tested against EC80 (100 nM) of CP55,940. Values are the mean ± SEM of at least three independent experiments in duplicate.