Table 2.
Comparison of affinity data for CB1 receptor of the set of reference compounds obtained through the radioligand competition binding assay and CB1 competition binding assays with Tag-lite® technology using CELT-335.
| Compound | Functional Activity | pKi CB1 | |
|---|---|---|---|
| Radioligand Binding | Tag-Lite® Binding (CELT-335) | ||
| Rimonabant | CB1 Antagonist | 8.21 [30] | 8.41 ± 0.07 |
| MJ15 | CB1 Antagonist | 7.20 ± 0.12 | 7.44 ± 0.08 |
| Adamantyl-quinolone | CB1/CB2 agonist | 7.31 ± 0.09 | 7.10 ± 0.08 |
| AMB-FUBICA | CB1/CB2 agonist | 7.32 ± 0.07 | 6.93 ± 0.13 |
| AB-FUBICA | CB1/CB2 agonist | 8.44 ± 0.11 | 9.52 ± 0.09 |
| MDMB-CHMICA | CB1/CB2 agonist | 9.38 [31] | 8.09 ± 0.11 |
| CBD | CB1/CB2 Antagonist | 5.37 [29] | 6.15 ± 0.13 |
Values represent the mean ± SEM of triplicate determinations. Reference is not indicated for those compounds whose affinity through the radioligand binding assay was measured experimentally following published protocols [17].