Affinity and kinetic binding proprieties of CB2R reference ligands determined by [3H]RO6957022 displacement and competition association experiments
| Compound | pKi (Ki) | kon | koff | RT | KD |
|---|---|---|---|---|---|
| nM | nM−1/min−1 | min−1 | minute | nM | |
| RO6957022 | 8.9 ± 0.05 (1.2) | 0.15 ± 0.03 | 0.19 ± 0.03 | 5.3 ± 0.7 | 1.3 ± 0.4 |
| CP55,940 | 9.3 ± 0.03 (0.50) | 0.22 ± 0.02 | 0.20 ± 0.02 | 5.0 ± 0.4 | 0.90 ± 0.1 |
| JWH-133 | 7.4 ± 0.07 (39) | 0.0042 ± 0.001 | 0.31 ± 0.07 | 3.2 ± 0.7 | 75 ± 24 |
| HU-308 | 7.6 ± 0.08 (25) | 0.011 ± 0.001 | 0.23 ± 0.01 | 4.2 ± 0.2 | 21 ± 3 |
| AM1241 | 8.2 ± 0.03 (6.3) | — | — | — | — |
| GW405833 | 8.4 ± 0.02 (3.5) | 0.25 ± 0.06 | 0.70 ± 0.1 | 1.4 ± 0.3 | 2.8 ± 0.8 |
| SR144528 | 8.3 ± 0.02 (5.0) | 0.028 ± 0.003 | 0.12 ± 0.02 | 8.7 ± 1.7 | 4.1 ± 0.9 |
| AM630 | 7.7 ± 0.03 (20) | — | — | — | — |
| AEA | — | 0.0024 ± 0.0004 | 0.73 ± 0.11 | 1.4 ± 0.2 | 305 ± 45 |
| 2-AG | — | 0.032 ± 0.005 | 3.2 ± 0.9 | 0.31 ± 0.09 | 99 ± 27 |
| NE | — | 0.042 ± 0.033 | 6.3 ± 1.0 | 0.16 ± 0.03 | 151 ± 24 |
Receptor affinities (Ki) were calculated using the Cheng- Prusoff equation (Cheng and Prusoff, 1973). Kinetic binding parameters (i.e., kon and koff) were obtained using the Motulsky-Mahan model (Motulsky and Mahan, 1984). The derived affinity values were calculated using the equation KD = koff/kon. The results shown are the mean ± S.E.M. of at least three individual experiments, em dashes indicate the absence of value for the mentioned compound.