Table 2.
Summary data for hCB2 functional assays carried out on CP 55,940 and 2,4,6-trisubstituted 1,3,5-triazines.
| Internalisation (1 h) |
cAMP (5 min) |
pERK (4 min) |
|||||||
|---|---|---|---|---|---|---|---|---|---|
| Compound # | pEC50 (±SEM) | Emax (±SEM)a | n | pEC50 (±SEM) | Emax (±SEM)b | n | pEC50 (±SEM) | Emax (±SEM)c | n |
| CP 55,940 | 8.72 (0.09) | –65.1 (2.4) | 4 | 8.48 (0.01) | –41.7 (1.0) | 3 | 8.03 (0.06) | +10.29 (0.94) | 3 |
| 7 | 7.34 (0.15) | –61.4 (2.7) | 4 | 7.07 (0.15) | –43.0 (3.0) | 3 | 5.74 (0.05) | +2.06 (0.08) | 3 |
| 10 | 7.05 (0.13) | –57.4 (2.3) | 4 | 6.98 (0.11)Δ | –33.0 (0.9)Δ | 3 | 5.97 (0.04) | +10.18 (1.16) | 3 |
| 13 | Not Measurable | +6.2 (3.1)∗ | 3 | 6.10 (0.17) | +44.7 (4.6) | 3 | 6.27 (0.07) | +1.22 (0.13) | 3 |
| 14 | 6.76 (0.11) | –61.8 (1.6) | 4 | 6.02 (0.17)Δ | –29.8 (0.5)Δ | 3 | 5.13 (0.06)∧ | +4.66 (0.16)∧ | 3 |
| 15 | 8.91 (0.11) | –56.5 (1.5) | 4 | 8.10 (0.11) | –39.6 (1.2) | 3 | 7.45 (0.07) | +9.96 (0.53) | 3 |
| 16 | 8.92 (0.09) | –50.0 (2.7) | 4 | 8.55 (0.16) | –35.6 (2.2) | 3 | 7.91 (0.08) | +7.63 (0.25) | 3 |
aInternalisation Emax represented as reduction (-) or increase (+) in surface expression, as a percentage of vehicle-treated control. bcAMP Emax represented as reduction (-) or increase (+) in cAMP as a percentage of forskolin-treated (100%) minus Vehicle-treated (0%) controls. cpERK Emax indicates increase in pERK as a percentage of PMA (100%) and U0126 (0%) controls, less Vehicle-treated control. ∗A concentration-response curve could not be fitted, therefore efficacy at the highest concentration tested (i.e., 10 μM) is noted instead of Emax. ΔParameters are approximate due to the possible influence of non-CB2-mediated effects. ∧A fully defined concentration-response curve could not be obtained, therefore this pEC50 can only be considered approximate, and efficacy at the highest concentration tested (i.e., 10 μM) is noted instead of Emax. Column “n” indicates the number of independent experiments performed.