Potency and efficacy of JWH-133 and THC in CB2R signaling response assays
| . | ERK phosphorylation . | β-arrestin2 recruitment . | Inhibition of cAMP . | |||
|---|---|---|---|---|---|---|
| EC50**** . | Emax, % . | EC50**** . | Emax, %** . | IC50 . | Maximum inhibition . | |
| JWH-133 | 19 ± 2 nM | 340 ± 63 | 49 ± 1 nM | 177 ± 6 | 16 ± 1 nM | 35 ± 4 |
| THC | 23 ± 3 µM | 475 ± 158 | 13 ± 1 µM | 144 ± 3 | Inactive | Inactive |
| . | ERK phosphorylation . | β-arrestin2 recruitment . | Inhibition of cAMP . | |||
|---|---|---|---|---|---|---|
| EC50**** . | Emax, % . | EC50**** . | Emax, %** . | IC50 . | Maximum inhibition . | |
| JWH-133 | 19 ± 2 nM | 340 ± 63 | 49 ± 1 nM | 177 ± 6 | 16 ± 1 nM | 35 ± 4 |
| THC | 23 ± 3 µM | 475 ± 158 | 13 ± 1 µM | 144 ± 3 | Inactive | Inactive |
CHO cells were stably transfected with the human CB2R and then used in PathHunter assays to assess the effect of varying concentrations of JWH-133 and THC on specified signaling pathways. Data are from 3 to 6 replicates per assay and are presented as the mean ± standard error of the mean.
EC50, 50% effective concentration; IC50, 50% inhibitory concentration.
P < .01, ****P < .0001.