Table 3.
hCB1R- or hCB2R-dependent recruitment of βarrestin2.
| Compound | hCB1R | hCB2R | ||
|---|---|---|---|---|
| EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) | |
| CP55,940 | 920 (700–1200) | 100 ± 5.6 | 560 (410–760) | 100 ± 3.4 |
| ∆9-THC | > 10,000 | 37 ± 7.5* | 94 (78–210)* | 46 ± 4.9* |
| ∆9-THCa | > 10,000 | 4.1 ± 1.5*^ | > 10,000 | 15 ± 2.5*^† |
| THCV | > 10,000 | 0.05 ± 2.1*^ | > 10,000 | 50 ± 6.8*† |
| CBD | > 10,000 | 1.0 ± 1.6*^ | 58 (44–74)*^ | 23 ± 2.8*† |
| CBDa | > 10,000 | 0.10 ± 0.11*^ | > 10,000 | 18 ± 2.5*^† |
| CBDV | > 10,000 | 0.96 ± 0.75*^ | > 10,000 | 64 ± 13*† |
| CBG | > 10,000 | 0.41 ± 0.45*^ | > 10,000 | 22 ± 1.2*^† |
| CBC | > 10,000 | 6.9 ± 0.96*^ | > 10,000 | 12 ± 2.8*^ |
hCB1R-or hCB2R-dependent recruitment of βarrestin2 was quantified in PathHunter CHO cells stably expressing hCB1R or hCB2R and treated with compounds for 90 min. Data were fit to a variable slope (4 parameter) non-linear regression in GraphPad (v. 8). n ≥ 6 independent experiments performed in triplicate. EMax refers to the top of the concentration–response curve. Data are expressed as nM with 95% CI or %CP55,940 response, mean ± SEM. *p < 0.05 compared to CP55,940; ^p < 0.05 compared to ∆9-THC within assay and measurement; †p < 0.05 compared to hCB1R within compound; as determined via non-overlapping 95% CI or one-way ANOVA followed by Tukey's post-hoc test. Corresponding graphs are presented in Figs. 4 and 7.