Table 2.
hCB1R- or hCB2R-dependent inhibition of FSK-stimulated cAMP accumulation.
| Compound | hCB1R | hCB2R | ||
|---|---|---|---|---|
| EC50 (nM) | Emax (%) | EC50 (nM) | Emax (%) | |
| CP55,940 | 7.7 (0.13–14) | 100 ± 6.2 | 4.0 (0.86–12) | 100 ± 8.2 |
| ∆9-THC | 240 (100–320)* | 56 ± 9.6* | 18.0 (5.0–102) | 76 ± 8.6* |
| ∆9-THCa | > 10,000 | 35 ± 11 | 1800 (360–3800)*^ | 95 ± 1.5^† |
| THCV | 260 (46–1200)* | 59 ± 3.9* | 280 (49–610)*^ | 79 ± 1.3*† |
| CBD | > 10,000 | 26 ± 1.6* | > 10,000 | 61 ± 2.3*† |
| CBDa | 30 (2.8–200) | 22 ± 1.1* | 140 (29–310)* | 32 ± 4.2*† |
| CBDV | > 10,000 | 68 ± 5.7* | 5.0 (0.46–33) | 51 ± 12* |
| CBG | 120 (7.4–700) | 68 ± 2.4* | 130 (30–550)* | 39 ± 11*^† |
| CBC | 190 (23–1700)* | 68 ± 9.7* | 7.1 (2.0–24) | 76 ± 5.4* |
hCB1R- or hCB2R-dependent inhibition of FSK-stimulated cAMP accumulation was quantified in HitHunter 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 within receptor; ^p < 0.05 compared to ∆9-THC within receptor; †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. 3 and 6.