Table 1.
[3H]CP55,940 displacement from hCB1R or hCB2R CHO cell membranes.
| Compound | hCB1R | hCB2R | ||
|---|---|---|---|---|
| Ki (nM) | Emin (%) | Ki (nM) | Emin (%) | |
| CP55,940 | 13 (5.6–33) | 0.0 ± 5.2 | 29 (13–67) | 0.0 ± 6.2 |
| ∆9-THC | 36 (17–62) | 10 ± 3.5 | 31 (15–62) | 7.4 ± 4.4 |
| ∆9-THCa | 620 (180–970)*^ | 67 ± 11*^ | 1.3 (0.33–6.3)*^† | 49 ± 7.2*^ |
| THCV | 22 (5.0–140) | 54 ± 4.1*^ | 47 (21–270) | 27 ± 9.5 |
| CBD | 200 (140–370)^ | 65 ± 11*^ | 240 (24–560) | 54 ± 9.3*^ |
| CBDa | > 10,000 | 96 ± 6.5*^ | 12 (4.9–77) | 30 ± 7.8† |
| CBDV | > 10,000 | 96 ± 5.1*^ | 140 (96–280)*^ | 22 ± 9.3† |
| CBG | 1300 (520–8400)*^ | 49 ± 7.2*^ | 490 (130–2500)*^ | 32 ± 8.1 |
| CBC | 11 (1.9–91) | 55 ± 3.7*^ | 27 (8.9–83) | 9.7 ± 5.9† |
Compound activity was quantified for [3H]CP55,940 binding in CHO cells stably expressing hCB1R or hCB2R and treated with compounds. Data were fit to a variable slope (4 parameter) non-linear regression in GraphPad (v. 8). n ≥ 6 independent experiments performed in duplicate. EMin refers to the bottom 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 between receptors; as determined via non-overlapping 95% CI or one-way ANOVA followed by Tukey's post-hoc test. Corresponding graphs are presented in Figs. 2 and 5.