Table 6.
Efficacy and potency of pure cannabinoids and of most of their corresponding ‘botanical drug substance’ (BDS) as inhibitors of COS cell MAGL
| Compounds | IC50 (µM) | Maximum concentration tested (% inhibition) |
|---|---|---|
| CBC | 50.1 ± 12.1 | 100 µM |
| 64.5 ± 3.6 | ||
| CBC-BDS | 91.4 ± 13.8 | 100 µM |
| 58.5 ± 8.1 | ||
| CBD | >100 µM | 100 µM |
| 0 | ||
| CBD-BDS | >50 µM | 50 µM |
| 23.0 ± 3.8 | ||
| CBG | 95.7 ± 32.4 | 100 µM |
| 54.2 ± 3.8 | ||
| CBG-BDS | 24.6 ± 8.4 | 100 µM |
| 66.1 ± 3.4 | ||
| CBN | >50 µM | 50 µM |
| 31.5 ± 3.3 | ||
| CBDA | >50 µM | 50 µM |
| 18.5 ± 2.1 | ||
| CBDA-BDS | 29.6 ± 1.1 | 50 µM |
| 94.0 ± 10.5 | ||
| CBGA | >50 µM | 50 µM |
| 17.2 ± 1.8 | ||
| CBDV | >100 µM | 100 µM |
| 2.5 ± 0.1 | ||
| CBDV-BDS | >50 µM | 50 µM |
| 5.2 ± 0.6 | ||
| CBGV | >50 µM | 50 µM |
| 4.9 ± 1.9 | ||
| CBGV-BDS | >50 µM | 50 µM |
| 37.9 ± 5.7 | ||
| THCA | 46.0 ± 1.2 | 100 µM |
| 86.0 ± 4.1 | ||
| THCA-BDS | 6.2 ± 1.2 | 50 µM |
| 86.3 ± 13.1 | ||
| THCV | >50 µM | 50 µM |
| 18.2 ± 5.4 | ||
| THCV-BDS | >50 µM | 50 µM |
| 23.5 ± 5.2 | ||
| THCVA | >50 µM | 50 µM |
| 16.9 ± 9.6 | ||
| THCVA-BDS | >50 µM | 50 µM |
| 39.8 ± 5.7 |
Data are means ± SEM of at least n = 3 separate experiments in which various concentrations (1, 10, 25, 50 or 100 µM) of the pure compounds/BDS were incubated. Efficacy was calculated as % of MAGL inhibition at the maximal concentration tested (which is shown in the first line of the cell).
CBC, cannabichromene; CBD, cannabidiol; CBDA, cannabidiol acid; CBDV, propyl analogue of CBD or cannabidivarin; CBG, cannabigerol; CBGV, cannabigivarin; CBN, cannabinol; MAGL, monoacylglycerol lipase; THC, Δ9-tetrahydrocannabinol; THCA, THC acid; THCV, propyl analogue of THC or tetrahydrocannabivarin; THCVA, tetrahydrocannabivarin acid.