Table 5.
Efficacy and potency of pure cannabinoids and of most of their corresponding ‘botanical drug substance’ (BDS) as inhibitors of human recombinant DAGLα
| Compounds | IC50 (µM) | Maximum concentration tested (% inhibition) |
|---|---|---|
| CBC | >100 µM | 100 µM |
| 39.5 ± 2.9 | ||
| CBC-BDS | >100 µM | 100 µM |
| 36.5 ± 7.1 | ||
| CBD | >100 µM | 100 µM |
| 0 | ||
| CBD-BDS | >50 µM | 50 µM |
| 8.5 ± 3.1 | ||
| CBG | >100 µM | 100 µM |
| 44.8 ± 4.1 | ||
| CBG-BDS | 65.7 ± 10.3 | 100 µM |
| 61.2 ± 4.9 | ||
| CBN | >50 µM | 50 µM |
| 26.9 ± 3.8 | ||
| CBDA | 19.4 ± 2.7 | 50 µM |
| 90.2 ± 2.6 | ||
| CBDA-BDS | 21.8 ± 1.3 | 50 µM |
| 87.4 ± 2.4 | ||
| CBGA | 30.5 ± 1.4 | 100 µM |
| 67.6 ± 0.3 | ||
| CBDV | 16.6 ± 4.1 | 100 µM |
| 83.3 ± 1.8 | ||
| CBDV-BDS | >50 µM | 50 µM |
| 16.2 ± 6.3 | ||
| CBGV | >50 µM | 50 µM |
| 18.9 ± 6.9 | ||
| CBGV-BDS | >50 µM | 50 µM |
| 47.1 ± 8.5 | ||
| THCA | 27.3 ± 1.6 | 50 µM |
| 86.2 ± 6.9 | ||
| THCA-BDS | 21.8 ± 2.8 | 50 µM |
| 97.6 ± 1.4 | ||
| THCV | >50 µM | 50 µM |
| 8.8 ± 0.7 | ||
| THCV-BDS | >50 µM | 50 µM |
| 0.5 ± 0.1 | ||
| THCVA | >50 µM | 100 µM |
| 71.6 ± 5.1 | ||
| THCVA-BDS | >50 µM | 100 µM |
| 52.1 ± 10.3 | ||
| CBDVA | 35.0 ± 5.6 | 50 µM |
| 61.0 ± 0.7 |
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 DAGLα 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; DAGLα, diacylglycerol lipase α; THC, Δ9-tetrahydrocannabinol; THCA, THC acid; THCV, propyl analogue of THC or tetrahydrocannabivarin; THCVA, tetrahydrocannabivarin acid.