Table 2.
Permeabilities of cannabinoids in wildtype, BCRP and P-glycoprotein MDCK cells.
| Wildtype | BCRP | P-glycoprotein | |||||||
|---|---|---|---|---|---|---|---|---|---|
| Substrate | P (B > A) | P (A > B) | r | P (B > A) | P (A > B) | r | P (B > A) | P (A > B) | r |
| CBD | 25 ± 3 | 41 ± 5 | 0.6 ± 0.2 | 86 ± 20* | 52 ± 8 | 1.6 ± 0.3 | 15 ± 3 | 25 ± 7 | 0.6 ± 0.3 |
| CBD + Elacridar | – | – | – | 37 ± 6a | 37 ± 6 | 1.0 ± 0.2 | – | – | – |
| CBDA | 37 ± 9 | 31 ± 8 | 1.2 ± 0.3 | 162 ± 24*** | 38 ± 11 | 4.2 ± 0.3 | 38 ± 4 | 24 ± 7 | 1.5 ± 0.3 |
| CBDA + Elacridar | – | – | – | 42 ± 6b | 121 ± 48 | 0.3 ± 0.3 | – | – | – |
| CBDV | 44 ± 5 | 43 ± 5 | 1.0 ± 0.2 | 90 ± 9*** | 63 ± 14 | 1.4 ± 0.2 | 34 ± 3 | 30 ± 8 | 1.1 ± 0.3 |
| CBDV + Elacridar | – | – | – | 68 ± 7* | 49 ± 8 | 1.4 ± 0.2 | – | – | – |
| CBDVA | 25 ± 2 | 22 ± 3 | 1.1 ± 0.2 | 47 ± 6** | 24 ± 9 | 2.0 ± 0.4 | 22 ± 2 | 14 ± 4 | 1.6 ± 0.3 |
| CBDVA + Elacridar | n/a | n/a | n/a | 8 ± 1b | n.d | n.d | – | – | – |
| CBG | 10 ± 3 | 12 ± 5 | 0.8 ± 0.5 | 53 ± 10*** | 47 ± 9** | 1.1 ± 0.3 | 14 ± 2 | 19 ± 5 | 0.7 ± 0.3 |
| CBG + Elacridar | – | – | – | 19 ± 6a | n.d | n.d | – | – | – |
| CBGA | 1 ± 1 | n.d | n.d | 5 ± 1 | n.d | n.d | 3 ± 1 | 5 ± 2 | 0.7 ± 0.5 |
| Δ9-THC | 3 ± 1 | 9 ± 3 | 0.3 ± 0.3 | 74 ± 28* | 54 ± 17* | 1.4 ± 0.5 | 4 ± 1 | 9 ± 3 | 0.5 ± 0.4 |
| Δ9-THC + Elacridar | – | – | – | 11 ± 2**,a | 15 ± 3a | 0.7 ± 0.2 | – | – | – |
| Δ9-THCA | n.d | n.d | n.d | 6 ± 2 | n.d | n.d | 8 ± 3 | 17 ± 5 | 0.5 ± 0.4 |
P Permeability calculations (× 10−5 cm/s).
n.d. not determined; slope of concentration–time curve was not significantly different from zero.
*p < 0.05, **p < 0.005, ***p < 0.0005 compared to corresponding wildtype condition.
ap < 0.05, bp < 0.0001 compared to without inhibitor.