Table 4.
Time-dependent inhibition of recombinant cytochrome P450 activity by cannabinoids.
| Enzyme | Substrate | Reaction | THC | CBDa | CBN | Reference | ||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| KI (μM) | kinact (min−1) | kinact/KI (min−1μM−1) | KI (μM) | kinact (min−1) | kinact/KI (min−1μM−1) | KI (μM) | kinact (min−1) | kinact/KI (min−1μM−1) | ||||
| CYP1A1 | 7-Ethoxyresorufin | O-deethylation | 1.2 | 0.023 | 0.019 | 5.9 | 0.316 | 0.054 | 0.09 | 0.019 | 0.21 | (Yamaori et al., 2010) |
| CYP1A2 | - | - | - | 0.59 | 0.109 | 0.19 | - | - | - | |||
| CYP1B1 | - | - | - | 3.1 | 0.027 | 0.0087 | - | - | - | |||
| CYP2A6 | Coumarin | 7-hydroxylation | 0.86 | 0.017 | .020 | - | - | - | 1.01 | 0.0091 | 0.0090 | (Yamaori et al., 2011) |
a
Also showed time-dependent inhibition of 7-ethoxyresorufin O-deethylation in human liver microsomes (kinact, 0.152 min−1; KI, 2.1 μM). Dashes indicate data were not available.