Probe substrate | Microsomes | THC | CBD | CBN | |||
---|---|---|---|---|---|---|---|
IC50 | IC50,u | IC50 | IC50,u | IC50 | IC50,u | ||
µM | µM | µM | µM | µM | µM | ||
Serotonin | rUGT1A6 | 10 ± 2.6 | 0.40 ± 0.10 | ||||
HKM | NA | 17 ± 3.7 | 1.0 ± 0.23 | NA | |||
HLM | 28 ± 6.5 | 1.4 ± 0.33 | |||||
Codeine | rUGT2B4 | 11 ± 2.7 | 0.47 ± 0.11 | 5.8 ± 1.2 | 0.22 ± 0.045 | ||
HKM | 55 ± 5.2 | 2.9 ± 0.27 | 39 ± 5.9 | 2.5 ± 0.37 | NA | ||
HLM | 13 ± 2.6 | 0.61 ± 0.13 | 8.0 ± 1.1 | 0.40 ± 0.058 | |||
AZT | rUGT2B7 | 33 ± 8.5 | 1.4 ± 0.36 | 21 ± 3.9 | 0.82 ± 0.15 | 49 ± 12 | 4.2 ± 1.1 |
HKM | 51 ± 12 | 2.6 ± 0.65 | 35 ± 3.5 | 2.2 ± 0.22 | 57 ± 7.5 | 6.9 ± 0.90 | |
HLM | 59 ± 6.6 | 2.8 ± 0.32 | 30 ± 4.1 | 1.5 ± 0.21 | 59 ± 8.6 | 5.5 ± 0.79 | |
Propofol | rUGT1A9 | 11 ± 3.0 | 0.45 ± 0.12 | 3.2 ± 0.52 | 0.12 ± 0.020 | 6.0 ± 0.75 | 0.51 ± 0.063 |
HKM | 12 ± 3.4 | 0.64 ± 0.18 | 5.5 ± 0.56 | 0.34 ± 0.035 | 7.5 ± 1.7 | 0.90 ± 0.20 | |
HLM | 30 ± 6.4 | 1.4 ± 0.31 | 19 ± 4.6 | 1.0 ± 0.24 | 31 ± 4.1 | 2.9 ± 0.38 | |
Furosemide | rUGT1A9 | 8.0 ± 0.47 | 0.33 ± 0.020 | 2.4 ± 0.66 | 0.090 ± 0.025 | 9.2 ± 2.1 | 0.78 ± 0.18 |
HKM | 10 ± 4.1 | 0.54 ± 0.22 | 3.6 ± 0.80 | 0.22 ± 0.049 | 15 ± 0.77 | 1.9 ± 0.092 | |
HLM | 32 ± 6.3 | 1.5 ± 0.30 | 29 ± 4.0 | 1.5 ± 0.20 | 34 ± 6.3 | 3.1 ± 0.58 | |
Acetaminophen | rUGT1A9 | 12 ± 3.7 | 0.49 ± 0.15 | 1.9 ± 0.29 | 0.073 ± 0.011 | 6.9 ± 0.54 | 0.59 ± 0.046 |
HKM | 15 ± 3.0 | 0.79 ± 0.16 | 3.8 ± 0.82 | 0.24 ± 0.05 | 21 ± 3.4 | 2.6 ± 0.41 | |
HLM | 29 ± 8.9 | 1.4 ± 0.43 | 12 ± 3.2 | 0.64 ± 0.16 | 30 ± 4.5 | 2.8 ± 0.96 |
IC50 values are presented as means ± S.D. of three independent experiments. IC50,u, binding-corrected IC50; NA, not analyzed.