TABLE 1

IC₅₀ values (µM) of cannabinoids against major hepatic UGT enzymes in microsomes from recombinant UGT–overexpressing cells, HLMs, or HKMs.

Probe substrate	Microsomes	THC		CBD		CBN
		IC₅₀	IC_50,u	IC₅₀	IC_50,u	IC₅₀	IC_50,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. IC_50,u, binding-corrected IC₅₀; NA, not analyzed.