Drug | UGT | P450 | ||||
---|---|---|---|---|---|---|
fu, mic | CLint, UGT | CLuint, UGT | fu, mic | CLint, P450 | CLuint, P450 | |
μl · min−1 · mg−1 | μl · min−1 · mg−1 | mg/ml | μl · min−1 · mg−1 | μl · min−1 · mg−1 | ||
Quercetin | 0.90a | 4620 ± 800b | 5133 | NT | N.D. | N.D. |
Raloxifene | 0.98 ± 0.11b | 2180 ± 60b | 2224 | 0.43 ± 0.06d | 8.90 ± 0.16d | 20.7 |
Bazedoxifene | 0.38 ± 0.05c | 166 ± 2c | 437 | 0.16 ± 0.01d | 4.70 ± 0.36d | 29.4 |
Diclofenac | 0.94 ± 0.05c | 59.0 ± 4.4c | 62.7 | N.T. | N.D. | N.D. |
Tolfenamic acid | 0.88 ± 0.10c | 155 ± 5c | 176 | N.T. | N.D. | N.D. |
Tolcapone | 0.39 ± 2c | 40.0 ± 0.5c | 103 | N.T. | N.D. | N.D. |
Entacapone | 1.00 ± 0.2c | 27.0 ± 3.8c | 27.0 | N.T. | N.D. | N.D. |
Telmisartan | 0.92 ± 0.05c | 20.0 ± 2.0c | 21.7 | N.T. | N.D. | N.D. |
Gemfibrozil | 0.97 ± 0.04c | 17.0 ± 2.1c | 17.5 | N.T. | N.D. | N.D. |
Etodolac | 1.1 ± 0.1d | 6.20 ± 0.86d | 5.7 | N.T. | N.D. | N.D. |
Indomethacin | 0.80 ± 0.06d | 4.20 ± 0.67d | 5.2 | N.T. | N.D. | N.D. |
N.T., not tested; N.D., no depletion.
↵a The fu, mic value of quercetin is cited from (Cubitt et al., 2009) because of degradation during equilibrium dialysis. Data are given as mean ± S.D.
↵b Microsomal protein concentration was 0.02 mg/ml.
↵c Microsomal protein concentration was 0.2 mg/ml.
↵d Microsomal protein concentration was 0.4 mg/ml.