Victim Substrate | rP450 | Victim Depletion CLint,appa | fm,P450 (Hepatic Abundance Method) | ISEF Substrateb | V/K ISEF Valueb | fm,P450 (ISEF Method)b |
---|---|---|---|---|---|---|
Caffeine | 1A1 | 1.0c | 0.36 | N.D. | N.D. | N.D. |
2B11 | 0.27 | 0.28 | N.D. | N.D. | N.D. | |
2C21 | 0.11 | 0.35 | N.D. | N.D. | N.D. | |
Midazolam | 2B11 | 2.72 | 0.43 | Temazepam | 2.92 | 0.89 |
Midazolam | 1.68 | 0.91 | ||||
2C21 | 1.08 | 0.57 | Diclofenac | 0.89 | 0.11 | |
Midazolam | 0.38 | 0.08 | ||||
3A12 | 0.0035 | <0.001 | Midazolam | 5.46 | <0.01 | |
Midazolam | 5.46 | <0.01 | ||||
Temazepam | 2B11 | 0.78 | 0.78 | Temazepam | 1.68 | 0.95 |
Temazepam | 1.68 | 0.98 | ||||
2C21 | 0.067 | 0.22 | Diclofenac | 1.10 | 0.05 | |
Temazepam | 0.38 | 0.02 | ||||
Bufuralol | 2C21 | 3.09 | 0.56 | Diclofenac | 7.70 | 0.83 |
Bufuralol | 0.38 | 0.20 | ||||
2D15 | 2.45 | 0.44 | Bufuralol | 2.41 | 0.17 | |
Bufuralol | 2.41 | 0.80 |
N.D., not determined due to low caffeine turnover.
↵a μl/min/pmol P450.
↵b ISEFs and corresponding fm values were calculated using the kinetics of the actual victim substrate or an alternate substrate for each rP450 as described under Materials and Methods.
↵c Due to low caffeine turnover, the relative rate of paraxanthine formation normalized to CYP1A1 is shown.