Table 1.
|
|
1′-OH Midazolam |
4-OH Midazolam |
||||
---|---|---|---|---|---|---|---|
Microsomes | Strain | Kma | Vmaxb | Vmax/Kmc | Kma | Vmaxb | Vmax/Kmc |
Liver | Cyp3a+/+ | 0.95 ± 0.18 | 630 ± 29 | 662 | 8.43 ± 0.27 | 224 ± 12.7 | 26.6 |
Cyp3a−/− | 6.38 ± 1.2 | 735 ± 11 | 115 | 17.5 ± 6.9 | 49.8 ± 5.0 | 2.36 | |
Human | 2.93 ± 0.33 | 2097 ± 155 | 715 | 38.7 ± 6.3 | 1226 ± 87 | 27.8 | |
Intestine | Cyp3a+/+ | 10.4 ± 1.8 | 62.3 ± 3.2 | 6.02 | 55.9 ± 2.0 | 38.0 ± 5.2 | 0.68 |
Cyp3a−/− | -d | -d | -d | -d | -d | -d | |
Human | 1.61 ± 0.04 | 596 ± 18 | 369 | 24.5 ± 3.3 | 330 ± 11 | 13.5 |
Km expressed in μM
Vmax expressed in pmol/min/mg protein
Vmax/Km expressed in μL/min/mg protein
No metabolite detected (detection limit <5 pmol/min/mg protein)