Microsome, Strain | 1′-OH Triazolam | 4-OH Triazolam | ||||
---|---|---|---|---|---|---|
Km | Vmax | Vmax/Km | Km | Vmax | Vmax/Km | |
μM | pmol/min/mg protein | μl/min/mg protein | μM | pmol/min/mg protein | μl/min/mg protein | |
Liver | ||||||
Wild-type | 11.7 ± 1.96 | 742 ± 16.4 | 63.5 | 124 ± 12.9 | 956 ± 75.1 | 7.74 |
Cyp3a(−/−) | 73.3 ± 18.8a | 115 ± 14.2a | 1.56 | 53.1 ± 1.32 | 27.6 ± 1.05 | 0.52 |
Cyp3a(−/−)Tg-3A4Hep | 58.4 ± 8.46 | 2145 ± 124 | 36.8 | 406 ± 80.0 | 6485 ± 907 | 16.0 |
Cyp3a(−/−)Tg-3A4Int | 40.1 ± 2.73a | 56.5 ± 3.14a | 1.41 | 72.9 ± 8.22 | 18.0 ± 0.99 | 0.25 |
Human | 37.2 ± 3.27 | 1156 ± 42.2 | 31.1 | 168 ± 26.1 | 2070 ± 124 | 12.3 |
Intestine | ||||||
Wild-type | b | b | b | b | ||
Cyp3a(−/−) | c | c | c | c | ||
Cyp3a(−/−)Tg-3A4Hep | c | c | c | c | ||
Cyp3a(−/−)Tg-3A4Int | 38.5 ± 4.04 | 194 ± 5.87 | 5.05 | 510 ± 27.6 | 894 ± 28.7 | 1.75 |
Human | 53.7 ± 3.01 | 847 ± 19.6 | 15.8 | 345 ± 40.8 | 2439 ± 215 | 7.07 |