Microsomes | 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 | |||||||
Control | Cyp3a(−/−)Tg-3A4Hep | 77.2 ± 3.75 | 1320 ± 34.4 | 17.1 | 343 ± 33.8 | 3366 ± 243 | 9.81 |
Gefitinib | Cyp3a(−/−)Tg-3A4Hep | 22.5 ± 1.46 | 2602 ± 60.2 | 115 | 502 ± 34.1 | 1677 ± 38.1 | 3.34 |
Intestine | |||||||
Control | Cyp3a(−/−)Tg-3A4Int | 22.5 ± 1.72 | 349 ± 6.18 | 15.5 | 277 ± 80.9 | 1089 ± 207 | 3.93 |
Gefitinib | Cyp3a(−/−)Tg-3A4Int | 8.23 ± 0.74 | 812 ± 12.0 | 98.6 | 1329 ± 131 | 1265 ± 97.0 | 0.95 |