Treatment | Pathway | Microsomes1-a | Hepatocytes1-b | ||||
---|---|---|---|---|---|---|---|
Vmax | KM | CLint | Vmax | KM | CLint | ||
nmol/min | μM | μl/min | nmol/min | μM | μl/min | ||
DEX | 4′-HDZ | 0.23 ± 0.07 | 11 ± 8 | 26.0 ± 10.4 | 0.19 ± 0.03 | 7 ± 3 | 33.4 ± 19.1 |
3-HDZ | 14.68 ± 1.70** | 39 ± 9* | 395.0 ± 136.3** | 3.45 ± 0.72** | 23 ± 3** † | 157.5 ± 49.2** | |
NDZ | 1.26 ± 0.22* | 23 ± 6* | 58.8 ± 25.2* | 0.33 ± 0.06* | 14 ± 4** | 24.8 ± 8.0** | |
PB | 4′-HDZ | 0.13 ± 0.04 | 7 ± 2 | 22.9 ± 17.8 | 0.17 ± 0.04 | 9 ± 3* | 20.4 ± 4.3** |
3-HDZ | 7.81 ± 1.18** | 135 ± 27 | 58.5 ± 3.2** | 4.67 ± 0.86** | 65 ± 19† | 73.2 ± 10.5** | |
NDZ | 2.70 ± 0.73** | 54 ± 9* | 50.7 ± 14.9** | 1.48 ± 0.19** | 56 ± 13* | 26.7 ± 2.7** | |
UT1-c | 4′-HDZ | 0.16 ± 0.07 | 5 ± 2 | 39.9 ± 27.6 | 0.20 ± 0.05 | 3 ± 1 | 57.9 ± 9.1 |
3-HDZ | 2.29 ± 0.64 | 119 ± 32 | 19.1 ± 0.8 | 1.19 ± 0.21 | 71 ± 11† | 17.3 ± 4.5 | |
NDZ | 0.78 ± 0.15 | 35 ± 5 | 22.3 ± 1.9 | 0.25 ± 0.02 | 35 ± 5 | 7.1 ± 1.1 |
Data are presented as means ± SD (N = 4). Mean from induced states significantly different from UT (* p < 0.05, ** p < 0.01). Hepatocyte KM significantly different from microsomal KM (
dagger; p < 0.05).
↵1-a Vmax andCLint are expressed per milligram of microsomal protein.
↵1-b Vmax andCLint are expressed per million cells.
↵1-c Data from Zomorodi et al. (9).