Table 7 Biotransformation of rac-F and rac-DHF in fresh liver homogenate.
From: The stereospecificity of flobufen metabolism in isolated guinea pig hepatocytes
incubation time (h) | activity nmol/mg protein | |||||
|---|---|---|---|---|---|---|
| Â | M-17203 | (2R;4S)-DHF | (2S;4R)-DHF | (2S;4S)-DHF | (2R;4R)-DHF | F |
| Â | substrate rac-F 0.5mM | |||||
1 | - | 11.1 ± 0.1 | 1.6 ± 0.1 | 3.9 ± 0.1 | 9.1 ± 0.2 | 89.2 ± 1.2 |
2 | - | 14.8 ± 0.1 | 3.2 ± 0.1 | 7.0 ± 0.1 | 16.0 ± 0.4 | 81.2 ± 1.2 |
4 | - | 18.3 ± 1.0 | 5.1 ± 0.3 | 7.7 ± 0.0 | 18.1 ± 0.4 | 69.5 ± 2.3 |
| Â | substrate rac-F 1.0 mM | |||||
1 | - | 14.2 ± 0.6 | 1.2 ± 0.0 | 4.5 ± 0.3 | 6.8 ± 0.3 | 138.4 ± 27.6 |
2 | - | 22.3 ± 0.6 | 2.9 ± 0.1 | 9.4 ± 0.3 | 15.1 ± 0.4 | 108.4 ± 5.8 |
4 | - | 30.7 ± 0.8 | 6.0 ± 0.2 | 10.5 ± 0.4 | 20.3 ± 0.5 | 106.4 ± 4.1 |
| Â | substrate rac-DHF 0.12 mM | |||||
1 | - | 5.4 ± 0.1 | 5.1 ± 0.1 | 5.7 ± 0.1 | 4.9 ± 0.1 | 0.3 ± 0.0 |
2 | - | 5.3 ± 0.2 | 5.5 ± 0.2 | 5.9 ± 0.3 | 5.1 ± 0.4 | 0.5 ± 0.1 |
4 | - | 5.4 ± 0.0 | 5.4 ± 0.0 | 4.7 ± 0.1 | 4.0 ± 0.0 | 1.1 ± 0.0 |
| Â | substrate rac-DHF 0.24 mM | |||||
1 | - | 12.2 ± 0.3 | 11.7 ± 0.3 | 12.5 ± 0.3 | 11.5 ± 0.3 | 0.6 ± 0.0 |
2 | - | 11.9 ± 0.2 | 11.9 ± 0.2 | 12.8 ± 0.2 | 11.8 ± 0.2 | 0.7 ± 0.1 |
4 | - | 12.1 ± 0.5 | 11.9 ± 0.5 | 11.4 ± 0.5 | 10.4 ± 0.5 | 2.0 ± 0.1 |