Binding of compounds in both microsomal and hepatocyte incubations
Substrate | [Microsomal Protein] | fumic | [Hepatocyte] | Kp | fuinc | Reference |
|---|---|---|---|---|---|---|
| mg/ml | 1 × 106 cells/ml | |||||
| S-Mephenytoin | 1 | 1 | 0.75 | 1a | Unpublished observations | |
| Tolbutamide | 0.5 | 1 | 0.5 | 1.1 | 0.99 | Carlile et al., 1999 |
| Diclofenac | 0.1 | 1 | 0.25 | 22 | 0.97 | Obach et al., 1999; unpublished observations |
| S-Warfarin | 1 | 0.9 | 1 | 15 | 0.93 | Obach et al., 1999; unpublished observations |
| Nifedipine | 0.25 | 0.85 | 0.25 | 0.85a | Unpublished observations | |
| Quinidine | 0.5 | 0.77 | 0.25 | 150 | 0.84 | Brown, 2004 |
| Testosterone | 0.5 | 0.71 | 0.1 | 0.93a | Unpublished observations | |
| Dextromethorphan | 0.5 | 0.68b | 1 | 50b | 0.8 | Witherow and Houston, 1999 |
| Bufuralol | 0.5 | 0.58 | 0.75 | 0.48a | Margolis and Obach, 2003 | |
| Terfenadine | 0.25 | 0.04 | 0.1 |
| 0.1a |
Baba et al., 2002
|
↵ a Values calculated using eq. 1 assuming binding at 1 mg/ml microsomal protein is equivalent to binding at 1 × 106 cells/ml (Austin et al., 2005).
↵ b Binding data obtained using rat microsomes and hepatocytes.