TABLE 4

Covalent binding of [14C]elzasonan (10 μM) to liver microsomes under various conditions

Data are presented as means ± S.D. Means represent three replicates.

MicrosomesConditionCovalent Binding
pmol [14C]elzasonan Eq bound/mg microsomal protein
Human− NADPH6.96 ± 0.39
+ NADPH191 ± 10
+ NADPH, + GSH (5 mM)91.0 ± 10.6
+ NADPH, + KCN (0.1 mM)165 ± 29
+ NADPH, + lysine (1.0 mM)185 ± 16
+ NADPH, + ketoconazole (1.0 μM)27.5 ± 2.7
+ NADPH, + cytosol (3 mg/ml)176 ± 47
+ NADPH, acid precipitation54.8 ± 6.7
Rat+ NADPH33.6 ± 7.8
Dog+ NADPH95.6 ± 13.9