Nonspecific binding of bufuralol fluoxetine, ezlopitant, imipramine, and quinidine to Sf9 cell microsomes and phospholipid
Unbound Fraction | |||||
---|---|---|---|---|---|
Bufuralol | Fluoxetine | Ezlopitant | Imipramine | Quinidine | |
Microsomal protein concentration (mg/ml) | |||||
0.2 | 0.91 | 0.16 | 0.041 | 0.47 | 0.80 |
0.5 | 0.58 | 0.051 | 0.016 | 0.34 | 0.63 |
2.0 | 0.44 | 0.025 | 0.0029 | 0.23 | 0.46 |
Phospholipid concentration (mg/ml) | |||||
0.2 | 0.78 | 0.14 | 0.023 | 0.43 | 0.75 |
0.5 | 0.65 | 0.099 | 0.0039 | 0.38 | 0.46 |
2.0 | 0.30 | 0.061 | 0.00033 | 0.15 | 0.31 |
The extent of binding for bufuralol, quinidine, and imipramine was minimal in the absence of additional microsomal protein or phospholipid. The unbound fractions for fluoxetine and ezlopitant at 8.8 μg/ml were 0.68 and 0.05, respectively.