Table 1

Amitriptyline binding to human liver microsomes and microsomes from human B-lymphoblastoid cells or insect cells

MatrixProtein ConcentrationFree Fraction
μg/ml
Pooled human liver microsomes501.075
1000.878
2000.629
5000.324
Pooled human liver microsomes (heat-inactivated)2000.502
Lymphoblast microsomes2500.816
5000.55
10000.257
Insect cell microsomes2500.675
Buffer (control)1.192

Values are unbound fractions determined at a spiked drug concentration of 50 μg/ml.