TABLE 2

Kinetic parameters for propranolol metabolite formation

Kinetic constants were determined over the concentration ranges 1 to 100 μM (CYP2D6) or 50 to 2000 μM (CYP2C9 preparations).


Enzyme

4-Hydroxy-propranolol

Desisopropyl-propranolol
KM
Vm
KM
Vm
μM min-1 μM min-1
CYP2D6 22 ± 7 66 ± 11 14 ± 6 5 ± 0.07
CYP2C9 >900 <0.5 >150 <0.5
R108E >900 <0.5 >150 <0.5
R108E/D293N
>900
<0.5
>150
<0.5