TABLE 2

CLint of bufuralol in recombinant CYP2D6 at varying substrate and protein concentrations


[Bufuralol]

[Total Protein]

[rCYP2D6 Protein]

t1/2

CLint

[Bufuralol]

[Total Protein]

[rCYP2D6 Protein]

t1/2

CLint
μM mg/ml mg/ml min ml/min/mg μM mg/ml mg/ml min ml/min/mg
0.3 0.8 0.08 48.5 0.18 1.0 0.8 0.08 26.6 0.33
0.8 0.15 46.9 0.18 0.8 0.15 23.2 0.37
0.8 0.3 32.5 0.27 0.8 0.3 25.5 0.34
0.8 0.5 27.3 0.32 0.8 0.5 21.7 0.40
0.8 0.75 29.0 0.30 0.8 0.75 23.4 0.37
0.8 1.0 34.0 0.25 0.8 1.0 22.5 0.38
0.8 1.5 22.9 0.38 0.8 1.5 18.8 0.46

0.8
2.0
22.1
0.39

0.8
2.0
27.6
0.31