Table 1

Determination of the relative contribution of CYP2C19, CYP2D6, and CYP1A2 to bufuralol 1′ hydroxylation in human liver using recombinant data

rCYPP-450 ContentApparentKmVmaxCYP Content in Human Liver MicrosomesCLint (Vmax/Km)Abundance-AdjustedCLint
pmol/mg μM nmol/min/nmol P-450 pmol/mg ml/min/nmol P-450 %
CYP2C19323636.9191.025
CYP2D6123.41281037.795
CYP1A2391764.56450.03<1

Method: Data previously generated for CYP2C19, CYP2D6, and CYP1A2 with bufuralol was recalculated on a nmol P-450 basis, and intrinsic clearances were then calculated.

  • 2-a Rates normalized with respect to specific content of each CYP present immunochemically in human liver microsomes (Rodrigues, 1999).