Table 4

Kinetic parameters of acenocoumarol and warfarin hydroxylations in human liver microsomes (sample HD10)

SubstrateMetaboliteKmVmaxVmax/Km
μM pmol · min−1 · mg μl · min−1 · mg
(R)-AC4-a 6-OH 130.816.80.54
6-OH 24-b 11737.00.32
7-OH16.98.40.49
8-OH 1144.10.32
8-OH 24-b 507.30.15
(S)-AC6-OH0.4710.421.2
7-OH0.3512.636.0
8-OH0.601.22.0
(R)-W6-OH 164.04.80.07
6-OH 24-b 38022.60.06
7-OH85.45.30.06
(S)-W6-OH 12.50.790.32
6-OH 24-b 1967.20.04
7-OH2.11.80.86

The data are the mean of incubations in triplicate.

  • 4-a  AC, acenocoumarol; W, warfarin.

  • 4-b  Kinetic constants of the low affinity (high Km) reaction.