Table 1

Kinetic parameters of CBZ 10,11-epoxidation, SMAP formation, and AND 6β-hydroxylation by human liver microsomes

ParameterCBZ 10,11-Epoxidation1-aSMAP Formation from ZNS1-bAND 6β-Hydroxylation1-a
CBZ OnlyPlus ANDPlus ZNSZNS OnlyPlus CBZPlus ANDAND OnlyPlus CBZPlus ZNS
K m1 71.6 K m  = 268.763.0 K m  = 843.5 K m  = 1441.8 K m  = 24118.05.73.47.9
K m2 1384.41789.5537.6382.4455.6
V max2 4.2 V max  = 2.75.2 V max  = 3.7 V max  = 3.5 V max  = 5.812.87.611.4
V max/K m 0.004430.002430.00024

Substrate concentrations used were 15 to 500 μM for CBZ, 15 to 1000 μM for ZNS, and 15 to 300 μM for AND. The reactions were performed in the absence or presence of 100 μM effectors. Units of the constants are as follows: Km (apparent), micromolars; and Vmax, nanomoles per milligram per minute.

  • 1-a  Analyzed by the modified two-site equation (Vmax1 = 0) V = (Vmax2S2/Km1Km2)/(1 + S/Km1 +S2/Km1Km2) (Korezekwa et al., 1998)

  • 1-b  Analyzed by Michaelis-Menten equation V = Vmax/(1 + (Km/S))