Table 2

Apparent kinetic parameters for the N-glucuronidation of 1-substituted imidazole substrates by human UGT1A4 expressed in baculovirus-infected insect cells

1-Substituted ImidazolesKmVmaxVmax/ Km
mM nmol/min/mg μl/min/mg
1-Phenyl ( 1a )3.15  ± 0.320.33  ± 0.010.11  ± 0.01
1-Benzyl ( 1b )2.48  ± 0.440.35  ± 0.030.14  ± 0.02
1-(4-Methoxyphenyl) ( 1d )0.70  ± 0.060.31  ± 0.020.45  ± 0.01
1-(4-Chlorophenyl) ( 1e )0.67  ± 0.050.29  ± 0.010.43  ± 0.02
1-(4-Bromophenyl) ( 1f )0.18  ± 0.020.17  ± 0.010.95  ± 0.14
1-(4-Trifluoromethyl) ( 1g )0.32  ± 0.010.16  ± 0.010.50  ± 0.03

Data are given as mean ± S.D. of three determinations, each carried out in duplicate.