TABLE 1

Kinetic parameters of denopamine glucuronidation in microsomes obtained from humans and experimental animals, and recombinant UGT2B7

Denopamine was incubated with microsomes and UDP-glucuronic acid for 30 min (10 min in the case of rat and rabbit liver microsomes). The kinetic parameters were calculated with GraphPad Prism software. Each value represents best-fit values ± S.E. of triplicate points.


Source of UGT

Km

Vmax

Vmax/Km
G1
G2
G1
G2
G1
G2
mM nmol/min/mg protein μl/min/mg protein
Rat livera 0.0022 ± 0.0003 2.68 ± 0.07 1220
Rabbit livera 0.018 ± 0.003 2.77 ± 0.12 152
Dog liverb 10.18 ± 0.61 3.51 ± 0.14 21.83 ± 0.99 5.68 ± 0.13 2.14 1.62
Monkey liverb 3.91 ± 0.13 1.84 ± 0.07 7.65 ± 0.15 6.25 ± 0.11 1.96 3.40
Human liverb 2.87 ± 0.17 7.29 ± 0.23 2.54
Human jejunumb 2.99 ± 0.30 1.17 ± 0.06 0.39
UGT2B7b

1.48 ± 0.05

3.58 ± 0.06

2.43
  • a The denopamine concentration ranged from 0.78 to 200 μM, and microsomal protein was 0.1 mg/ml.

  • b The denopamine concentration ranged from 15.6 to 4000 μM, and microsomal protein was 0.5 mg/ml.