Table 2

Glucuronidation activity in expressed human UGT isoenzymes

UGT1A3UGT1A4UGT1A6UGT1A9
nmol/min/mg protein
4-Arylalkyl-1H-imidazoles
 LevomedetomidineN.D.0.009N.D.N.D.
 DetomidineN.D.0.014N.D.N.D.
 AtipamezoleN.D.0.007N.D.N.D.
Phenolic compounds
 4-NitrophenolN.M.N.M.5.87N.M.
 Scopoletin0.052N.M.N.M.N.M.
 EntacaponeN.M.N.M.N.M.4.22
Amines
 4-Aminobiphenyl0.0020.225N.D.0.031

UGT assays were conducted as described under Materials and Methods using 500 μM substrate concentration. All values represent an average of two determinations.

  • N.D., indicates that glucuronide formation was not detected (detection limit 0.8 pmol/min/mg of protein); N.M., not measured.