TABLE 1

Relative rates of CBZ β-D-glucuronide formation by human tissue microsomes and cloned/expressed UGTs The control substrates used to confirm activity at a concentration of 2 mM. All values are within the normal range expected for these substrates (Gaiser et al., 2003). Morphine glucuronidation rates for human tissues were included to give a better indication of relative UGT2B7 levels, although it should be noted that morphine is not exclusively a UGT2B7 substrate.


Source of UGT

UGT Activity

Probe Substrate

UGT Activity with Probe Substrate
pmol/mg/min pmol/mg/min
Human liver 3.2 1-Naphthol 4000
Morphine 520
Human kidney 0.45 1-Naphthol 3000
Morphine 140
Human intestine 0.32 1-Naphthol 1000
Morphine 135
1A1 (from V79) 0 Octylgallate 500
1A3 (from V79) 0 2-Aminobiphenyl 70
1A6 (from V79) 0 1-Naphthol 2500
1A9 (from V79) 0 Propofol 1000
2B4 (from V79) 0 Morphine 4.5
2B7 (from V79) 0.5 Morphine 350
1A4 (from baculovirus)
0
2-Aminobiphenyl
400