UGT Source | Entacapone Activity | Tolcapone Activity | Control Activity | |||
---|---|---|---|---|---|---|
50 μM | 2 mM | 50 μM | 2 mM | Substrate (500 μM) | 2 mM | |
nmol min−1mg−1 | nmol min−1 mg−1 | nmol min−1 mg−1 | ||||
UGT1A1 | 0.002 | 0.036, 0.0261-a | N.D. | N.D. | Octylgallate | 0.81 |
UGT1A6 | N.D. | N.D. | N.D. | N.D. | 1-Naphthol | 1.4 |
UGT1A9 | 0.17 | 1.3 | 0.010 | 0.73 | Propofol | 0.78 |
UGT2B7 | 0.006 | 0.073 | 0.002 | 0.034 | 4-Hydroxyestrone | 0.45 |
UGT2B15 | 0.003 | 0.045 | 0.001 | N.D. | 8-Hydroxyquinoline | 0.36 |
HLM | 0.14 | 2.0 | 0.008 | 0.69 | ||
HKM | 0.08 | 2.3 | 0.015 | 0.76 |
N.D., not detectable; HLM, human liver microsomes; HKM, human kidney microsomes.
↵1-a Two peaks detected.