Substrate | UGT2B7Y | UGT2B7H |
---|---|---|
Glucuronidation Rate pmol/min/mg protein | Glucuronidation Rate pmol/min/mg protein | |
Morphinan Derivatives | ||
Normorphine | 80 ± 7 | 0, 3 |
Norcodeine | 29, 24 | 5, 22 |
(−) Morphine | 3304 ± 90 | 2152, 2580 |
3-Glucuronide formation | ||
(−) Morphine | 415 ± 8 | 384, 388 |
6-Glucuronide formation | ||
Oxymorphone | 2300 ± 125 | 3139, 2944 |
Hydromorphone | 1550 ± 120 | 1028, 1118 |
Dihydromorphine | 530 ± 120 | 617, 856 |
Levorphanol | 25, 33 | 0, 19 |
Codeine | 114 ± 10 | 54, 80 |
Naloxone | 3400 ± 340 | 3462, 2908 |
Nalorphine | 3400 ± 700 | 1051, 1483 |
Naltrexone | 1050 ± 120 | 670, 662 |
Nalmefene | 625 ± 110 | 380, 412 |
Naltrindole | 453 ± 75 | 349, 456 |
Naltriben | 150, 97 | 0, 0 |
Nalbuphine | 1100 ± 110 | 862, 758 |
Oripavine derivatives | ||
Norbuprenorphine | 90 ± 11 | 0, 45 |
Buprenorphine | 280 ± 23 | 280, 478 |
Diprenorphine | 384 ± 34 | 180, 257 |
Membrane preparations of HK293 cells stably expressing either UGT2B7Y or H were used. The assays were performed as described in the Method section. Values represent mean rates ± SEM using membranes from three different passages of cultured cells or two passages are shown. The aglycone concentrations ranged from 0.25 mM to 5 mM, concentrations which evoked rates approaching Vmax.