Table 1. Kinetic parameters for morphine-3-glucuronide and morphine-6-glucuronide catalyzed by UGT2B7*N single recombinant allozymes.
| UGT2B7*N |
Km (μmol/L) |
Vmax (pmol·min−1·mg−1 protein) |
CLint (μL·min−1·mg−1 protein) |
CLint (M3G)/ CLint (M6G) | % of 2B7*1HA |
||||
|---|---|---|---|---|---|---|---|---|---|
| M3G | M6G | M3G | M6G | M3G | M6G | M3G | M6G | ||
| UGT2B7*1-HA | 33.93±9.004 | 55.10±12.40 | 358.7±31.12 | 324.4±28.26 | 10.57 | 5.887 | 1.795 | 100.0 | 100.0 |
| UGT2B7*1-CFP | 29.78±5.759 | 42.49±6.399* | 328.7±19.85 | 282.0±15.02 | 11.04 | 6.637 | 1.663 | 104.4 | 112.7 |
| UGT2B7*71S-HA | 36.06±8.092 | 66.07±16.66* | 494.5±37.06 | 337.6±35.12 | 13.71 | 5.110 | 2.683 | 129.7 | 86.80 |
| UGT2B7*71S-CFP | 32.29±6.169 | 54.43±9.753 | 429.3±26.35 | 421.8±29.15 | 13.30 | 7.749 | 1.716 | 125.8 | 131.6 |
| UGT2B7*2-HA | 64.41±11.14** | 75.81±12.30** | 1772±125.3** | 1522±106.9** | 27.51** | 20.08* | 1.370 | 260.3 | 341.1 |
| UGT2B7*2-CFP | 57.55±9.407** | 71.75±11.81** | 1444±92.77** | 1486±103.8** | 25.09** | 20.71* | 1.211 | 237.4 | 351.8 |
| UGT2B7*5-HA | 23.28±3.728** | 28.70±4.436** | 1769±81.07** | 1525±72.68** | 75.99** | 53.14** | 1.430 | 718.9 | 902.7 |
| UGT2B7*5-CFP | 17.29±2.855** | 20.10±4.250** | 1718±72.90** | 1604±92.04** | 99.36** | 79.80** | 1.245 | 940.0 | 1356 |
Kinetics analysis of common SNPs of UGT2B7 mediate the glucuronide metabolism of morphine. Data are the mean±SD of three independent determinations, the asterisks indicate differences that are statistically significant compared to 2B7*1HA (*P<0.05; **P<0.01).