Estimates of Michaelis-Menten parameters for oxymorphone formation and the competitive Ki for quinidine.
Values in parentheses represent the 95% confidence intervals of the regression estimates.
Liver Microsomes | Km1 | Vmax1 | E1 a | E2 | Ki | CYP2D6 Contentb | |
|---|---|---|---|---|---|---|---|
| μM | pmol/mg/min | μl/mg/min | nM | pmol/mg | |||
| Xenotech | 113 | 92 | 0.81 | 0.17 | 26.7 | ||
| (63—163) | (55—128) | (0.14—0.21) | (17.2—36.2) | ||||
| HLM141 | 149 | 356 | 2.39 | 0.63 | 12.9 | 40 | |
| (102—210) | (237—475) | (0.5—0.8) | (7.5—18.4) | ||||
| HLM146 | 178 | 115 | 0.64 | 0.09 | 8.3 | 10 | |
| (98—258) | (63—166) | (0.04—0.13) | (2.0—14.7) | ||||
| HLM148 | 114 | 156 | 1.37 | 0.15 | 11.2 | 10 | |
| (59—179) | (101—211) | (0.12—0.18) | (6.5—15.9) | ||||
| HLM153 | 98 | 89 | 0.91 | 0.16 | 7.9 | ||
| (67—130) | (64—114) | (0.13—0.19) | (5.2—10.7) | ||||
| Mean ± S.D. | 130 ± 33 | 161 ± 112 | 1.2 ± 0.7 | 0.21 ± 0.22 | 13.4 ± 7.7 |
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