Apparent Michaelis-Menten kinetic parameters of the formation of (+)- and (−)-9-hydroxyrisperidone in human liver microsomes
| Genotype | (+)-9-Hydroxylation | (−)-9-Hydroxylation | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Km1 | Vmax1 | CLint | Km2 | Vmax2 | CLint | Km | Vmax | CLint | ||
| HL-47 | 0.46 | 5.3 | 11.6 | 63 | 450 | 7.04 | 87.8 | 481 | 5.49 | |
| HL-49 | *1/*4 | —1-a | —1-a | —1-a | 41 | 189 | 4.61 | 101 | 328 | 3.25 |
| HL-51 | *1/*1 | —1-a | —1-a | —1-a | 50 | 224 | 4.50 | 181 | 376 | 2.08 |
| HL-54 | *1/*1 | 0.06 | 2.2 | 39.0 | 23 | 124 | 5.44 | 52 | 146 | 2.81 |
| HL-55 | *1/*1 | 0.12 | 1.8 | 14.6 | 30 | 270 | 8.88 | 103 | 323 | 3.14 |
| HL-67 | *1*/4 | 0.41 | 14.7 | 35.5 | 49 | 460 | 9.43 | 91.6 | 602 | 6.57 |
| Mean ± S.D. | 0.26 ± 0.18 | 6.0 ± 5.2 | 25.2 ± 12.2 | 42 ± 14 | 286 ± 139 | 6.65 ± 2.15 | 109 ± 42.5 | 376 ± 155 | 3.89 ± 1.74 | |
Km is expressed as micromolar,Vmax as formed metabolite per minute and per milligram of microsomal protein, and CLint as microliters per minute per milligram of microsomal protein.
↵1-a Monophasic Eadie-Hofstee plot.