Kinetic parameters of nor-VER, D617, M1, M2, M3, and M4 metabolites in human CYP3A4. The values are expressed as mean of three and S.D.
Parameters | R-(+)- or S-(-)-VER | Metabolite | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| nor-VER | D617 | M1 | M2 | M3 | M4 | |||||||
| Km1 (μM) | R | 4.24 ± 1.33 | 2.26 ± 3.13 | 1.25 ± 1.40 | 3.49 ± 1.83 | 9.03 ± 9.34 | 4.46 ± 2.11 | |||||
| S | 4.85 ± 0.55 | 3.48 ± 0.45 | 4.73 ± 2.63 | 3.23 ± 1.81 | 5.90 ± 0.76 | 3.52 ± 1.01 | ||||||
| Vmax1 (pmol/min/mg) | R | 486 ± 105 | 140 ± 151 | 1.21 ± 0.73 | 2.29 ± 0.76 | 8.75 ± 9.47 | 5.00 ± 1.16 | |||||
| S | 995 ± 61 | 403 ± 29 | 7.29 ± 3.37 | 6.56 ± 2.81 | 3.80 ± 0.28 | 6.04 ± 1.06 | ||||||
| Km2 (μM) | R | 102 ± 41 | 21.7 ± 10.5 | 43.4 ± 6.5 | 63.6 ± 12.9 | 59.0 ± 66.4 | 180 ± 38 | |||||
| S | 96.8 ± 12.8 | 101.9 ± 28.1 | 45.5 ± 21.9 | 37.8 ± 17.3 | 156 ± 29 | 69.0 ± 14.2 | ||||||
| Vmax2 (pmol/min/mg) | R | 2479 ± 526 | 813 ± 92 | 14.5 ± 0.6 | 8.27 ± 0.65 | 9.92 ± 8.95 | 22.2 ± 1.0 | |||||
| S | 2929 ± 187 | 641 ± 83 | 11.0 ± 3.1 | 10.6 ± 2.6 | 4.79 ± 0.21 | 11.9 ± 0.9 | ||||||
| a | R | 0.611 ± 0.376 | 0.674 ± 0.260 | NA | NA | NA | NA | |||||
| S | 0.493 ± 0.056 | NA | NA | NA | NA | NA | ||||||
| b | R | 0.066 ± 0.055 | 0.402 ± 0.544 | NA | NA | NA | NA | |||||
| S | 0 | 0.107 ± 0.081 | NA | NA | NA | NA | ||||||
| c | R | 958 ± 1928 | 42.2 ± 316.2 | NA | NA | NA | NA | |||||
| S | 2066 ± 1537 | ∞ | NA | NA | NA | NA | ||||||
| d | R | 294 ± 132 | 2369 ± 4435 | NA | NA | NA | NA | |||||
|
|
S
| 560 ± 84 | 584 ± 267 | NA | NA | NA | NA | |||||
NA, not applicable.