MDA Formation | DHEA Formation | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Vmax | Km | Vmax/Km | Vmax | Km | Vmax/Km | ||||||
R,S-MDEA | CYP1A2 | 19 ± 0.6 | 91 ± 11 | 0.21 | ND | ND | ND | ||||
CYP2B6 | 23 ± 0.8 | 124 ± 17 | 0.19 | ND | ND | ND | |||||
CYP2C19 | 22 ± 0.9 | 110 ± 17 | 0.20 | 3.0 ± 0.1 | 54 ± 7 | 0.06 | |||||
CYP2D6 | 3.3 ± 0.4* | 4.6 ± 1.9* | 0.72 | 9.2 ± 0.5 | 2.8 ± 0.9 | 3.29 | |||||
CYP3A4 | 2.4 ± 0.4* | 10 ± 4.8* | 0.24 | 0.8 ± 0.1* | 45 ± 16* | 0.02 | |||||
R-MDEA (racemic MDEA) | CYP1A2 | 10 ± 0.4 | 65 ± 11 | 0.15 | ND | ND | ND | ||||
CYP2B6 | 12 ± 0.5 | 82 ± 13 | 0.15 | ND | ND | ND | |||||
CYP2C19 | 10 ± 0.5 | 126 ± 6 | 0.08 | ND | ND | ND | |||||
CYP2D6 | 3.2 ± 0.2* | 6.5 ± 0.6* | 0.49 | 4.4 ± 0.3 | 2.0 ± 0.6 | 2.20 | |||||
CYP3A4 | 2.1 ± 0.2* | 16 ± 2.4* | 0.13 | 0.4 ± 0.2* | 21 ± 5* | 0.02 | |||||
S-MDEA (racemic MDEA) | CYP1A2 | 9.0 ± 0.4 | 32 ± 6 | 0.28 | ND | ND | ND | ||||
CYP2B6 | 11 ± 0.7 | 53 ± 15 | 0.21 | ND | ND | ND | |||||
CYP2C19 | 12 ± 0.4 | 31 ± 19 | 0.39 | 2.9 ± 0.3 | 25 ± 8 | 0.12 | |||||
CYP2D6 | 2.2 ± 0.2* | 11 ± 0.2* | 0.20 | 4.8 ± 0.3 | 1.0 ± 0.3 | 4.80 | |||||
CYP3A4 | 3.8 ± 0.3* | 18 ± 1.7* | 0.21 | 0.3 ± 0.08* | 13 ± 4* | 0.02 | |||||
R-MDEA (single enantiomers) | CYP1A2 | 13 ± 0.5 | 179 ± 21 | 0.07 | ND | ND | ND | ||||
CYP2B6 | 18 ± 1.2 | 115 ± 34 | 0.16 | ND | ND | ND | |||||
CYP2C19 | 15 ± 0.4 | 187 ± 19 | 0.08 | 2.4 ± 0.1 | 139 ± 20 | 0.02 | |||||
CYP2D6 | 2.5 ± 0.5* | 3.6 ± 2.7* | 0.69 | 9.3 ± 0.2 | 1.4 ± 0.2 | 6.64 | |||||
CYP3A4 | 13 ± 2.0* | 76 ± 18* | 0.17 | 1.1 ± 0.08* | 38 ± 7* | 0.03 | |||||
S-MDEA (single enantiomers) | CYP1A2 | 16 ± 0.8 | 126 ± 21 | 0.13 | ND | ND | ND | ||||
CYP2B6 | 19 ± 0.8 | 99 ± 20 | 0.19 | ND | ND | ND | |||||
CYP2C19 | 8.7 ± 1.5* | 1.8 ± 0.9* | 4.83 | 3.3 ± 0.1 | 18 ± 2.8 | 0.18 | |||||
CYP2D6 | 5.1 ± 0.3 | 20 ± 5 | 0.26 | 9.5 ± 0.1 | 0.7 ± 0.07 | 13.57 | |||||
| CYP3A4 | 3.2 ± 0.4* | 7.3 ± 2.5* | 0.44 | 0.7 ± 0.2* | 36 ± 8* | 0.02 |
ND, not determined.
↵* Kinetic data estimated according to eq. 2.