Catalytic activities of expressed CYP2D isoforms toward S (+) - and R (−) -mianserin
| Substrate | CYP2D | Activity | |||
|---|---|---|---|---|---|
| 8-Hydroxylation | N-Demethylation | N-Oxidation | M1 | ||
| nmol/min/nmol P-450 | |||||
| 2D1 | 1.50 ± 0.12 | 1.36 ± 0.17 | 0.38 ± 0.04 | N.D. | |
| 2D2 | 2.53 ± 0.22 | N.D. | N.D. | N.D. | |
| R(−) mianserin | 2D3 | 1.33 ± 0.15 | 7.50 ± 0.33 | N.D. | N.D. |
| 2D4 | 4.03 ± 0.20 | 8.38 ± 0.28 | N.D. | 0.99 ± 0.12 | |
| 2D6 | 1.48 ± 0.12 | 2.37 ± 0.21 | N.D. | 0.35 ± 0.06 | |
| 2D1 | 0.08 ± 0.02 | 1.00 ± 0.14 | N.D. | N.D. | |
| 2D2 | 1.67 ± 0.11 | 0.76 ± 0.11 | N.D. | N.D. | |
| S (+) mianserin | 2D3 | 1.73 ± 0.18 | 14.42 ± 2.25 | N.D. | N.D. |
| 2D4 | 0.37 ± 0.08 | 5.80 ± 0.35 | N.D. | 0.25 ± 0.04 | |
| 2D6 | 2.32 ± 0.17 | 0.33 ± 0.03 | N.D. | N.D. | |
Each value represents the mean ± S.D. of three determinations. Amount of M1 is calculated by using calibration curve for 8-hydroxymianserin. Each substrate concentration is 100 μM.
N.D., not detected.