The inhibitory effect of (S,S)-reboxetine and (R,R)-reboxetine on specific CYP enzyme activities in cDNA expressed CYP microsomes
| P-450 Enzyme | Percent Metabolite Formation for Various P-450 Marker Substrates Compared with Control | |||
|---|---|---|---|---|
| (S,S)-Reboxetine (10 μM) | (S,S)-Reboxetine (100 μM) | (R,R)-Reboxetine (10 μM) | (R,R)-Reboxetine (100 μM) | |
| CYP1A2 | 100.1 ± 7.8% | 104.9 ± 13.6% | 87.7 ± 15.2% | 58.2 ± 9.4% |
| CYP2C9 | 98.6 ± 2.2% | 86.6 ± 2.2% | 97.7 ± 1.6% | 89.5 ± 0.9% |
| CYP2C19 | 82.8 ± 4.6% | 73.4 ± 4.4% | 96.2 ± 1.8% | 93.4 ± 2.1% |
| CYP2D6 | 44.1 ± 3.0% | 10.5 ± 4.5% | 70.1 ± 5.2% | 28.1 ± 10.2% |
| CYP2E1 | 108.9 ± 5.5% | 97.1 ± 4.9% | 97.1 ± 5.0% | 97.9 ± 4.2% |
| CYP3A4 | 56.2 ± 4.1% | 23.3 ± 6.2% | 62.6 ± 4.9% | 22.9 ± 5.5% |
Values are the mean ± S.D. of triplicate determinations. Incubation conditions and concentrations of CYP marker substrates are as described in Experimental Procedures.