Effect of P450 enzyme-specific inhibitors on SZ metabolism in HLM
Data are means ± S.D.
| Inhibitor | Inhibition | ||||||
|---|---|---|---|---|---|---|---|
| SZ | EMD 148107 | EMD 329989 | EMD 50929 | M203 | M364d | M362 | |
| % | |||||||
| Furafyllinea | 15.3 ± 0.6 | 7.1 ± 4.4 | 59.7 ± 6.5 | 36.9 ± 9.0 | 13.1 ± 1.9 | −0.4 ± 4.8 | 23.2 ± 16.7 |
| Pilocarpine | 8.5 ± 2.9 | 11.7 ± 6.1 | −13.2 ± 9.1 | 12.4 ± 10.0 | 4.3 ± 8.7 | −6.2 ± 6.6 | 11.5 ± 27.9 |
| Quercetin | 20.7 ± 3.3 | 8.8 ± 3.3 | 19.6 ± 2.9 | 52.4 ± 12.9 | 5.3 ± 4.6 | 30.0 ± 4.5 | −10.3 ± 35.0 |
| Sulfaphenazole | 4.4 ± 7.9 | 25.6 ± 5.5 | −4.6 ± 15.8 | 21 ± 15.7 | −8.2 ± 4 | −19.2 ± 6.9 | −17.2 ± 12.4 |
| S-Mephenytoin | −1.0 ± 3.8 | −5.5 ± 4.4 | −5.0 ± 4.4 | −5.7 ± 2.9 | −5.7 ± 6.9 | −15.4 ± 1.9 | −20.7 ± 12.4 |
| (+)-N-3-Benzylnirvanol | −3.0 ± 1.7 | −10.3 ± 9.2 | −5.9 ± 6.8 | 15.2 ± 8.7 | −13.8 ± 3.2 | −13.8 ± 12.3 | −10.3 ± 6.0 |
| Quinidine | 0.6 ± 8.7 | −9.2 ± 6.1 | −6.8 ± 9.5 | 7.6 ± 6.6 | −7.4 ± 18.5 | −7.5 ± 2.5 | −41.4 ± 15.0 |
| Diethyldithiocarbamatea | 3.5 ± 1.9 | −4.7 ± 2.9 | 16.1 ± 10.5 | 37.3 ± 9.5 | −10.0 ± 7.0 | −11.9 ± 8.2 | 10.1 ± 1.7 |
| Ketoconazole | 40.1 ± 4.3 | 4.0 ± 3.2 | −28.8 ± 3.6 | 70.5 ± 7.2 | 64.9 ± 2.8 | 33.8 ± 13.1 | 112 ± 11 |
↵a A 15-min preincubation before addition of substrate.