50分別為7.07、0.40、2.82 μmol/L,對其他4個酶(CYP1A2、CYP2D6、CYP2C9和CYP2C19)的IC50均大于10 μmol/L。結(jié)論 3種化合物對CYP3A4活力均有抑制作用,其中ML-4000的抑制能力最強。3種化合物對其他4個酶基本沒有抑制作用。;Objective To investigate the inhibition of ML-3000 and two NO donor derivatives in pyrrolizine on five human cytochrome P450 isozymes CYP2D6, CYP1A2, CYP2C9, CYP2C19, and CYP3A4. Methods Inhibition of ML-3000, ML-4000, and ML-5000 on five human cytochrome P450 isozymes CYP2D6, CYP1A2, CYP2C9, CYP2C19, and CYP3A4 was determined with High Throughput Inhibitor Sceening Kit. Results IC50 values of ML-3000, ML-4000, and ML-5000 to CYP3A4 were 7.07, 0.40, and 2.82 μmol/L, respectively. IC50 values of ML-3000, ML-4000, and ML-5000 to others were more than 10 μmol/L. Conclusion Three compounds have the inhibitory effects on CYP3A4. Among them, ML-4000 has the strongest inhibition. The three compounds show no inhibition on the other four enzymes."/> 50;cytochrome P450; NO donor compound; IC50"/>

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首頁 > 過刊瀏覽>2013年第36卷第4期 >2013,36(4):249-252
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吡咯里嗪類非甾體抗炎藥ML-3000衍生物對人P450同工酶的體外抑制作用

In vitro inhibition of ML-3000 derivatives in non-steroidal anti-inflammatory drugs of pyrrolizine on human cytochrome P450 isozymes

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