Involvement of CYP3A4 in the metabolism of bromperidol in vitro.
Involvement of CYP3A4 in the metabolism of bromperidol in vitro.
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CYP3A4 参与溴哌啶醇的体外代谢。
DOI：
10.1034/j.1600-0773.2000.d01-27.x
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发表时间：
2000
期刊：
影响因子：
--
通讯作者：
Y. Inoue
中科院分区：
文献类型：
--
作者：
S. Sato;T. Someya;O. Shioiri;T. Koitabashi;Y. Inoue
在本研究中，使用细胞系中表达的人细胞色素P450同工酶（CYP 1A 2、CYP 2C 19、CYP 2D 6和CYP 3A 4）来阐明其在溴哌利多代谢中的作用。我们发现，CYP 3A 4催化溴哌利多及其代谢产物，还原溴哌利多的N-脱烷基化。CYP 3A 4还催化溴哌利多脱水为溴哌利多1，2，3，6-四氢吡啶，将溴哌利多代谢为溴哌利多吡啶盐，并催化还原的溴哌利多氧化回溴哌利多。CYP 1A 2、CYP 2C 19和CYP 2D 6不催化这些反应。
In this study, human cytochrome P450 isoenzymes (CYP1A2, CYP2C19, CYP2D6, and CYP3A4) expressed in a cell line were used to elucidate their roles in the metabolism of bromperidol. We found that CYP3A4 catalyzes the N-dealkylation of bromperidol and its metabolite, reduced bromperidol. CYP3A4 also catalyzes the dehydration of bromperidol to bromperidol 1,2,3,6-tetrahydropyridine, metabolizes bromperidol to bromperidol pyridinium, and catalyzes the oxidation of reduced bromperidol back to bromperidol. CYP1A2, CYP2C19, and CYP2D6 do not catalyze these reactions.