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Transformation of Amoxapine byCunninghamella elegans

机译:秀丽隐杆线虫对阿莫沙平的转化

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We examined Cunninghamella elegans to determine its ability to transform amoxapine, a tricyclic antidepressant belonging to the dibenzoxazepine class of drugs. Approximately 57% of the exogenous amoxapine was metabolized to three metabolites that were isolated by high-performance liquid chromatography and were identified by nuclear magnetic resonance and mass spectrometry as 7-hydroxyamoxapine (48%),N-formyl-7-hydroxyamoxapine (31%), andN-formylamoxapine (21%). 7-Hydroxyamoxapine, a mammalian metabolite with biological activity, now can be produced in milligram quantities for toxicological evaluation.
机译:我们检查了秀丽线虫以确定其转化阿莫沙平的能力,阿莫沙平是一种属于三苯并二氮杂pine类药物的三环抗抑郁药。约57%的外源阿莫沙平被代谢为三种代谢物,这些代谢物通过高效液相色谱法分离,并通过核磁共振和质谱鉴定为7-羟基阿莫沙平(48%),N-甲酰基-7-羟基阿莫沙平( 31%)和N-甲拉莫沙平(21%)。 7-羟莫沙平是一种具有生物活性的哺乳动物代谢产物,目前可以毫克量生产用于毒理学评估。

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