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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Kammerer R C, Schmitz D A

Department of Pharmacology, University of California, Los Angeles 90024-1735.

Xenobiotica. 1988 Sep;18(9):1085-96. doi: 10.3109/00498258809042231.

In vitro metabolism of methaphenilene (MFN) and pyribenzamine (PBZ) was compared to that of methapyriline (MPH) in rat, because chronic treatment with MPH causes cancer in rats, whereas MFN and PBZ cause no cancer. 2. G.l.c. and mass spectrometry were used to identify 7 metabolites of MFN and 6 of PBZ in extracts of rat liver microsome incubations. 3. Quantification of the metabolic pathways revealed that N-oxide formation is considerably more important for both MFN and PBZ than for MPH, and only MPH forms an amide as a metabolic product. 4. Quantitative balance studies show that a lower recovery is apparent for metabolic experiments with MPH than for either MFN or PBZ under all conditions examined, indicating that significant metabolic pathways for MPH exist which are not being measured under these conditions.

将美沙芬林（MFN）和吡苄明（PBZ）在大鼠体内的体外代谢与甲基吡啶啉（MPH）进行了比较，因为长期用MPH处理会导致大鼠患癌，而MFN和PBZ不会致癌。2. 采用气相色谱法和质谱法鉴定大鼠肝微粒体孵育提取物中MFN的7种代谢产物和PBZ的6种代谢产物。3. 代谢途径的定量分析表明，N-氧化形成对MFN和PBZ而言比MPH更为重要得多，并且只有MPH形成酰胺作为代谢产物。4. 定量平衡研究表明，在所研究的所有条件下，MPH代谢实验的回收率明显低于MFN或PBZ，这表明存在MPH的重要代谢途径，但在这些条件下未被测定。

Kammerer R C, Schmitz D A

Department of Pharmacology, University of California, Los Angeles 90024-1735.

Xenobiotica. 1988 Sep;18(9):1085-96. doi: 10.3109/00498258809042231.

In vitro metabolism of methaphenilene (MFN) and pyribenzamine (PBZ) was compared to that of methapyriline (MPH) in rat, because chronic treatment with MPH causes cancer in rats, whereas MFN and PBZ cause no cancer. 2. G.l.c. and mass spectrometry were used to identify 7 metabolites of MFN and 6 of PBZ in extracts of rat liver microsome incubations. 3. Quantification of the metabolic pathways revealed that N-oxide formation is considerably more important for both MFN and PBZ than for MPH, and only MPH forms an amide as a metabolic product. 4. Quantitative balance studies show that a lower recovery is apparent for metabolic experiments with MPH than for either MFN or PBZ under all conditions examined, indicating that significant metabolic pathways for MPH exist which are not being measured under these conditions.

将美沙芬林（MFN）和吡苄明（PBZ）在大鼠体内的体外代谢与甲基吡啶啉（MPH）进行了比较，因为长期用MPH处理会导致大鼠患癌，而MFN和PBZ不会致癌。2. 采用气相色谱法和质谱法鉴定大鼠肝微粒体孵育提取物中MFN的7种代谢产物和PBZ的6种代谢产物。3. 代谢途径的定量分析表明，N-氧化形成对MFN和PBZ而言比MPH更为重要得多，并且只有MPH形成酰胺作为代谢产物。4. 定量平衡研究表明，在所研究的所有条件下，MPH代谢实验的回收率明显低于MFN或PBZ，这表明存在MPH的重要代谢途径，但在这些条件下未被测定。