Kammerer R C, Schmitz D A
Xenobiotica. 1986 Jul;16(7):671-80. doi: 10.3109/00498258609043557.
The metabolism of methapyrilene(I) in rat-liver 9000 g supernatant fraction produced four new metabolites positively identified by comparison of g.l.c. retention times and mass-spectral fragmentation patterns with those of authentic materials. These compounds are 2-thiophene-methanol(VI), 2-thiophenecarboxylic acid(VII), N-2-pyridyl-N'-dimethylethylenediamine(IX) and 2-aminopyridine(X). In addition, the previously known metabolite 2-[(2-thienylmethyl)amino]-pyridine(VIII) was also positively identified. Six other metabolites were tentatively identified by analysis of the mass-spectral fragmentation patterns of both the trimethylsilyl and the tertiary butyldimethylsilyl derivatives of each compound. These compounds are tentatively identified as: normethapyrilene(II), (hydroxypyridyl)-methapyrilene(XII), methapyrilenamide(XIV), (hydroxypyridyl)-normethapyrilene(XVI), (hydroxypyridyl)-desmethylmethapyrilenamide(XVII), and (hydroxypyridyl) methapyrilenamide(XVIII). Quantification of II, VI-X, XII and XIV account for approx. 65% of the metabolized methapyrilene.
在大鼠肝脏9000g上清液组分中，甲吡咯烷（I）的代谢产生了四种新的代谢物，通过与标准品的气相色谱保留时间和质谱碎片模式进行比较，这些代谢物得到了明确鉴定。这些化合物分别是2-噻吩甲醇（VI）、2-噻吩羧酸（VII）、N-2-吡啶基-N'-二甲基乙二胺（IX）和2-氨基吡啶（X）。此外，之前已知的代谢物2-[(2-噻吩基甲基)氨基]-吡啶（VIII）也得到了明确鉴定。通过对每种化合物的三甲基硅烷基和叔丁基二甲基硅烷基衍生物的质谱碎片模式进行分析，初步鉴定出了另外六种代谢物。这些化合物初步鉴定为：去甲甲吡咯烷（II）、（羟基吡啶基）-甲吡咯烷（XII）、甲吡咯烷酰胺（XIV）、（羟基吡啶基）-去甲甲吡咯烷（XVI）、（羟基吡啶基）-去甲基甲吡咯烷酰胺（XVII）和（羟基吡啶基）甲吡咯烷酰胺（XVIII）。对II、VI-X、XII和XIV的定量分析表明，它们约占代谢后的甲吡咯烷的65%。
