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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

UCLA Medical Center, Dept. of Pharmacology 90024-1735.

Xenobiotica. 1987 Sep;17(9):1121-30. doi: 10.3109/00498258709044211.

The metabolism of N,N-dimethyl-N'-(2-pyridyl)-N'-(2-thienylmethyl)-1,2- ethanediamine(methapyrilene, I) by liver microsomes from rat, guinea pig, and rabbit has been examined. 2. Methapyrilene-N-oxide, (III), normethapyrilene, (II), 2-thiophene methanol, (VI), 2-thiophene carboxylic acid, (VII), N-(2-pyridyl)-N',N'-dimethylethylenediamine, (IX), and methapyrilene amide, (XIV) were found in all species. 3. N-(2-Thienylmethyl)-2-amino pyridine, (VIII), 2-aminopyridine, (X), and (5-hydroxypridyl)-methapyrilene, (XII), were detected in rat and rabbit only. 4. N-Hydroxynormethapyrilene, (XXI), was tentatively identified by mass spectral fragmentation patterns only in rabbit liver microsomes incubations; however, it was found in 9000 g supernatant fraction incubations of rabbit, rat and guinea pig. 5. The formation of IX and XII was quantitatively more important in the rat than in either rabbit or guinea pig.

已对大鼠、豚鼠和兔肝脏微粒体对N,N-二甲基-N'-(2-吡啶基)-N'-(2-噻吩甲基)-1,2-乙二胺（美吡拉敏，I）的代谢进行了研究。2. 在所有物种中均发现了美吡拉敏-N-氧化物（III）、去甲美吡拉敏（II）、2-噻吩甲醇（VI）、2-噻吩羧酸（VII）、N-(2-吡啶基)-N',N'-二甲基乙二胺（IX）和美吡拉敏酰胺（XIV）。3. 仅在大鼠和兔中检测到N-(2-噻吩甲基)-2-氨基吡啶（VIII）、2-氨基吡啶（X）和(5-羟基吡啶基)-美吡拉敏（XII）。4. N-羟基去甲美吡拉敏（XXI）仅通过质谱裂解模式在兔肝脏微粒体孵育中初步鉴定；然而，在兔、大鼠和豚鼠的9000g上清液部分孵育中均发现了它。5. IX和XII的形成在大鼠中比在兔或豚鼠中在数量上更重要。

Kammerer R C, Schmitz D A

UCLA Medical Center, Dept. of Pharmacology 90024-1735.

Xenobiotica. 1987 Sep;17(9):1121-30. doi: 10.3109/00498258709044211.

The metabolism of N,N-dimethyl-N'-(2-pyridyl)-N'-(2-thienylmethyl)-1,2- ethanediamine(methapyrilene, I) by liver microsomes from rat, guinea pig, and rabbit has been examined. 2. Methapyrilene-N-oxide, (III), normethapyrilene, (II), 2-thiophene methanol, (VI), 2-thiophene carboxylic acid, (VII), N-(2-pyridyl)-N',N'-dimethylethylenediamine, (IX), and methapyrilene amide, (XIV) were found in all species. 3. N-(2-Thienylmethyl)-2-amino pyridine, (VIII), 2-aminopyridine, (X), and (5-hydroxypridyl)-methapyrilene, (XII), were detected in rat and rabbit only. 4. N-Hydroxynormethapyrilene, (XXI), was tentatively identified by mass spectral fragmentation patterns only in rabbit liver microsomes incubations; however, it was found in 9000 g supernatant fraction incubations of rabbit, rat and guinea pig. 5. The formation of IX and XII was quantitatively more important in the rat than in either rabbit or guinea pig.

已对大鼠、豚鼠和兔肝脏微粒体对N,N-二甲基-N'-(2-吡啶基)-N'-(2-噻吩甲基)-1,2-乙二胺（美吡拉敏，I）的代谢进行了研究。2. 在所有物种中均发现了美吡拉敏-N-氧化物（III）、去甲美吡拉敏（II）、2-噻吩甲醇（VI）、2-噻吩羧酸（VII）、N-(2-吡啶基)-N',N'-二甲基乙二胺（IX）和美吡拉敏酰胺（XIV）。3. 仅在大鼠和兔中检测到N-(2-噻吩甲基)-2-氨基吡啶（VIII）、2-氨基吡啶（X）和(5-羟基吡啶基)-美吡拉敏（XII）。4. N-羟基去甲美吡拉敏（XXI）仅通过质谱裂解模式在兔肝脏微粒体孵育中初步鉴定；然而，在兔、大鼠和豚鼠的9000g上清液部分孵育中均发现了它。5. IX和XII的形成在大鼠中比在兔或豚鼠中在数量上更重要。