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豚鼠肝微粒体制剂对阿托品、东莨菪碱及相应去甲生物碱的代谢性N-氧化作用。

Metabolic N-oxidation of atropine, hyoscine and the corresponding nor-alkaloids by guinea-pig liver microsomal preparations.

作者信息

Phillipson J D, Handa S S, Gorrod J W

出版信息

J Pharm Pharmacol. 1976 Sep;28(9):687-91. doi: 10.1111/j.2042-7158.1976.tb02837.x.

Abstract

Incubation of guinea-pig liver microsomal preparations with atropine or hyoscine resulted in the formation of the corresponding nor-alkaloids and both isomers of atropine N-oxide from atropine and one isomer of hyoscine N-oxide from hyoscine. Separate incubations of guinea-pig liver microsomal preparations with nor-atropine and nor-hyoscine yielded the corresponding hydroxylamines. The N-oxide and hydroxylamine metabolites were identified by comparison of their t.l.c. behavior and m.x. with prepared compounds and also by their reduction to the corresponding tertiary or secondary amines.

摘要

将豚鼠肝微粒体制剂与阿托品或东莨菪碱一起温育,会导致相应去甲生物碱的形成,阿托品会生成阿托品N-氧化物的两种异构体,东莨菪碱会生成东莨菪碱N-氧化物的一种异构体。将豚鼠肝微粒体制剂分别与去甲阿托品和去甲东莨菪碱温育,会产生相应的羟胺。通过比较它们的薄层层析行为和熔点与制备的化合物,并通过将它们还原为相应的叔胺或仲胺,来鉴定N-氧化物和羟胺代谢物。

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