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犬体内部分β-激动剂多沙米诺的生物转化

Biotransformation of the partial beta-agonist doxaminol in dog.

作者信息

Neidlein R, Volland C, Strein K

机构信息

Pharmaceutical-Chemical Institute, University of Heidelberg, Fed. Rep. of Germany.

出版信息

Arzneimittelforschung. 1990 Feb;40(2 Pt 1):130-6.

PMID:1970733
Abstract

The biotransformation of the positive inotropic compound doxaminol (N-methyl-N-(2-hydroxy-3-phenoxy-propyl)-11-(2-amino-ethyl)-6,11- dihydrodibenz[b,e]oxepine, neutral fumarate; BM 10.188) was examined in bastard shepherd dogs. Metabolic products, formed by oxidative cleavage of various side chain carbon atoms of the molecule, as well as conjugated complexes with glucuronic and sulfuric acid, were isolated from urine and plasma. As main metabolites 2-hydroxy-3-phenoxy-propionic acid and phenoxyacetic acid were formed. By means of 1HNMR and 13C-NMR spectroscopy and various mass spectroscopic methods, the chemical structures of the metabolites were elucidated.

摘要

在杂种牧羊犬中研究了正性肌力化合物多沙米诺(N-甲基-N-(2-羟基-3-苯氧基丙基)-11-(2-氨基乙基)-6,11-二氢二苯并[b,e]噁庚因,富马酸中性盐;BM 10.188)的生物转化。从尿液和血浆中分离出了由分子中各种侧链碳原子氧化裂解形成的代谢产物,以及与葡萄糖醛酸和硫酸的共轭复合物。形成的主要代谢产物为2-羟基-3-苯氧基丙酸和苯氧基乙酸。通过1H NMR和13C-NMR光谱以及各种质谱方法阐明了代谢产物的化学结构。

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