Neidlein R, Volland C, Kramer W
Pharmazeutisch-Chemisches Institut, Universität Heidelberg.
Arch Pharm (Weinheim). 1990 May;323(5):259-65. doi: 10.1002/ardp.19903230503.
The biotransformation of the positively inotropically active compound N-methyl-N-(2-hydroxy-3-phenoxy-propyl)-11-(2-aminoethyl)-6,11- dihydrodibenz[b,e]-oxepine, neutral fumarate, (Doxaminol, racemic mixture of diastereomeres) in dogs is examined. The metabolits M1-M7 were isolated and their chemical structures identified by 1H-NMR, 13C-NMR and mass spectroscopic methods. 2-Hydroxy-3-phenoxypropionic acid, phenoxyacetic acid, 3-(4'-hydroxy)-phenoxy-1,2-propandiol and phenylacetic acid were formed by side chain oxidation of the parent molecule. Furthermore, the following conjugates were characterized: Doxaminol-O-glucuronide, 4'-hydroxydoxaminol-O-glucuronide, and 1-hydroxy-3-phenoxy-2-propyl sulfate.
对正性肌力活性化合物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]氧杂卓中性富马酸盐（多沙米诺，非对映异构体的外消旋混合物）在犬体内的生物转化进行了研究。分离出代谢物M1-M7，并通过1H-NMR、13C-NMR和质谱法鉴定了它们的化学结构。母体分子的侧链氧化形成了2-羟基-3-苯氧基丙酸、苯氧基乙酸、3-(4'-羟基)-苯氧基-1,2-丙二醇和苯乙酸。此外，还对以下缀合物进行了表征：多沙米诺-O-葡萄糖醛酸苷、4'-羟基多沙米诺-O-葡萄糖醛酸苷和1-羟基-3-苯氧基-2-丙基硫酸盐。
