Nusser E, Nill K, Breyer-Pfaff U
Department of Toxicology, University of Tübingen, F.R.G.
J Chromatogr. 1990 Jun 8;528(1):163-71. doi: 10.1016/s0378-4347(00)82371-3.
E- and Z-10-hydroxyamitriptyline (E- and Z-10-OH-AT) are racemic alcoholic metabolites of the antidepressant amitriptyline. Their enantiomers were separated by high-performance liquid chromatography as diastereomeric derivatives using R-(+)-alpha-methoxy-alpha-trifluoromethylphenylacetyl chloride (Mosher's reagent). Although E-10-hydroxyamitriptyline excreted in patient urine in free form or as the O-glucuronide consisted primarily of the (-)-enantiomer, the N-glucuronide contained similar amounts of the two enantiomers. Z-10-OH-AT was analysed in one patient and an excess of the (+)-isomer was found in the unconjugated, total conjugated and N-glucuronidated metabolite. The specific optical rotation of (-)-E-10-OH-AT was determined.
E型和Z型10-羟基阿米替林（E-和Z-10-OH-AT）是抗抑郁药阿米替林的外消旋醇代谢物。使用R-(+)-α-甲氧基-α-三氟甲基苯基乙酰氯（莫舍尔试剂），通过高效液相色谱将它们的对映体分离为非对映体衍生物。尽管以游离形式或O-葡萄糖醛酸苷形式排泄在患者尿液中的E-10-羟基阿米替林主要由(-)-对映体组成，但N-葡萄糖醛酸苷中两种对映体的含量相似。对一名患者的Z-10-OH-AT进行了分析，发现在未结合、总结合和N-葡萄糖醛酸化代谢物中(+)-异构体过量。测定了(-)-E-10-OH-AT的比旋光度。
