Blake T J, Beattie I G
Department of Drug Metabolism and Pharmacokinetics, Smith Kline & French Research Ltd, The Frythe, Welwyn, Herts, UK.
Biomed Environ Mass Spectrom. 1989 Oct;18(10):860-6. doi: 10.1002/bms.1200181004.
This paper describes the development and application of a combined thermospray liquid chromatographic/mass spectrometric and liquid chromatographic/tandem mass spectrometric method for distinguishing between five isomeric metabolites of Temelastine, comprising four hydroxylated metabolites and one N-oxide. The method allows the unambiguous characterization of all of the isomers either on their own or in the presence of each other. Clear results were obtained for the characterization of these metabolites in biological samples. Temelastine showed extensive phase I and phase II metabolism and the methodology was used to study the aglycone structures of the glucuronide conjugates derived from the hydroxylated metabolites. Photo-diode array ultraviolet spectroscopy was used as a complementary technique to help elucidate the site of glucuronidation in these species.
本文描述了一种热喷雾液相色谱/质谱联用和液相色谱/串联质谱联用方法的开发与应用，该方法用于区分替美斯汀的五种异构体代谢物，包括四种羟基化代谢物和一种N - 氧化物。该方法能够明确表征所有这些异构体，无论是单独存在还是相互共存时。在生物样品中对这些代谢物进行表征时获得了清晰的结果。替美斯汀表现出广泛的I相和II相代谢，该方法被用于研究源自羟基化代谢物的葡萄糖醛酸苷缀合物的苷元结构。光电二极管阵列紫外光谱法作为一种辅助技术，用于帮助阐明这些物质中葡萄糖醛酸化的位点。
