Department of Pharmacy & Pharmacology, Slotervaart Hospital/The Netherlands Cancer Institute, Louwesweg 6, 1066 EC, Amsterdam, The Netherlands.
J Pharm Biomed Anal. 2011 Jun 1;55(3):518-26. doi: 10.1016/j.jpba.2011.02.009. Epub 2011 Feb 18.
A comprehensive overview is presented of currently known phase I metabolites of tamoxifen consisting of their systematic name and molecular structure. Reference standards are utilized to elucidate the MS(n) fragmentation patterns of these metabolites using a linear ion trap mass spectrometer. UV-absorption spectra are recorded and absorption maxima are defined. Serum extracts from ten breast cancer patients receiving 40mg tamoxifen once daily were qualitatively analyzed for tamoxifen phase I metabolites using a liquid chromatography-tandem mass spectrometry set-up. In total, 19 metabolites have been identified in these serum samples. Additionally a synthetic method for the preparation of the putative metabolite 3',4'-dihydroxytamoxifen is described.
本文综述了目前已知的他莫昔芬 I 期代谢物，包括它们的系统名和分子结构。利用线性离子阱质谱仪，参考标准来阐明这些代谢物的 MS(n) 碎片模式。记录紫外吸收光谱并定义吸收最大值。利用液相色谱-串联质谱装置，对 10 名每日接受 40mg 他莫昔芬治疗的乳腺癌患者的血清提取物进行了他莫昔芬 I 期代谢物的定性分析。在这些血清样本中，共鉴定出 19 种代谢物。此外，还描述了制备假定代谢物 3'，4'-二羟基他莫昔芬的合成方法。
