[18F]氟-β-氟亚甲基间酪氨酸类似物，用于突触前多巴胺末梢的潜在正电子发射断层显像剂：合成与光谱表征
[18F]fluoro-beta-fluoromethylene-m-tyrosine analogs, potential PET agents for presynaptic dopamine terminals: synthesis and spectroscopic characterization.
作者信息
Murali D, DeJesus O T, Sunderland J J, Nickles R J
机构信息
Department of Medical Physics, University of Wisconsin, Madison 53706.
出版信息
Int J Rad Appl Instrum A. 1992 Aug;43(8):969-77. doi: 10.1016/0883-2889(92)90215-z.
18F-labeled (E)-beta-fluoromethylene-DL-m-tyrosine (FMMT) was prepared by the direct reaction of FMMT with [18F]acetylhypofluorite (AcOF) resulting into three product isomers. Extensive 1H, 13C and 19F-NMR spectroscopic analysis identify these products to be 2-fluoro, 6-fluoro-FMMT and 2,6-difluoro-FMMT. The HPLC isolated radiochemical EOB yields of these products were 22, 25 and 14%, respectively, based on starting [18F]AcOF. The specific activity at the end of a synthesis time of an hour was ca 200 mCi/mmol. With the possible advantage of "metabolic trapping" in dopamine nerve terminals via covalent binding to MAO and reduced metabolite formation, [18F]F-FMMT may potentially be the optimal PET tracer for CNS dopamine nerve terminals.
18F标记的（E）-β-氟亚甲基-DL-m-酪氨酸（FMMT）通过FMMT与[18F]乙酰次氟酸（AcOF）直接反应制备，得到三种产物异构体。广泛的1H、13C和19F-NMR光谱分析确定这些产物为2-氟-FMMT、6-氟-FMMT和2,6-二氟-FMMT。基于起始的[18F]AcOF，这些产物经HPLC分离后的放射化学放化产率分别为22%、25%和14%。在一小时合成时间结束时的比活度约为200 mCi/mmol。由于通过与单胺氧化酶共价结合在多巴胺神经末梢可能具有“代谢捕获”优势以及减少代谢物形成，[18F]F-FMMT可能是用于中枢神经系统多巴胺神经末梢的最佳正电子发射断层显像（PET）示踪剂。
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