富电子碘鎓叶立德的氟标记：在潜在5-羟色胺受体正电子发射断层扫描配体放射性合成中的应用
F-Labelling of electron rich iodonium ylides: application to the radiosynthesis of potential 5-HT receptor PET ligands.
作者信息
Petersen I N, Villadsen J, Hansen H D, Madsen J, Jensen A A, Gillings N, Lehel S, Herth M M, Knudsen G M, Kristensen J L
机构信息
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
出版信息
Org Biomol Chem. 2017 May 23;15(20):4351-4358. doi: 10.1039/c7ob00628d.
F-Labelling of aromatic moieties was limited to electron deficient aromatic systems for many years but recent developments have provided access to the direct labelling of electron rich aromatic systems. Herein we report the synthesis and F-labelling of iodonium ylide precursors in the pursuit of F-labelled 5-HT receptor agonist PET-ligands. Subsequent evaluation in pigs showed high brain uptake of the PET ligands but a blocking dose of ketanserin did not significantly reduce the signal in relevant brain regions - indicating that the ligands do not interact specifically with the 5-HT receptor in vivo.
多年来，芳香基团的氟标记仅限于缺电子芳香体系，但最近的进展使得富电子芳香体系的直接标记成为可能。在此，我们报告了碘鎓叶立德前体的合成及氟标记，以寻求氟标记的5-羟色胺（5-HT）受体激动剂正电子发射断层扫描（PET）配体。随后在猪身上进行的评估显示，PET配体在大脑中的摄取量很高，但酮色林的阻断剂量并未显著降低相关脑区的信号，这表明这些配体在体内并未与5-HT受体发生特异性相互作用。
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