用于μ阿片受体PET成像的18F标记舒芬太尼。
18F-labeled sufentanil for PET-imaging of mu-opioid receptors.
作者信息
Henriksen Gjermund, Platzer Stefan, Hauser Andrea, Willoch Frode, Berthele Achim, Schwaiger Markus, Wester Hans-Jürgen
机构信息
Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaningerstrasse 22, 81675 München, Germany.
出版信息
Bioorg Med Chem Lett. 2005 Apr 1;15(7):1773-7. doi: 10.1016/j.bmcl.2005.02.049.
The synthesis of an (18)F-labeled sufentanil analogue with apparent high mu-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenyl-2-(+/-)-[(18)F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the mu-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in mu-opioid receptor mapping and quantitation with positron emission tomography.
据报道合成了一种具有明显高μ-阿片受体选择性的（18）F标记舒芬太尼类似物。给小鼠静脉注射N-[4-(甲氧基甲基)-1-[2-(2-噻吩基)乙基]-4-哌啶基]-N-苯基-2-(+/-)-[(18)F]氟丙酰胺后，在脑中摄取量高，且区域脑活性分布与μ-阿片受体表达模式相符。所开发的配体是用于正电子发射断层扫描中μ-阿片受体定位和定量扩展方案的一种有前景的示踪剂。
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