典型文献
Synthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand:(S)-(+)-and(R)-(-)-[18F]FBFP
文献摘要：
Racemic[18F]FBFP([18F]1)proved to be a potent σ1 receptor radiotracer with superior imag-ing properties.The pure enantiomers of unlabeled compounds(S)-and(R)-1 and the corre-sponding iodonium ylide precursors were synthesized and characterized.The two enantiomers(S)-1 and(R)-1 exhibited comparable high affinity for σ1 receptors and selectivity over σ2 recep-tors.The Ca2+fluorescence assay indicated that(R)-1 behaved as an antagonist and(S)-1 as an agonist for σ1 receptors.The 18F-labeled enantiomers(S)-and(R)-[18F]1 were obtained in＞99％enantiomeric purity from the corresponding enantiopure iodonium ylide precursors with radiochemi-cal yield of 24.4％±2.6％and molar activity of 86-214 GBq/pmol.In ICR mice both(S)-and(R)-[18F]1 displayed comparable high brain uptake,brain-to-blood ratio,in vivo stability and binding specificity in the brain and peripheral organs.In micro-positron emission tomography(PET)imaging studies in rats,(S)-[18F]1 exhibited faster clearance from the brain than(R)-[18F]1,indicating different brain kinetics of the two enantiomers.Both(S)-and(R)-[18F]1 warrant further evaluation in primates to translate a single enantiomer with more suitable kinetics for imaging the σ1 receptors in humans.
文献关键词：
中图分类号：
作者姓名：
Tao Wang;Ying Zhang;Xiaojun Zhang;Leyuan Chen;Mingqiang Zheng;Jinming Zhang;Peter Brust;Winnie Deuther-Conrad;Yiyun Huang;Hongmei Jia
作者机构：
Key Laboratory of Radiopharmaceuticals(Beijing Normal University),Ministry of Education,College of Chemistry,Beijing Normal University,Beijing 100875,China;Nuclear Medicine Department,The First Medical Center of Chinese PLA General Hospital,Beijing 100853,China;Institute of Radiation Medicine,Peking Union Medical College&Chinese Academy of Medical Sciences,Tianjin 300192,China;Yale PET Center,Department of Radiology and Biomedical Imaging,Yale University School of Medicine,New Haven,CT 06520-8048,United States;Helmholtz-Zentrum Dresden-Rossendorf,Institute of Radiopharmaceutical Cancer Research,Department of Neuroradiopharmaceuticals,Leipzig 04318,Germany
文献出处：
引用格式：
[1]Tao Wang;Ying Zhang;Xiaojun Zhang;Leyuan Chen;Mingqiang Zheng;Jinming Zhang;Peter Brust;Winnie Deuther-Conrad;Yiyun Huang;Hongmei Jia-.Synthesis and characterization of the two enantiomers of a chiral sigma-1 receptor radioligand:(S)-(+)-and(R)-(-)-[18F]FBFP)[J].中国化学快报（英文版）,2022(07):3543-3548
A类：
radioligand,FBFP,Racemic,radiotracer,iodonium,ylide,Ca2+fluorescence,enantiopure,radiochemi
B类：
Synthesis,characterization,two,enantiomers,chiral,sigma,18F,proved,potent,superior,properties,unlabeled,compounds,precursors,were,synthesized,characterized,exhibited,comparable,high,affinity,receptors,selectivity,over,assay,indicated,that,behaved,antagonist,obtained,enantiomeric,purity,from,corresponding,cal,yield,molar,activity,GBq,pmol,In,ICR,mice,both,displayed,brain,uptake,blood,ratio,vivo,stability,binding,specificity,peripheral,organs,micro,positron,emission,tomography,PET,imaging,studies,rats,faster,clearance,than,indicating,different,kinetics,Both,warrant,further,evaluation,primates,translate,single,more,suitable,humans
AB值：
0.465785
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