机构：[a]Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.[b]Department of Nuclear Medicine, Xuanwu Hospital, Capital Medical University, Beijing 100053, P. R. China首都医科大学宣武医院[c]Wuhan Institute for Neuroscience and Neuroengineering, South-Central University for Nationalities, Wuhan 430074, P. R. China
In continuation of our investigation of the dibenzylideneacetone scaffold as A beta imaging probes, a series of derivatives containing pyridine rings with lower lipophilicity was synthesized and evaluated. Some of these probes displayed high affinities to A beta(1-42) aggregates, which ranged from 18.0 to 8.2 nM. The high and specific binding of the radiolabeled tracers was further confirmed by in vitro autoradiography on brain sections from AD patients and transgenic mouse. In biodistribution experiments, two F-18-labeled tracers [F-18]17a and [F-18]18 displayed high initial brain uptake ( 5.05 and 6.24% ID g(-1), respectively, at 2 min postinjection) and fast clearance from the brain with brain(2 min)/ brain(60 min) ratios of 6.08 and 8.00. These results demonstrate that the probes [F-18]17a and [F-18]18 with a dibenzylideneacetone structure containing pyridine rings have great strength in imaging A beta plaques in the brain.
基金：
the National Natural Science Foundation of China (no. 21571022 and 21201019),
the National Science and Technology Major Projects for Major New Drugs Innovation and Development (no. 2014ZX09507007-002).
第一作者机构：[a]Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.
通讯作者：
通讯机构：[a]Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.
推荐引用方式(GB/T 7714)：
Xiaomei Cui ,Xiaoyang Zhang ,Cheng Peng ,et al.Radiolabeled pyridinyl analogues of dibenzylideneacetone as beta-amyloid imaging probes[J].RSC ADVANCES.2016,6(50):44646-44654.doi:10.1039/c6ra05168e.
APA：
Xiaomei Cui,,Xiaoyang Zhang,,Cheng Peng,,Jiapei Dai,,Boli Liu&Mengchao Cui.(2016).Radiolabeled pyridinyl analogues of dibenzylideneacetone as beta-amyloid imaging probes.RSC ADVANCES,6,(50)
MLA：
Xiaomei Cui,,et al."Radiolabeled pyridinyl analogues of dibenzylideneacetone as beta-amyloid imaging probes".RSC ADVANCES 6..50(2016):44646-44654
