Wang Lu, Cheng Ran, Fujinaga Masayuki, Yang Jian, Zhang Yiding, Hatori Akiko, Kumata Katsushi, Yang Jing, Vasdev Neil, Du Yunfei, Ran Chongzhao, Zhang Ming-Rong, Liang Steven H
Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School , Boston, Massachusetts 02114, United States.
School of Pharmaceutical Science and Technology, Tianjin University , 92 Weijin Road, Nankai District, Tianjin, China.
J Med Chem. 2017 Jun 22;60(12):5222-5227. doi: 10.1021/acs.jmedchem.7b00432. Epub 2017 Jun 5.
A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a F-ligand, [F]2 ([F]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [F]2 demonstrated saturable specific binding to TSPO, substantially elevated brain uptake, and slow washout of bound PET signal in the preclinical models of brain neuroinflammation (cerebral ischemia and Alzheimer's disease).
一种合适的TSPO PET配体可以在活体大脑中可视化并量化神经炎症。在此，我们报告一种F配体，[F]2（[F]FDPA），基于我们的螺环碘鎓叶立德（SCIDY）策略，它能以高产量和高比活度进行放射性标记。在脑神经炎症（脑缺血和阿尔茨海默病）的临床前模型中，[F]2显示出对TSPO的可饱和特异性结合、显著提高的脑摄取以及结合的PET信号的缓慢洗脱。
