A Facile Radiolabeling of [F-18]FDPA via Spirocyclic Iodonium Ylides: Preliminary PET Imaging Studies in Preclinical Models of Neuroinflammation

作者：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.^*

来源：Journal of Medicinal Chemistry, 2017, 60(12): 5222-5227.

DOI：10.1021/acs.jmedchem.7b00432

• PROTEIN 18 KDA
• ALZHEIMERS-DISEASE
• BENZODIAZEPINE-RECEPTOR
• MICROGLIAL ACTIVATION
• RAT-BRAIN
• TSPO
• RADIOFLUORINATION
• LIGAND
• QUANTIFICATION
• VISUALIZATION

A suitable TSPO PET ligand may visualize and quantify neuroinflammation in a living brain. Herein we report a F-18-ligand, [F-18]2 ([F-18]FDPA), is radiolabeled in high yield and high specific activity based on our spirocyclic iodonium ylide (SCIDY) strategy. [F-18]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).

• 出版日期2017-6-22
• 单位天津大学