Development of next-generation PET ligand for neuroinflammation and comparison with current ligands

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K09979
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Institutes for Quantum and Radiological Science and Technology
• Principal Investigator: JI BIN 国立研究開発法人量子科学技術研究開発機構, 放射線医学総合研究所 脳機能イメージング研究部, 主任研究員(任常) (80392223)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: PET / 神経炎症 / Translocator Protein

Outline of Final Research Achievements

18F-FEBMP, a novel PET ligand for neuroinflammation originally developed in QST, has more sensitively captured TSPO expression in brains from tauopathy mouse and quinolone-induced neuroinflammation marmoset models, compared with two typical TSPO ligands, 11C-PK11195 and 11C-Ac5216. This newly developed ligand has high brain uptake and affinity for TSPO. However, PET scans with it failed to detected TSPO expression in normal macaque monkey brain likely due to slow washout rate. So, we have concluded that 18F-FEBMP is very useful for neuroinflammation imaging in preclinical studies. However, it is required for application in human subjects to optimized chemical structure for rapid washout from brain.

Free Research Field

核医学、神経病理学