Development of PET probes for imaging of redox status in the brain

2015 Fiscal Year Final Research Report

• Project/Area Number: 25461895
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Institute of Radiological Sciences
• Principal Investigator: Okamura Toshimitsu 国立研究開発法人放射線医学総合研究所, 分子イメージング研究センター, 研究員 (80443068)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: PET / レドックス

Outline of Final Research Achievements

The purpose of this study was to investigate the feasibility of imaging brain redox status using a 11C-labeled dihydroquinoline derivative ([11C]DHQ1) for positron emission tomography. The lipophilic [11C]DHQ1 was rapidly oxidized to its hydrophilic form in mouse brain homogenate. The redox modulators diphenyleneiodonium and apocynin significantly decreased the oxidation velocity of [11C]DHQ1, and apocynin caused concentration-dependent inhibition of the oxidation velocity. Furthermore, [11C]DHQ1 diffused into the brain after administration and underwent oxidation into the hydrophilic metabolite, which then slowly decreased. By contrast, apocynin treatment caused a rapid decrease of radioactivity in the brain and inhibited the in vivo oxidation of [11C]DHQ1 to the hydrophilic metabolite. Thus, [11C]DHQ1 is a potential tracer for imaging of redox status in the brain.

Free Research Field

放射性医薬品