Quantitative PET imaging of AMPA receptors in humans

• Project/Area Number: 15K09977
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: National Center for Geriatrics and Gerontology (2016-2017); National Institute of Radiological Sciences (2015)
• Principal Investigator: KIMURA Yasuyuki 国立研究開発法人国立長寿医療研究センター, 脳機能画像診断開発部, 室長 (20423171)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Project Status: Completed (Fiscal Year 2017)
• Budget Amount: ¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000); Fiscal Year 2017: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000); Fiscal Year 2016: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000); Fiscal Year 2015: ¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000)
• Keywords: AMPA受容体 / 陽電子断層撮像法 / PET / 陽電子断層撮影法 / 陽電子射出断層撮影

Outline of Final Research Achievements

In the current study, we performed a human PET study using a novel PET imaging agent for AMPA receptors, and evaluated the safety and utility of this radioligand as a PET imaging agent. Four healthy male subjects were scanned with a PET scanner. Arterial blood sampling and metabolite analysis were performed to obtain input functions. PET qauntification showed a possibility of radiometabolites entering the brain and small radioligand binding potential values in the cortical regions, which suggested specific binding component of the PET signal in the brain. In conclusion, kinetic analyses support some specific binding of the PET ligand in the human cortex. However, this ligand may not be suitable for practical AMPA receptor PET imaging due to the small dynamic range and metabolite in the brain.

Research Products

• [Journal Article] A human PET study of [11C]HMS011, a potential radioligand for AMPA receptors (2018)
  • Author(s): Keisuke Takahata et al.,
  • Journal Title: EJNMMI research Volume: 16 Issue: 1 Pages: 63-63
  • DOI: 10.1186/s13550-017-0313-0
  • Peer Reviewed / Open Access / Int'l Joint Research
• [Presentation] A human PET study of [11C]HMS011, a potential radioligand for AMPA receptors (2017)
  • Author(s): Keisuke Takahata, Yasuyuki Kimura, Chie Seki, Masanori Ichise, Kazunori Kawamura, Soichiro Kitamura, Manabu Kubota, Sho Moriguchi, Tatsuya Ishi, Yuhei Takado, Fumitoshi Niwa, Hironobu Endo, Tomohisa Nagashima, Ming-Rong Zhang, Tetsuya Suhara, and Makoto Higuchi
  • Organizer: Society of Nuclear Medicine and Molecular Imaging Annual Meeting 2017
  • Int'l Joint Research