Basic study of PET imaging of PKC, a intracellular transduction enzyme

• Project/Area Number: 21591601
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Single-year Grants
• Section: 一般
• Research Field: Radiation science
• Research Institution: The Institute of Physical and Chemical Research
• Principal Investigator: TAKAHASHI Kazuhiro 独立行政法人理化学研究所, イメージング基盤ユニット, ユニットリーダー (20370257)
• Project Period (FY): 2009 – 2011
• Project Status: Completed (Fiscal Year 2011)
• Budget Amount: ¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000); Fiscal Year 2011: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2010: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000); Fiscal Year 2009: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
• Keywords: シグナル伝達 / 生体分子 / 脳神経 / 標識合成 / PKC / PET / 分子イメージング / radiopharmaceuticals / radiophamaceuticals

Research Abstract

We synthesize N-[^<11> C] methyl-bisindolylmaleimideIII, a selective inhibitor for protein kinase C(PKC), in order to estimate the roll of PKC in the ischemic brain. The radiochemical yield was 30-50%, radiochemical purity was> 95%. The synthetic time was 30 min. Blood clearance was fast and the concentration in blood was low after few minutes. Bio-distributions of this labeled compound showed high uptake in liver and kidney. The uptake in brain was very low. So this tracer was not suitable for estimation of PKC in the ischemic brain.