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

细胞内转导酶PKC的PET成像基础研究

• 批准号: 21591601
• 负责人: TAKAHASHI Kazuhiro
• 金额: $ 2.66万
• 依托单位: The Institute of Physical and Chemical Research
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2009
• 资助国家: 日本
• 起止时间: 2009 至 2011
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-21591601/
• 关键词: 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

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.

我们合成了蛋白激酶C(PKC)的选择性抑制剂N-[11&gt；C]甲基双吲哚马来酰亚胺III，以估计PKC在缺血脑中的滚动。放化产率为30-50%，放化纯度为95%。合成时间为30min。几分钟后血液清除快，血药浓度低。该标记化合物在肝脏和肾脏的生物分布显示出较高的摄取。脑内摄取很低。因此，该示踪剂不适用于脑缺血后PKC的测定。