用于神经炎症 PET 成像的 [C]ER176 合成的替代策略。
Alternative strategies for the synthesis of [C]ER176 for PET imaging of neuroinflammation.
机构信息
Departments of Medical Physics, University of Wisconsin-Madison School of Medicine and Public Health, Madison, WI, USA; Waisman Laboratory for Brain Imaging and Behavior, University of Wisconsin-Madison, Madison, WI, USA.
Waisman Laboratory for Brain Imaging and Behavior, University of Wisconsin-Madison, Madison, WI, USA.
出版信息
Appl Radiat Isot. 2021 Dec;178:109954. doi: 10.1016/j.apradiso.2021.109954. Epub 2021 Sep 17.
[C]ER176 is a next generation PET radioligand for imaging 18 kDa translocator protein, a biomarker for neuroinflammation. The goal of this work was to investigate alternative strategies for the radiochemical synthesis, purification, and formulation of [C]ER176. An optimized tri-solvent high-performance liquid chromatography (HPLC) protocol is described to separate the hydro-de-chlorinated byproduct from [C]ER176. A newly implemented solid phase extraction work-up efficiently removed HPLC solvent while maintaining chemical purity and overall radiochemical yield and purity. This new HPLC purification and final formulation was completed within 40 min, providing 2.7 ± 0.5 GBq of [C]ER176 at end of synthesis with 1400 ± 300 GBq/μmol molar activity while meeting all specifications for radiopharmaceutical quality control tests for human research use.
[C]ER176 是一种用于成像 18 kDa 转位蛋白（神经炎症的生物标志物）的下一代 PET 放射性配体。这项工作的目的是研究 [C]ER176 的放射化学合成、纯化和制剂的替代策略。本文描述了一种优化的三溶剂高效液相色谱（HPLC）方案，用于分离 [C]ER176 的氢去氯副产物。新实施的固相萃取操作程序有效地去除了 HPLC 溶剂，同时保持了化学纯度和整体放射化学产率和纯度。这种新的 HPLC 纯化和最终制剂在 40 分钟内完成，提供了 2.7±0.5GBq 的 [C]ER176，在合成结束时摩尔活度为 1400±300GBq/μmol，同时满足了人类研究用放射性药物质量控制测试的所有规格。
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