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Alternative strategies for the synthesis of [11C]ER176 for PET imaging of neuroinflammation

Abstract

[C-11]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-11]ER176. An optimized tri-solvent high-performance liquid chromatography (HPLC) protocol is described to separate the hydro-de-chlorinated byproduct from [C-11]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-11]ER176 at end of synthesis with 1400 +/- 300 GBq/ mu mol molar activity while meeting all specifications for radiopharmaceutical quality control tests for human research use.

article Article
date_range 2021
language English
link Link of the paper
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Featured Keywords

Neuroinflammation
PET
Radiochemistry
ER176
11-Carbon
TSPO
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