Journal
APPLIED RADIATION AND ISOTOPES
Volume 70, Issue 8, Pages 1779-1783Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.apradiso.2012.03.006
Keywords
Positron emission tomography; [C-11]PBR28; Radiopharmaceutical synthesis; Peripheral benzodiazepine receptor (PBR); Microglial activation
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Funding
- Office of Biological and Environmental Research (BER) of the Office of Science (SC), at the US Department of Energy [DE-FG02-08ER64645]
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In order to image the translocator protein (TSPO) 18 kDa in the clinic using positron emission tomography (PET) imaging, we had a cause to prepare [C-11]PBR28. In this communication we highlight our novel, recently developed, one-pot synthesis of the desmethyl-PBR28 precursor, as well as present an optimized fully automated preparation of [C-11]PBR28 using a GE TRACERlab FXC-Pro. Following radiolabelling, purification is achieved by HPLC and, to the best of our knowledge, the first reported example of reconstituting [C-11]PBR28 into ethanolic saline using solid-phase extraction (SPE). This procedure is operationally simple, and provides high quality doses of [C-11]PBR28 suitable for use in clinical PET imaging studies. Typical radiochemical yield using the optimized method is 3.6% yield (EOS, n = 3), radiochemical and chemical purity are consistently >99%, and specific activities are 14,523 Ci/mmol. (C) 2012 Elsevier Ltd. All rights reserved.
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