title: Fully automated radiosynthesis of [¹¹C]PBR28, a radiopharmaceutical for the translocator protein (TSPO) 18 kDa, using a GE TRACERlab FXC-Pro.
abstract: In order to image the translocator protein (TSPO) 18kDa in the clinic using positron emission tomography (PET) imaging, we had a cause to prepare [(11)C]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 [(11)C]PBR28 using a GE TRACERlab FX(C-Pro). Following radiolabelling, purification is achieved by HPLC and, to the best of our knowledge, the first reported example of reconstituting [(11)C]PBR28 into ethanolic saline using solid-phase extraction (SPE). This procedure is operationally simple, and provides high quality doses of [(11)C]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 14,523Ci/mmol.
authors.affiliation: Department of Radiology, University of Michigan, Ann Arbor, MI 48109, USA.
authors.forename: Raphaël
authors.initials: R
authors.lastname: Hoareau
authors.forename: Xia
authors.initials: X
authors.lastname: Shao
authors.forename: Bradford D
authors.initials: BD
authors.lastname: Henderson
authors.forename: Peter J H
authors.initials: PJ
authors.lastname: Scott
mesh_terms: D000081:Acetamides / Q000737:chemistry*; D001331:Automation; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D011725:Pyridines / Q000737:chemistry*; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D018079:Receptors, GABA / Q000737:chemistry*
chemical_list: D000081:Acetamides; D002250:Carbon Radioisotopes; C526798:N-(2-methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide; D011725:Pyridines; D019275:Radiopharmaceuticals; D018079:Receptors, GABA; C499229:TSPO protein, human