title: Automated production of [¹⁸F]VAT suitable for clinical PET study of vesicular acetylcholine transporter.
abstract: Automated production of a promising radiopharmaceutical (-)-(1-(8-(2-[(18)F]fluoroethoxy)-3-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)-piperidin-4-yl)(4-fluorophenyl)methanone ([(18)F]VAT) for the vesicular acetylcholine transporter(VAChT) was achieved using a two-step procedure in a current Good Manufacturing Practices fashion. The production of [(18)F]VAT was accomplished in approximately 140 min, with radiochemical yield of ~15.0% (decay corrected), specific activity>111 GBq/µmol, radiochemical purity>99% and mass of VAT ~3.4 μg/batch (n>10). The radiopharmaceutical product meets all quality control criteria for human use, and is suitable for clinical PET studies of VAChT.
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA.
authors.forename: Xuyi
authors.initials: X
authors.lastname: Yue
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA.
authors.forename: Christopher
authors.initials: C
authors.lastname: Bognar
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA.
authors.forename: Xiang
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA.
authors.forename: Gregory G
authors.initials: GG
authors.lastname: Gaehle
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA.
authors.forename: Stephen M
authors.initials: SM
authors.lastname: Moerlein
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA.
authors.forename: Joel S
authors.initials: JS
authors.lastname: Perlmutter
authors.affiliation: Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO, USA. Electronic address: tuz@mir.wustl.edu.
authors.forename: Zhude
authors.initials: Z
authors.lastname: Tu
mesh_terms: D005462:Fluorine Radioisotopes / Q000737:chemistry* / Q000592:standards; D006801:Humans; D015394:Molecular Structure; D009284:Naphthols / Q000138:chemical synthesis* / Q000737:chemistry; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000592:standards; D049268:Positron-Emission Tomography / Q000379:methods*; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000592:standards; D050494:Vesicular Acetylcholine Transport Proteins / Q000378:metabolism*
chemical_list: C000611062:(1-(8-(2-fluoroethoxy)-3-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)piperidin-4-yl)(4-fluorophenyl)methanone; D005462:Fluorine Radioisotopes; D009284:Naphthols; D010880:Piperidines; D019275:Radiopharmaceuticals; C493459:SLC18A3 protein, human; D050494:Vesicular Acetylcholine Transport Proteins
keywords: Automation; Clinical studies; Fluorine-18; Positron emission tomography; Vesicular acetylcholine transporter