title: Parameter evaluation and fully-automated radiosynthesis of [(11)C]harmine for imaging of MAO-A for clinical trials.
abstract: The aim of the present study was the evaluation and automation of the radiosynthesis of [(11)C]harmine for clinical trials. The following parameters have been investigated: amount of base, precursor concentration, solvent, reaction temperature and time. The optimum reaction conditions were determined to be 2-3mg/mL precursor activated with 1eq. 5M NaOH in DMSO, 80°C reaction temperature and 2min reaction time. Under these conditions 6.1±1GBq (51.0±11% based on [(11)C]CH3I, corrected for decay) of [(11)C]harmine (n=72) were obtained. The specific activity was 101.32±28.2GBq/µmol (at EOS). All quality control parameters were in accordance with the standards for parenteral human application. Due to its reliability and high yields, this fully-automated synthesis method can be used as routine set-up.
authors.affiliation: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
authors.forename: C
authors.initials: C
authors.lastname: Philippe
authors.affiliation: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
authors.forename: M
authors.initials: M
authors.lastname: Zeilinger
authors.affiliation: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
authors.forename: M
authors.initials: M
authors.lastname: Mitterhauser
authors.affiliation: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
authors.forename: M
authors.initials: M
authors.lastname: Dumanic
authors.affiliation: Department of Psychiatry and Psychotherapy, Medical University of Vienna, 1090 Vienna, Austria.
authors.forename: R
authors.initials: R
authors.lastname: Lanzenberger
authors.affiliation: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria.
authors.forename: M
authors.initials: M
authors.lastname: Hacker
authors.affiliation: Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, A-1090 Vienna, Austria. Electronic address: wolfgang.wadsak@meduniwien.ac.at.
authors.forename: W
authors.initials: W
authors.lastname: Wadsak
mesh_terms: D001921:Brain / Q000000981:diagnostic imaging / Q000201:enzymology; D002250:Carbon Radioisotopes / Q000592:standards; D060326:Chemistry Techniques, Synthetic / Q000295:instrumentation / Q000379:methods; D002986:Clinical Trials as Topic; D006247:Harmine / Q000138:chemical synthesis* / Q000592:standards; D006801:Humans; D008995:Monoamine Oxidase / Q000378:metabolism*; D049268:Positron-Emission Tomography; D011786:Quality Control; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000592:standards
chemical_list: D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D006247:Harmine; D008995:Monoamine Oxidase; C579458:monoamine oxidase A, human
keywords: Carbon-11; MAO-A; Monoamine oxidase; PET; Radiosynthesis; [(11)C]harmine