Parameter evaluation and fully-automated radiosynthesis of [C-11]harmine for imaging of MAO-A for clinical trials

摘要

The aim of the present study was the evaluation and automation of the radiosynthesis of [C-11]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 2-3 mg/mL precursor activated with 1 eq. 5 M NaOH in DMSO, 80 degrees C reaction temperature and 2 min reaction time. Under these conditions 6.1 +/- 1 GBq (51.0 +/- 11% based on [C-11]CH3I, corrected for decay) of [C-11]harmine (n=72) were obtained. The specific activity was 10132 +/- 28.2 GBq/mu mol (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 setup. (C) 2015 The Authors. Published by Elsevier Ltd.