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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 2–3 mg/mL precursor activated with 1 eq. 5 M NaOH in DMSO, 80 °C reaction temperature and 2 min reaction time. Under these conditions 6.1±1 GBq (51.0±11% based on [ 11 C]CH 3 I, corrected for decay) of [ 11 C]harmine ( n =72) were obtained. The specific activity was 101.32±28.2 GBq/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. [ABSTRACT FROM AUTHOR]

Abstract: [Carbonyl-11C]WAY-100635 is a potent and effective antagonist for the 5-HT1A receptor subtype. We aimed to assess the status of [carbonyl-11C]WAY-100635 and its main radio-metabolites, [carbonyl-11C]desmethyl-WAY-100635 and [carbonyl- 11C]cyclohexanecarboxylic acid, on the basis of an improved radio-HPLC method. Common methods were characterized by preparative HPLC columns with long runtimes and/or high flow rates. Considering the short half-life of C-11, we developed a more rapid and solvent saving HPLC assay, allowing a fast, efficient and reliable quantification of these major metabolites. [Copyright &y& Elsevier]