258875-17-1Relevant academic research and scientific papers
Radiosynthesis of Carbon-11 labelled N-methyl-2-(arylthio)benzylamines: Potential radiotracers for the serotonin reuptake receptor
Wilson, Alan A.,Houle, Sylvain
, p. 1277 - 1288 (1999)
The potent and selective serotonin reuptake inhibitor, N,N-dimethyl-2-(2-amino-4-trifluoromethylphenylthio)benzylamine (1), and a potential metabolite, N-methyl-2-(2-amino-4-trifluoromethylphenylthio)benzylamine (2) were radiolabelled with Carbon-11 as potential positron emission tomography (PET) radiotracers. Both [11C]-(1) and [11C]-(2) were obtained in good radiochemical yield by alkylation of their respective normethyl precursors with [11C]-iodomethane in dimethylformamide. Upon HPLC purification and formulation radiochemically pure products were obtained in 25-30% yield (from [11C]-iodomethane, uncorrected) with specific activities of 25-40 GBq/mole. To further establish the site of labeling, [13C]-(1) and [13C]-(2) were also synthesised, using [13C]-iodomethane, for 13C NMR analysis. Preliminary biodistribution studies in rats show that both [11C]-(1) and [11C]-(2) efficiently and rapidly cross the blood brain barrier.
