Abstract
In order to evaluate the neurobiological mechanism causing the psychogenic effects of methylenedioxy-derivatives of amphetamine, the carbon-11 labeled analogues of 3,4-methylenedioxymethamphetamine (MDMA),2 and 2,N-dimethyl-4,5-methylenedioxyamphetamine (MADAM-6)4 were prepared for application in in-vivo PET studies by methylation of 3,4-methylenedioxyamphetamine (MDA)1 and 2-methyl-4,5-methylenedioxyamphetamine3 with [11C]CH3I. The radiochemical yield was determined in dependence on time, temperature and amount of precursor. The best conditions for a fast labeling reaction with carbon-11 on a preparative scale were found to be a reaction time of 10 min using 1 mg of the corresponding dimethyl-precursors1 or3, thus obtaining radiochemical yields of 60% (based on produced [11C]CH3I). Biodistribution studies were performed in rats, a high brain to blood ratio of 7.5 was observed for [11C]MDMA in contrast to a ratio of 3.7 for [11C]MADAM-6.
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Patt, M., Gündisch, D., Wüllner, U. et al. N-[11C]methyl-3,4-methylenedioxyamphetamine (Ecstasy) and 2-methyl-N-[11C]methyl-4,5-methylenedioxyamphetamine: Synthesis and biodistribution studies. J Radioanal Nucl Chem 240, 535–540 (1999). https://doi.org/10.1007/BF02349410
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DOI: https://doi.org/10.1007/BF02349410