N-[11C]methyl-3,4-methylenedioxyamphetamine (Ecstasy) and 2-methyl-N-[11C]methyl-4,5-methylenedioxyamphetamine: Synthesis and biodistribution studies |
| |
| Authors: | M Patt D Gündisch U Wüllner A Blocher K -A Kovar H -J Machulla |
| |
| Institution: | (1) Section Radiopharmacy, PET-Center, Eberhardt-Karls-University Tübingen, Germany;(2) Institute of Pharmacy, Eberhardt-Karls-University Tübingen, Germany;(3) Department of Neurology, Eberhardt-Karls-University Tübingen, Germany |
| |
| 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. |
| |
| Keywords: | |
| 本文献已被 SpringerLink 等数据库收录！ |
|
