MDMA/MADAM-6 Synthesis/Biodistribution , Hive Serious Chemistry


		Rhodium (Chief Bee) 04-21-04 08:37 No 502056				MDMA/MADAM-6 Synthesis/Biodistribution
						N-[¹¹C]methyl-3,4-methylenedioxyamphetamine (Ecstasy) and 2-methyl-N-[¹¹C]methyl-4,5-methylenedioxyamphetamine: Synthesis and biodistribution studies M. Patt, D. Gündisch, U. Wüllner, A. Blocher, K.-A. Kovar, H.-J. Machulla Journal of Radioanalytical and Nuclear Chemistry 240(2), 535–540 (1999) (../rhodium/pdf /mdma.madam-6.pdf) 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-methylenedioxyamphetamine 3 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-precursors 1 or 3, 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. ^{The Hive - Clandestine Chemists Without Borders}