Authors:
M. Patt Eberhardt-Karls-University Tübingen Section Radiopharmacy, PET-Center Germany

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D. Gündisch Eberhardt-Karls-University Tübingen Institute of Pharmacy Germany

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U. Wüllner Eberhardt-Karls-University Tübingen Department of Neurology Germany

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A. Blocher
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K. Kovar Eberhardt-Karls-University Tübingen Institute of Pharmacy Germany

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H. Machulla Eberhardt-Karls-University Tübingen Section Radiopharmacy, PET-Center Germany

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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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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation
1968
Volumes
per Year
1
Issues
per Year
12
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)