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

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D. GündischEberhardt-Karls-University Institute of Pharmacy Tübingen Germany

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U. WüllnerEberhardt-Karls-University Department of Neurology Tübingen Germany

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A. StahlschmidtEberhardt-Karls-University Section Radiopharmacy, PET-Center Tübingen Germany

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K. KovarEberhardt-Karls-University Institute of Pharmacy Tübingen Germany

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

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Abstract  

N-[11C]methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine ([11C]MBDB) 3 was prepared by methylation of the demethyl precursor BDB with [11C]CHI. The radiosynthesis was optimized with regard to temperature, reaction time and amount of precursor, best results (i.e., 84% radiochemical yield, based on [11C]CH3I activity) were obtained using 3 mg BDB at a reaction temperature of 130 °C in 8 minutes. With respect to a facilitated workup routine, productions were performed with 0.6 mg BDB at 110 °C for 10 minutes, yielding more than 50% of 3. The radiochemical purity of the final tracer solution was >98%, the specific activity was determined to be 300 GBq/mol (8000 Ci/mmol). Biodistribution, studies in rats showed two major metabolic pathways as indicated by an increasing liver uptake (9.1% ID/organ at 5 minutes to 21% ID/organ at 30 minutes) and a high urine activity (up to 16% ID/g). In brain tracer uptake was more than 1%, with a brain to blood ratio of almost 12 resulting from a very rapid blood clearance of 3.

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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)

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