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J Nucl Med. 2008; 49 (Supplement 1):308P
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Radiopharmaceutical Chemistry: Radiopharmacy

Radiopharmacy Posters

Preparation and biological evaluation of [18F]Flumazenil synthesized utilizing a modified microwave reactor system

Katheryn Mandap1, Tatsuo Ido1, Shingo Kasamatsu1, Tetsuya Mori1, Yasushi Kiyono1, Talakad Lohith1, Masato Kobayashi1 and Yasuhisa Fujibayashi1

1 Biomedical Imaging Research Center, University of Fukui, Fukui, Japan

1309

Objectives: This study presents a development in the radiosynthesis of [18F]Flumazenil ([18F]FMZ) incorporating a modified single-mode microwave reactor system. Preliminary biological evaluations were conducted to ensure its utility for routine clinical practice.

Methods: Preparation of dry K18F/K222 complex and radiofluorination of the nitro-flumazenil precursor were achieved using the modified microwave reactor system (capable of stop and flow operation and pressurized reaction). The crude product was pre-purified in a C18 SepPak cartridge followed by reversed-phase preparative HPLC. The isolated [18F]FMZ was evaporated in vacuo and reconstituted. Biodistribution study was performed at 5, 15, 30 and 60 min on mice. PET imaging was also done on mice and rats.

Results: Optimum incorporation of 18F- in the nitro-flumazenil precursor could be obtained in 5 min time utilizing 2 mg of precursor in DMF reacted at 160 C (employing an average microwave power of 25W). The incorporation yield obtained was 39±4%. Radiochemical yield obtained at the end of synthesis was about 17% with the total synthesis time of about 60 min. Biodistribution study showed optimum accumulation in the brain at 5 min with low non-specific binding to other organs. Moreover, no increase in bone uptake was observed indicating the stability of the compound against defluorination. PET imaging of mice and rats showed optimum brain uptake of [18F]FMZ at 10 min after injection.

Conclusions: The developed [18F]FMZ radiosynthesis system which incorporates the utilization of a modified microwave reactor system offers shorter reaction time, simplicity in operation and applicability for use in routine clinical study.





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Right arrow Articles by Fujibayashi, Y.