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KMID : 0861420100140020104
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Korean Journal of Nuclear Medicine Technology
2010 Volume.14 No. 2 p.104 ~ p.109
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Automated Synthesis of [18F]Fallypride for Routine Clinical Use
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Park Jun-Hyung
Moon Byung-Seok
Lee Hong-Jin
Lee Hyo-Jun
Lee In-Won
Lee Byung-Chul
Kim Sang-Eun
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Abstract
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Purpose: [18F]Fallypride plays an effective radiotracer for the study of dopamine D2/D3 receptor occupancy, neuropsychiatric disorders and aging in humans. This tracer has the potential for clinical use, but automated labeling efficiency showed low radiochemical yields about 5∼20% with relatively long labelling time of fluorine-18. In present study, we describe an improved automatic synthesis of [18F]Fallypride using different base concentration for routine clinical use.
Materials and Methods: Fully automated synthetic process of [18F]Fallypride was perform using the TracerLab FXFN synthesizer under various labeling conditions and tosyl-fallypride was used as a precursor. [18F]Fluoride was extracted with various concentration of K2.2.2./K2CO3 from 18O-enriched water trapped on the ion exchange cartridge. After azeotropic drying, the labeling reaction proceeded in CH3CN at 100 °C for 10 or 30 min. The reaction mixture was purified by reverse phase HPLC and collected organic solution was exchanged by tc-18 Sep-Pak for the clinically available solution.
Results: The optimal labeling condition of [18F]Fallypride in the automatic production was that 2 mg of tosyl-fallypride in
acetonitrile (1 mL) was incubated at 100 °C for 10 min with K2.2.2./K2CO3 (11/0.8 mg). [18F]Fallypride was obtained with high radiochemical yield about 66±1.4% (decay-corrected, n=28) within 51±1.2 min including HPLC purification and solid-phase purification for the final formulation.
Conclusion: [18F]Fallypride was prepared with a significantly improved radiochemical yield with high specific activity and shorten synthetic time. In addition, this automated procedure provides the high reproducibility with no synthesis failures (n=28).
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KEYWORD
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[18F]Fallypride,, Automated radiosynthesis, Dopamine D2/D3 receptor
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