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KMID : 0861420110150020072
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Korean Journal of Nuclear Medicine Technology
2011 Volume.15 No. 2 p.72 ~ p.75
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A Study on the Automation and Optimization of 9-(4-[18F] Fluoro-3-hydroxymethylbutyl) Guanine Synthesis
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Ahn Jae-Seok
Hong Sung-Tack
Kang Se-Hoon
Won Woo-Jae
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Abstract
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Purpose: The HSV1-tk reporter gene system is the most widely used system because of its advantage is that it is
possible to monitor directly without the introduction of a separate reporter gene in case of HSV1-tk suicide gene
therapy. This study was performed to automate 9-(4-[18F] Fluoro-3-hydroxymethylbutyl) guanine ([18F] FHBG)
that are widely used as substrate for the HSV1-tk reporter gene in living organisms with positron emission
tomography (PET) and find the optimized conditions of synthesis.
Materials and Methods:Fully automated
synthesis of [18F] FHBG was performed using Explora-RN (CTI, USA) module. We have changed of reaction
time (3, 5, 10 min) and temperature (110, 120, 130°C) for the optimized conditions of synthesis. Also we
experimented to find the optimal concentration of precursor (5, 7, 10 mg).
Results:[18F] FHBG was purified by
HPLC system and collected at around 10-12 min. Synthesis using Explora-RN module showed a 32.0±1.2%
yield of radiochemical (decay corrected), the purity was greater than 98%. And the entire synthesis time was less
than 48 min. Temperature of the highest synthesis yield was 130°C, reaction time was 5 minutes and
concentration of precursor was 10 mg (recommended volume in manual) (n=36). In contrast to radiochemical
yield of precursor 10 mg (32±1.2%), yield of 5 and 7 mg precursor was unstable.
Conclusion: Automation of [18F] FHBG synthesis at Explora-RN module has been completed. In addition, we were able to obtain optimized reaction time, temperature and concentration of precursor. Therefore this study would be provided more rapid synthesis and higher radiochemical yield.
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KEYWORD
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HSV1-tk , [18F] FHBG , Explora-RN module
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