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  • Title: A simplified one-pot automated synthesis of [18F]FHBG for imaging reporter gene expression.
    Author: Tang G, Tang X, Li H, Wang M, Li B, Liang M, Wu H, Wang Q.
    Journal: Nucl Med Commun; 2010 Mar; 31(3):211-6. PubMed ID: 20032804.
    Abstract:
    BACKGROUND: 9-(4-[F]fluoro-3-hydroxymethylbutyl) guanine ([F]FHBG) has been used as a reporter probe to image the expression of the herpes simplex virus type 1 thymidine kinase (TK) reporter gene in living organisms with positron emission tomography (PET). However, the routine production of [F]FHBG presents many challenging laboratory requirements. AIM: To develop a simple one-pot fully-automated synthesis procedure of [F]FHBG amenable for its routine use in reporter gene expression PET imaging studies. METHODS: A TRACERlab FXF-N synthesizer was substantially modified and adapted to the synthesis of [F]FHBG through the two-step one-pot procedure. After the fluorination reaction of the tosylate precursor and the hydrolysis of the intermediate product in the same reaction vessel, the final product was purified by Sep-Pak cartridges instead of the high performance liquid chromatography system. RESULTS: The fully automated synthesis of [F]FHBG with Sep-Pak purification was performed within a short synthesis time. The decay-uncorrected radiochemical yield of [F]FHBG was 8-14% (n=10), the radiochemical purity was more than 99%, and the entire synthesis time was less than 40 min. In addition, the PET image of theTK-transfected nude mice model indicated a much higher uptake of [F]FHBG in the TK-transfected tumor region than in the control tumor region. CONCLUSION: The automated synthesis of [F]FHBG is very easy to carry out using one-pot reactions combined with Sep-Pak purification. The synthetic [F]FHBG can be used for PET imaging and monitoring of in vivo herpes simplex virus type 1 TK gene expression.
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