Radiosynthesis of [18F]-flumazenil Using an Isotopic Approach

利用同位素方法放射合成[18F]-氟马西尼

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Abstract

BACKGROUND: Fluorine-18 ((18)F) flumazenil (FMZ) has been synthesized using various precursors, and its role has been explored in imaging Gamma-aminobutyric acid-A receptors. AIM AND OBJECTIVE: The main objective was to synthesize ((18)F) FMZ using isotopic substitution. MATERIALS AND METHODS: Around 18 ± 2 GBq was added to the module, dried, and radiolabeling was standardized with 3.0 mg of the FMZ precursor at various temperatures (110°C -160°C) for 10-30 min. The product was finally eluted with 20% ethanol (in phosphate buffer). The final product was characterized by high-performance liquid chromatography (HPLC). The stability was evaluated in water, saline, and phosphate-buffered saline for 4 h. RESULTS: The radiolabelling efficiency of cartridge-based purification was 16 ± 4% (n = 10) with a radiochemical purity of 96.5 ± 1.8%, whereas in HPLC-based purification, the yield was 10 ± 4% (n = 5) with a radiochemical purity of 97.3 ± 1.4%. The specific activity was 120 ± 20 GBq/μmol. CONCLUSIONS: ((18)F) FMZ was successfully synthesized using an isotopic approach and could be used as an alternative cheaper option for the synthesis.

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