18F-Labeling of Radiotracers Functionalized with a Silicon Fluoride Acceptor (SiFA) for Positron Emission Tomography

作者： David Connolly*1, Justin J. Bailey*1, Harun Ilhan2,3, Peter Bartenstein2,3, Carmen Wängler4, Björn Wängler5, Melinda Wuest1, Frank Wuest1, Ralf Schirrmacher1 1Department of Oncology,University of Alberta, 2Department of Nuclear Medicine,University Hospital of Munich, 3ENETS Centre of Excellence, Interdisciplinary Center of Neuroendocrine Tumors of the GastroEnteroPancreatic System,LMU Munich, 4Biomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine,Medical Faculty Mannheim of Heidelberg University, 5Molecular Imaging and Radiochemistry, Department of Clinical Radiology and Nuclear Medicine,Medical Faculty Mannheim of Heidelberg University

简介：

Overview

This article demonstrates a simplified method for labeling ligands with fluorine-18 (F-18) using silicon fluoride acceptor compounds (SiFAs). This approach facilitates the use of F-18 in positron emission tomography (PET) imaging, which is crucial for diagnosing various diseases.

Key Study Components

Area of Science

• Radiopharmaceutical synthesis
• Positron emission tomography (PET)
• Medical imaging

Background

• Fluorine-18 is a key radionuclide for PET imaging.
• It has a half-life of 109 minutes and decays primarily by positron emission.
• Labeling peptides and proteins with F-18 is challenging due to complex synthesis requirements.
• SiFA motifs simplify the labeling process, reducing the need for extensive training and equipment.

Purpose of Study

• To demonstrate a straightforward F-18 labeling protocol.
• To enhance the accessibility of F-18 labeling for various ligands.
• To improve the efficiency of PET imaging techniques.

Methods Used

• Utilization of silicon fluoride acceptor compounds (SiFAs).
• Labeling ligands with fluorine-18.
• Injection of labeled ligands for imaging.
• Evaluation of reaction conditions and precursor quantities.

Main Results

• The SiFA-based method allows for efficient F-18 labeling.
• Reduces the amount of precursor needed for synthesis.
• Enables milder reaction conditions compared to traditional methods.
• Facilitates the production of radiotracers for PET imaging.

Conclusions

• The SiFA approach simplifies the synthesis of F-18 labeled compounds.
• This method can broaden the application of PET imaging in clinical settings.
• Future research may explore additional applications of SiFAs in radiopharmaceuticals.

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