Radiosynthesis and evaluation of an 18F-labeled silicon containing exendin-4 peptide as a PET probe for imaging insulinoma

18F 标记含硅的 exendin-4 肽的放射合成及作为胰岛素瘤成像 PET 探针的评估

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作者:Lukas O Dialer, Andreas Jodal, Roger Schibli, Simon M Ametamey, Martin Béhé

Background

Analogues of exendin-4 have been radiolabeled for imaging the glucagon-like peptide type 1 receptors (GLP-1R) which are overexpressed in insulinoma. The

Conclusions

This exendin-4 analogue, 18F-2, is a potential probe for imaging GLP-1R positive tumors.

Results

18F-2 was produced in a radiochemical yield (decay corrected) of 1.5% and a molar activity of max. 16 GBq/μmol. The GLP-1R positive tumors were clearly visualized by PET imaging. Biodistribution studies showed reduced uptake of 18F-2 in the kidneys compared to radiometal labeled exendin-4 derivatives. The radiotracer showed specific tumour uptake which remained steady over 2 h. Conclusions: This exendin-4 analogue, 18F-2, is a potential probe for imaging GLP-1R positive tumors.

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