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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 aim of this research was to synthesize an  18 F–labeled silicon containing exendin-4 peptide ( 18 F- 2 ) and to evaluate its in vitro and  in vivo  behavior in CHL-GLP-1 receptor positive tumor-bearing mice.    18 F–labeled silicon containing exendin-4 peptide ( 18 F- 2 ) was prepared via one-step nucleophilic substitution of a silane precursor with  18 F–fluoride in the presence of acetic acid and K222.  18 F- 2  was then administered to tumor-bearing mice for PET imaging and  ex vivo  biodistribution experiments.    Results    18 F- 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  18 F- 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,  18 F- 2 , is a potential probe for imaging GLP-1R positive tumors.

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