Radiosynthesis and evaluation of an 18F-labeled silicon containing exendin-4 peptide as a PET probe for imaging insulinoma.
- Dialer LO 1Center for Radiopharmaceutical Sciences (CRS) of ETH, PSI and USZ, Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Hönggerberg, ETH Zurich, Zurich, Switzerland.
- Jodal A 2Center for Radiopharmaceutical Sciences (CRS), Research Department Biology and Chemistry, Paul Scherrer Institut, CH-5232 Villigen, Switzerland.
- Schibli R 1Center for Radiopharmaceutical Sciences (CRS) of ETH, PSI and USZ, Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Hönggerberg, ETH Zurich, Zurich, Switzerland.
- Ametamey SM 1Center for Radiopharmaceutical Sciences (CRS) of ETH, PSI and USZ, Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Hönggerberg, ETH Zurich, Zurich, Switzerland.
- Béhé M 2Center for Radiopharmaceutical Sciences (CRS), Research Department Biology and Chemistry, Paul Scherrer Institut, CH-5232 Villigen, Switzerland.
- 2018-03-06
Published in:
- EJNMMI radiopharmacy and chemistry. - 2018
English
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 18F-labeled silicon containing exendin-4 peptide (18F-2) and to evaluate its in vitro and in vivo behavior in CHL-GLP-1 receptor positive tumor-bearing mice. 18F-labeled silicon containing exendin-4 peptide (18F-2) was prepared via one-step nucleophilic substitution of a silane precursor with 18F-fluoride in the presence of acetic acid and K222. 18F-2 was then administered to tumor-bearing mice for PET imaging and ex vivo biodistribution experiments.
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.
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 18F-labeled silicon containing exendin-4 peptide (18F-2) and to evaluate its in vitro and in vivo behavior in CHL-GLP-1 receptor positive tumor-bearing mice. 18F-labeled silicon containing exendin-4 peptide (18F-2) was prepared via one-step nucleophilic substitution of a silane precursor with 18F-fluoride in the presence of acetic acid and K222. 18F-2 was then administered to tumor-bearing mice for PET imaging and ex vivo biodistribution experiments.
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.
- Language
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- English
- Open access status
- gold
- Identifiers
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- DOI 10.1186/s41181-017-0036-6
- PMID 29503858
- Persistent URL
- https://sonar.ch/global/documents/185726
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