64Cu- and 68Ga-labelled [Nle(14),Lys(40)(Ahx-NODAGA)NH2]-exendin-4 for pancreatic beta cell imaging in rats.
Kirsi Mikkola, Mikkola Kirsi, Cheng-Bin Yim, Yim Cheng-Bin, Veronica Fagerholm, Fagerholm Veronica, Tamiko Ishizu, Ishizu Tamiko, Viki-Veikko Elomaa, Elomaa Viki-Veikko, Johan Rajander, Rajander Johan, Jori Jurttila, Jurttila Jori, Tiina Saanijoki, Saanijoki Tiina, Tuula Tolvanen, Tolvanen Tuula, Marko Tirri, Tirri Marko, Eleni Gourni, Gourni Eleni, Martin Béhé, Béhé Martin, Martin Gotthardt, Gotthardt Martin, Jean Claude Reubi, Reubi Jean Claude, Helmut Mäcke, Mäcke Helmut, Anne Roivainen, Roivainen Anne, Olof Solin, Solin Olof, Pirjo Nuutila, Nuutila Pirjo
Molecular imaging and biology 2014 AprGlucagon-like peptide-1 receptor (GLP-1R) is a molecular target for imaging of pancreatic beta cells. We compared the ability of [Nle(14),Lys(40)(Ahx-NODAGA-(64)Cu)NH2]-exendin-4 ([(64)Cu]NODAGA-exendin-4) and [Nle(14),Lys(40)(Ahx-NODAGA-(68)Ga)NH2]-exendin-4 ([(68)Ga]NODAGA-exendin-4) to detect native pancreatic islets in rodents. The stability, lipophilicity and affinity of the radiotracers to the GLP-1R were determined in vitro. The biodistribution of the tracers was assessed using autoradiography, ex vivo biodistribution and PET imaging. Estimates for human radiation dosimetry were calculated. We found GLP-1R-specific labelling of pancreatic islets. However, the pancreas could not be visualised in PET images. The highest uptake of the tracers was observed in the kidneys. Effective dose estimates for [(64)Cu]NODAGA-exendin-4 and [(68)Ga]NODAGA-exendin-4 were 0.144 and 0.012 mSv/MBq, respectively. [(64)Cu]NODAGA-exendin-4 might be more effective for labelling islets than [(68)Ga]NODAGA-exendin-4. This is probably due to the lower specific radioactivity of [(68)Ga]NODAGA-exendin-4 compared to [(64)Cu]NODAGA-exendin-4. The radiation dose in the kidneys may limit the use of [(64)Cu]NODAGA-exendin-4 as a clinical tracer.
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Kirsi Mikkola, Mikkola Kirsi, Cheng-Bin Yim, Yim Cheng-Bin, Veronica Fagerholm, Fagerholm Veronica, Tamiko Ishizu, Ishizu Tamiko, Viki-Veikko Elomaa, Elomaa Viki-Veikko, Johan Rajander, Rajander Johan, Jori Jurttila, Jurttila Jori, Tiina Saanijoki, Saanijoki Tiina, Tuula Tolvanen, Tolvanen Tuula, Marko Tirri, Tirri Marko, Eleni Gourni, Gourni Eleni, Martin Béhé, Béhé Martin, Martin Gotthardt, Gotthardt Martin, Jean Claude Reubi, Reubi Jean Claude, Helmut Mäcke, Mäcke Helmut, Anne Roivainen, Roivainen Anne, Olof Solin, Solin Olof, Pirjo Nuutila, Nuutila Pirjo. 64Cu- and 68Ga-labelled [Nle(14),Lys(40)(Ahx-NODAGA)NH2]-exendin-4 for pancreatic beta cell imaging in rats. Molecular imaging and biology. 2014 Apr;16(2):255-63
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PMID: 24101374
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