64Cu- and 68Ga-labelled [Nle(14),Lys(40)(Ahx-NODAGA)NH2]-exendin-4 for pancreatic beta cell imaging in rats.

Mikkola, Kirsi; Kirsi, Mikkola; Yim, Cheng-Bin; Cheng-Bin, Yim; Fagerholm, Veronica; Veronica, Fagerholm; Ishizu, Tamiko; Tamiko, Ishizu; Elomaa, Viki-Veikko; Viki-Veikko, Elomaa; Rajander, Johan; Johan, Rajander; Jurttila, Jori; Jori, Jurttila; Saanijoki, Tiina; Tiina, Saanijoki; Tolvanen, Tuula; Tuula, Tolvanen; Tirri, Marko; Marko, Tirri; ... (2014). 64Cu- and 68Ga-labelled [Nle(14),Lys(40)(Ahx-NODAGA)NH2]-exendin-4 for pancreatic beta cell imaging in rats. Molecular imaging and biology, 16(2), pp. 255-263. Springer 10.1007/s11307-013-0691-2

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PURPOSE Glucagon-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. PROCEDURES 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. RESULTS 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. CONCLUSION [(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.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Reubi, Jean-Claude

Subjects:

500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health

ISSN:

1536-1632

Publisher:

Springer

Language:

English

Submitter:

Andrea Arnold

Date Deposited:

09 Oct 2014 10:59

Last Modified:

09 Oct 2014 10:59

Publisher DOI:

10.1007/s11307-013-0691-2

PubMed ID:

24101374

URI:

https://boris.unibe.ch/id/eprint/52039

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