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Bertrand, R.* ; Hamp, I.* ; Brönstrup, M.* ; Weck, R.* ; Lukacevic, M.* ; Polyak, A.* ; Ross, T.L.* ; Gotthardt, M.* ; Plettenburg, O. ; Derdau, V.*

Synthesis of GPR40 targeting 3H- and 18F-probes towards selective beta cell imaging.

J. Labelled Comp. Radiopharm. 59, 604-610 (2016)
DOI PMC
Open Access Green as soon as Postprint is submitted to ZB.
Diabetes affects an increasing number of patients worldwide and is responsible for a significant rise in healthcare expenses. Imaging of β-cells in vivo is expected to contribute to an improved understanding of the underlying pathophysiology, improved diagnosis, and development of new treatment options for diabetes. Here, we describe the first radiosyntheses of [(3) H]-TAK875 and [(18) F]-TAK875 derivatives to be used as β-cell imaging probes addressing the free fatty acid receptor 1 (FFAR1/GPR40). The fluorine-labeled derivative showed similar agonistic activity as TAK875 in a functional assay. The radiosynthesis of the (18) F-labelled tracer 2a was achieved with 16.7 ± 5.7% radiochemical yield in a total synthesis time of 60-70 min.
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Publication type Article: Journal article
Document type Scientific Article
Corresponding Author
Keywords Gpr40 ; Beta Cell Imaging ; Fluorine-18 ; Tritium; Positron-emission-tomography; Type-2 Diabetes-mellitus; Ene Click Chemistry; Free Fatty-acids; Receptor; Discovery; Tak-875; Agonist
ISSN (print) / ISBN 0362-4803
e-ISSN 1099-1344
Journal Journal of Labelled Compounds and Radiopharmaceuticals
Quellenangaben Volume: 59, Issue: 14, Pages: 604-610 Article Number: , Supplement: ,
Publisher Wiley
Publishing Place Hoboken
Non-patent literature Publications
Reviewing status Peer reviewed
Institute(s) Institute of Medicinal Chemistry (IMC)