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Open Access Green as soon as Postprint is submitted to ZB.
Synthesis of GPR40 targeting 3H- and 18F-probes towards selective beta cell imaging.
J. Labelled Comp. Radiopharm. 59, 604-610 (2016)
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
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
Language
Publication Year
2016
HGF-reported in Year
2016
ISSN (print) / ISBN
0362-4803
e-ISSN
1099-1344
Quellenangaben
Volume: 59,
Issue: 14,
Pages: 604-610
Publisher
Wiley
Publishing Place
Hoboken
Reviewing status
Peer reviewed
Institute(s)
Institute of Medicinal Chemistry (IMC)
POF-Topic(s)
30203 - Molecular Targets and Therapies
Research field(s)
Enabling and Novel Technologies
PSP Element(s)
G-506300-001
WOS ID
WOS:000392837700003
Scopus ID
84994259783
PubMed ID
27282912
Erfassungsdatum
2016-09-09