Details
| Original language | English |
|---|---|
| Pages (from-to) | 604-610 |
| Number of pages | 7 |
| Journal | Journal of Labelled Compounds and Radiopharmaceuticals |
| Volume | 59 |
| Issue number | 14 |
| Early online date | 10 Jun 2016 |
| Publication status | Published - 1 Dec 2016 |
Abstract
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 [3H]-TAK875 and [18F]-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 18F-labelled tracer 2a was achieved with 16.7 ± 5.7% radiochemical yield in a total synthesis time of 60–70 min.
Keywords
- beta cell imaging, fluorine-18, GPR40, tritium
ASJC Scopus subject areas
- Chemistry(all)
- Analytical Chemistry
- Biochemistry, Genetics and Molecular Biology(all)
- Biochemistry
- Medicine(all)
- Radiology Nuclear Medicine and imaging
- Pharmacology, Toxicology and Pharmaceutics(all)
- Drug Discovery
- Chemistry(all)
- Spectroscopy
- Chemistry(all)
- Organic Chemistry
Sustainable Development Goals
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In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 59, No. 14, 01.12.2016, p. 604-610.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Synthesis of GPR40 targeting 3H- and 18F-probes towards selective beta cell imaging
AU - Bertrand, Romain
AU - Hamp, Isabel
AU - Brönstrup, Mark
AU - Weck, Remo
AU - Lukacevic, Mario
AU - Polyak, Andras
AU - Ross, Tobias L.
AU - Gotthardt, Martin
AU - Plettenburg, Oliver
AU - Derdau, Volker
N1 - Funding Information: The research leading to these results has received funding from the People Programme (Marie Curie Actions) of the European Union's Seventh Framework Programme FP7/2007–2013/ under REA grant agreement no. 289932. We acknowledge Ute Messinger and Jenny Schubert for their help with providing analytical data, Juergen Dedio, Birgit Herzog, Inge Kress-Fischer, and Matthias Lohmann for performing the FLIPR Ca
PY - 2016/12/1
Y1 - 2016/12/1
N2 - 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 [3H]-TAK875 and [18F]-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 18F-labelled tracer 2a was achieved with 16.7 ± 5.7% radiochemical yield in a total synthesis time of 60–70 min.
AB - 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 [3H]-TAK875 and [18F]-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 18F-labelled tracer 2a was achieved with 16.7 ± 5.7% radiochemical yield in a total synthesis time of 60–70 min.
KW - beta cell imaging
KW - fluorine-18
KW - GPR40
KW - tritium
UR - http://www.scopus.com/inward/record.url?scp=84994259783&partnerID=8YFLogxK
U2 - 10.1002/jlcr.3412
DO - 10.1002/jlcr.3412
M3 - Article
C2 - 27282912
AN - SCOPUS:84994259783
VL - 59
SP - 604
EP - 610
JO - Journal of Labelled Compounds and Radiopharmaceuticals
JF - Journal of Labelled Compounds and Radiopharmaceuticals
SN - 0362-4803
IS - 14
ER -