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Int. J. Mol. Sci. 2017, 18(4), 768; doi:10.3390/ijms18040768

Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging

1
Helmholtz-Zentrum Dresden-Rossendorf e. V., Institute of Radiopharmaceutical Cancer Research, 04318 Leipzig, Germany
2
Institute of Biochemistry, Universität Leipzig, 04103 Leipzig, Germany
3
Department of Psychiatry, Universität Leipzig, 04103 Leipzig, Germany
4
Rudolf Boehm Institute of Pharmacology and Toxicology, Medical Faculty, Universität Leipzig, 04107 Leipzig, Germany
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Academic Editor: Suzanne L. Dickson
Received: 26 January 2017 / Revised: 23 March 2017 / Accepted: 31 March 2017 / Published: 5 April 2017
(This article belongs to the Special Issue Neurobiological Perspectives on Ghrelin)
View Full-Text   |   Download PDF [1981 KB, uploaded 5 April 2017]   |  

Abstract

The ghrelin receptor (GhrR) is a widely investigated target in several diseases. However, the current knowledge of its role and distribution in the brain is limited. Recently, the small and non-peptidic compound (S)-6-(4-bromo-2-fluorophenoxy)-3-((1-isopropylpiperidin-3-yl)methyl)-2-methylpyrido[3,2-d]pyrimidin-4(3H)-one ((S)-9) has been described as a GhrR ligand with high binding affinity. Here, we describe the synthesis of fluorinated derivatives, the in vitro evaluation of their potency as partial agonists and selectivity at GhrRs, and their physicochemical properties. These results identified compounds (S)-9, (R)-9, and (S)-16 as suitable parent molecules for 18F-labeled positron emission tomography (PET) radiotracers to enable future investigation of GhrR in the brain. View Full-Text
Keywords: brain; ghrelin receptor; fluorine; positron emission tomography brain; ghrelin receptor; fluorine; positron emission tomography
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Moldovan, R.-P.; Els-Heindl, S.; Worm, D.J.; Kniess, T.; Kluge, M.; Beck-Sickinger, A.G.; Deuther-Conrad, W.; Krügel, U.; Brust, P. Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging. Int. J. Mol. Sci. 2017, 18, 768.

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