Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging
AbstractThe 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
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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.
Moldovan R-P, Els-Heindl S, Worm DJ, Kniess T, Kluge M, Beck-Sickinger AG, Deuther-Conrad W, Krügel U, Brust P. Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging. International Journal of Molecular Sciences. 2017; 18(4):768.Chicago/Turabian Style
Moldovan, Rareş-Petru; Els-Heindl, Sylvia; Worm, Dennis J.; Kniess, Torsten; Kluge, Michael; Beck-Sickinger, Annette G.; Deuther-Conrad, Winnie; Krügel, Ute; Brust, Peter. 2017. "Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging." Int. J. Mol. Sci. 18, no. 4: 768.
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