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

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.

Identiferoai:union.ndltd.org:DRESDEN/oai:qucosa:de:qucosa:88806
Date03 January 2024
CreatorsMoldovan, Rares-Petru, Els-Heindl, Sylvia, Worm, Dennis J., Kniess, Torsten, Kluge, Michael, Beck-Sickinger, Annette G., Deuther-Conrad, Winnie, Krügel, Ute, Brust, Peter
PublisherMDPI
Source SetsHochschulschriftenserver (HSSS) der SLUB Dresden
LanguageEnglish
Detected LanguageEnglish
Typeinfo:eu-repo/semantics/publishedVersion, doc-type:article, info:eu-repo/semantics/article, doc-type:Text
Rightsinfo:eu-repo/semantics/openAccess
Relation10.3390/ijms18040768

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