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.
| Identifer | oai:union.ndltd.org:DRESDEN/oai:qucosa:de:qucosa:88806 |
| Date | 03 January 2024 |
| Creators | Moldovan, Rares-Petru, Els-Heindl, Sylvia, Worm, Dennis J., Kniess, Torsten, Kluge, Michael, Beck-Sickinger, Annette G., Deuther-Conrad, Winnie, Krügel, Ute, Brust, Peter |
| Publisher | MDPI |
| Source Sets | Hochschulschriftenserver (HSSS) der SLUB Dresden |
| Language | English |
| Detected Language | English |
| Type | info:eu-repo/semantics/publishedVersion, doc-type:article, info:eu-repo/semantics/article, doc-type:Text |
| Rights | info:eu-repo/semantics/openAccess |
| Relation | 10.3390/ijms18040768 |
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