期刊
MEDCHEMCOMM
卷 7, 期 11, 页码 2136-2144出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c6md00339g
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资金
- Department of Drug Design and Pharmacology
- Academy of Sciences of the Czech Republic [RVO: 61388963]
- Lundbeck Foundation [R170-2014-979] Funding Source: researchfish
The kainic acid receptors belong to the class of ionotropic glutamate receptors and comprise five subunits named GluK1-5. Radioligands are essential tools for use in binding assays aimed at ligand-receptor structure-activity-relationship studies. Previous work has led to the synthesis of GluK1 radioligands [H-3]SYM2081, [H-3]-UBP310 and [H-3]-ATPA, however all strategies were work-intensive and thus not attractive. Herein, we report the synthesis of [H-3]-NF608 and subsequent pharmacological evaluation at homomeric recombinant rat GluK1 receptors. Binding affinities of a series of standard GluK1 ligands were shown to be in line with previously reported affinities obtained by use of already reported radioligands.
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