Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno.3,2-d] pyrimidin1(2H)- yl) propanoic acid ([3H]-NF608)

Anna Alcaide, Laura Marconi, Ales Marek, Isabell Haym, Birgitte Nielsen, Stine Møllerud, Mikael Jensen, Paola Conti, Darryl S. Pickering, Lennart Bunch

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    Abstract

    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.
    Original languageEnglish
    JournalMedChemComm
    Volume7
    Issue number11
    Pages (from-to)2136-2144
    Number of pages9
    ISSN2040-2503
    DOIs
    Publication statusPublished - 2016

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