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Issue 11, 2016
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Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)

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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 [3H]-SYM2081, [3H]-UBP310 and [3H]-ATPA, however all strategies were work-intensive and thus not attractive. Herein, we report the synthesis of [3H]-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.

Graphical abstract: Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)

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Publication details

The article was received on 17 Jun 2016, accepted on 17 Aug 2016 and first published on 02 Sep 2016


Article type: Research Article
DOI: 10.1039/C6MD00339G
Citation: Med. Chem. Commun., 2016,7, 2136-2144
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    Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)

    A. Alcaide, L. Marconi, A. Marek, I. Haym, B. Nielsen, S. Møllerud, M. Jensen, P. Conti, D. S. Pickering and L. Bunch, Med. Chem. Commun., 2016, 7, 2136
    DOI: 10.1039/C6MD00339G

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