Jump to main content
Jump to site search

Issue 11, 2016
Previous Article Next Article

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)

Author affiliations

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)

Back to tab navigation

Supplementary files

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
  • Open access: Creative Commons BY license
  •   Request permissions

    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

    This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material.

    Reproduced material should be attributed as follows:

    • For reproduction of material from NJC:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
    • For reproduction of material from PCCP:
      [Original citation] - Published by the PCCP Owner Societies.
    • For reproduction of material from PPS:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
    • For reproduction of material from all other RSC journals:
      [Original citation] - Published by The Royal Society of Chemistry.

    Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.

Search articles by author

Spotlight

Advertisements