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)

Research output: Contribution to journalJournal articleResearchpeer-review

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

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

ID: 164572302