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(2 H)-yl)propanoic acid ([3H]-NF608)
Articolo
Data di Pubblicazione:
2016
Citazione:
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(2 H)-yl)propanoic acid ([3H]-NF608) / A. Alcaide, L. Marconi, A. Marek, I. Haym, B. Nielsen, S. Møllerud, M. Jensen, P. Conti, D.S. Pickering, L. Bunch. - In: MEDCHEMCOMM. - ISSN 2040-2503. - 7:11(2016), pp. 2136-2144. [10.1039/c6md00339g]
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.
Tipologia IRIS:
01 - Articolo su periodico
Elenco autori:
A. Alcaide, L. Marconi, A. Marek, I. Haym, B. Nielsen, S. Møllerud, M. Jensen, P. Conti, D.S. Pickering, L. Bunch
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