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.
|Titolo:||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)|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||2016|
|Digital Object Identifier (DOI):||10.1039/c6md00339g|
|Appare nelle tipologie:||01 - Articolo su periodico|