Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno.3,2-d] pyrimidin1(2H)- yl) propanoic acid ([3H]-NF608)
التفاصيل البيبلوغرافية
العنوان:
Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno.3,2-d] pyrimidin1(2H)- yl) propanoic acid ([3H]-NF608)
Alcaide, A, Marconi, L, Marek, A, Haym, I, Nielsen, B, Møllerud, S, Jensen, M, Conti, P, Pickering, D S & Bunch, L 2016, ' Synthesis and pharmacological characterization of the selective GluK1 radioligand (S)-2-amino-3-(6-[ 3 H]-2,4-dioxo-3,4-dihydrothieno.3,2-d] pyrimidin1(2H)-yl) propanoic acid ([ 3 H]-NF608) ', MedChemComm, vol. 7, no. 11, pp. 2136-2144 . https://doi.org/10.1039/c6md00339g
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 [H-3]SYM2081, [H-3]-UBP310 and [H-3]-ATPA, however all strategies were work-intensive and thus not attractive. Herein, we report the synthesis of [H-3]-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.
