Chalupnik, Paulina; Vialko, Alina; Pickering, Darryl S.; Hinkkanen, Markus; Donbosco, Stephanie; Moeller, Thor C.; Jensen, Anders A.; Nielsen, Birgitte; Bay, Yasmin; Kristensen, Anders S.; Johansen, Tommy N.; Latka, Kamil; Bajda, Marek; Szymanska, Ewa published the artcile< Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype>, COA of Formula: C9H8O, the main research area is quinoxalinedione preparation glutamate receptor antagonist; glutamate receptors; kainate receptors; subunit selectivity.
In search of selective ligands for the GluK3 kainate receptor subtype, a series of I [R = 3-Me Ph, 4-Me Ph, 4-Et Ph, etc] analogs was synthesized and pharmacol. characterized at selected recombinant ionotropic glutamate receptors. Among them, compound I [R = imidazo[1,2-b]pyridazin-3-ylmethyl] was found to be a competitive GluK3 antagonist with submicromolar affinity and unprecedented high binding selectivity, showing a 400-fold preference for GluK3 over other homomeric receptors GluK1, GluK2, GluK5 and GluA2. Furthermore, in functional assays performed for selected metabotropic glutamate receptor subtypes, I [R = imidazo[1,2-b]pyridazin-3-ylmethyl] did not show agonist or antagonist activity. The mol. determinants underlying the observed affinity profile of I [R = imidazo[1,2-b]pyridazin-3-ylmethyl] were analyzed using mol. docking and mol. dynamics simulations performed for individual GluK1 and GluK3 ligand-binding domains.
International Journal of Molecular Sciences published new progress about Kainate receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (GluK3). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, COA of Formula: C9H8O.
Referemce:
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