Name: 4-EthynylpyridineIn 2022 ,《Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype》 appeared in International Journal of Molecular Sciences. The author of the article were 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. The article conveys some information:
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.4-Ethynylpyridine(cas: 2510-22-7Name: 4-Ethynylpyridine) was used in this study.
4-Ethynylpyridine(cas: 2510-22-7) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Name: 4-Ethynylpyridine