Selective Kainate Receptor (GluK1) Ligands Structurally Based upon 1 H-Cyclopentapyrimidin-2, 4 (1 H, 3 H)-dione: Synthesis, Molecular Modeling, and …

…, S Butini, S Sanna Coccone, S Gemma…

文献索引：Venskutonyte, Raminta; Butini, Stefania; Sanna Coccone, Salvatore; Gemma, Sandra; Brindisi, Margherita; Kumar, Vinod; Guarino, Egeria; Maramai, Samuele; Valenti, Salvatore; Amir, Ahmad; Valades, Elena Anton; Frydenvang, Karla; Kastrup, Jette S.; Novellino, Ettore; Campiani, Giuseppe; Pickering, Darryl S. Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4793 - 4805

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被引用次数: 13

摘要

The physiological function of kainate receptors (GluK1–GluK5) in the central nervous system is not fully understood yet. With the aim of developing potent and selective GluK1 ligands, we have synthesized a series of new thiophene-based GluK1 agonists (6a–c) and antagonists (7a–d). Pharmacological evaluation revealed that they are selective for the GluK1 subunit, with 7b being the most subtype-selective ligand reported to date (GluK1 vs ...