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…

Index: 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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Citation Number: 13

Abstract

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 ...