Document Report Card

ID: ALA1140154

Journal: J Med Chem

Title: 1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.

Authors: Butini S, Pickering DS, Morelli E, Coccone SS, Trotta F, De Angelis M, Guarino E, Fiorini I, Campiani G, Novellino E, Schousboe A, Christensen JK, Gemma S.

Abstract: (S)-CPW399 ((S)-1) is a potent and excitotoxic AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate receptor (KA-R) subunit iGluR5. Derivatives 5 and 7, with their unique pharmacological profile, may lead to a better understanding of the different roles and modes of action of iGluR1-5 subunits, paving the way for the synthesis of new potent, subunit selective iGluR5 modulators.

CiteXplore: 18811139

DOI: 10.1021/jm800865a