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

J Med Chem. 2008 Oct 23;51(20):6614-8. doi: 10.1021/jm800865a.

Stefania Butini ¹, Darryl S Pickering, Elena Morelli, Salvatore Sanna Coccone, Francesco Trotta, Meri De Angelis, Egeria Guarino, Isabella Fiorini, Giuseppe Campiani, Ettore Novellino, Arne Schousboe, Jeppe K Christensen, Sandra Gemma

Affiliations

Affiliation

1 European Research Centre for Drug Discovery and Development (NatSynDrugs), Banchi di Sotto 55, 53100 Siena, Italy.

PMID: 18811139 DOI: 10.1021/jm800865a

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.

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