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

Research output: Contribution to journalJournal articleResearchpeer-review

  • Stefania Butini
  • Pickering, Darryl S
  • Elena Morelli
  • Salvatore Sanna Coccone
  • Francesco Trotta
  • Meri De Angelis
  • Egeria Guarino
  • Isabella Fiorini
  • Giuseppe Campiani
  • Ettore Novellino
  • Schousboe, Arne
  • Jeppe K Christensen
  • Sandra Gemma
(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.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Issue number20
Pages (from-to)6614-8
Publication statusPublished - 2008

ID: 6747715