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XB-ART-38858
J Med Chem 2008 Oct 23;5120:6614-8. doi: 10.1021/jm800865a.
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1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.

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 .


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(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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???displayArticle.link??? J Med Chem