(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. © 2008 American Chemical Society.

Butini, S., Pickering, D.S., Morelli, E., Coccone, S.S., Trotta, F., De Angelis, M., et al. (2008). 1H-Cyclopentapyrimidine-2,4(1H,3H)-dione-Related Ionotropic Glutamate Receptors Ligands. Structure-Activity Relationships and Identification of Potent and Selective iGluR5 Modulators. JOURNAL OF MEDICINAL CHEMISTRY, 51(20), 6614-6618 [10.1021/jm800865a].

1H-Cyclopentapyrimidine-2,4(1H,3H)-dione-Related Ionotropic Glutamate Receptors Ligands. Structure-Activity Relationships and Identification of Potent and Selective iGluR5 Modulators

Butini, Stefania;Trotta, Francesco;De Angelis, Meri;Guarino, Egeria;Fiorini, Isabella;Campiani, Giuseppe;Gemma, Sandra
2008-01-01

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. © 2008 American Chemical Society.
2008
Butini, S., Pickering, D.S., Morelli, E., Coccone, S.S., Trotta, F., De Angelis, M., et al. (2008). 1H-Cyclopentapyrimidine-2,4(1H,3H)-dione-Related Ionotropic Glutamate Receptors Ligands. Structure-Activity Relationships and Identification of Potent and Selective iGluR5 Modulators. JOURNAL OF MEDICINAL CHEMISTRY, 51(20), 6614-6618 [10.1021/jm800865a].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/4304
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