(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.File | Dimensione | Formato | |
---|---|---|---|
2008_jmc_AMPA_KA.pdf
non disponibili
Tipologia:
Abstract
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
108.32 kB
Formato
Adobe PDF
|
108.32 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/4304
Attenzione
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo