(S)-CPW399 (2b) is a novel, potent, and subtype-selective AMPA receptor full agonist that, unlike (S)-willardiine and related compounds, in mouse cerebellar granule cells, stimulated an increase in [Ca2+]i, and induced neuronal cell death in a time- and concentration-dependent manner. Compound 2b appears to be a weakly desensitizing, full agonist at AMPA receptors and therefore represents a new pharmacological tool to investigate the role of AMPA receptors in excitotoxicity and their molecular mechanisms of desensitization.
Characterization of the 1H-Cyclopentapyrimidine-2,4(1H,3H)-dione Derivative (S)-CPW399 as a Novel, Potent, and Subtype-Selective AMPA Receptor Full Agonist with Partial Desensitization Properties / Campiani, G., Morelli, E., Nacci, V., Fattorusso, C., Ramunno, A., Novellino, E., Greenwood, J., Liljefors, T., Griffiths, R., Schousboe, A., Pickering, D.S., Sinclair, C.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 44:(2001), pp. 4501-4504. [10.1021/jm015552m]
Characterization of the 1H-Cyclopentapyrimidine-2,4(1H,3H)-dione Derivative (S)-CPW399 as a Novel, Potent, and Subtype-Selective AMPA Receptor Full Agonist with Partial Desensitization Properties
MORELLI E.;FATTORUSSO, CATERINA;NOVELLINO E.;
2001
Abstract
(S)-CPW399 (2b) is a novel, potent, and subtype-selective AMPA receptor full agonist that, unlike (S)-willardiine and related compounds, in mouse cerebellar granule cells, stimulated an increase in [Ca2+]i, and induced neuronal cell death in a time- and concentration-dependent manner. Compound 2b appears to be a weakly desensitizing, full agonist at AMPA receptors and therefore represents a new pharmacological tool to investigate the role of AMPA receptors in excitotoxicity and their molecular mechanisms of desensitization.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
