(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.
Campiani, G., Morelli, E., Nacci, V., Fattorusso, C., Ramunno, A., Novellino, E., et al. (2001). Characterisation of 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. JOURNAL OF MEDICINAL CHEMISTRY, 44(26), 4501-4504 [10.1021/jm015552m].
Characterisation of 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.;Nacci V.;
2001-01-01
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.File | Dimensione | Formato | |
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https://hdl.handle.net/11365/8165
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