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. 2001 Dec 20;44(26):4501-4.
doi: 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

G Campiani  1 , E Morelli, V Nacci, C Fattorusso, A Ramunno, E Novellino, J Greenwood, T Liljefors, R Griffiths, C Sinclair, H Reavy, A S Kristensen, D S Pickering, A Schousboe, A Cagnotto, E Fumagalli, T Mennini
Affiliations

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

G Campiani et al. J Med Chem. .

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 [Ca(2+)](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.

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