- 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
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(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,Morelli,Nacci,Fattorusso,Ramunno,Novellino,Greenwood,Liljefors,Griffiths,Sinclair,Reavy,Kristensen,Pickering,Schousboe,Cagnotto,Fumagalli,Mennini
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p. 4501 - 4504
(2007/10/03)
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