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, 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

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)4501-4504
Number of pages4
JournalJournal of Medicinal Chemistry
Volume44
Issue number26
DOIs
Publication statusPublished - Dec 20 2001

ASJC Scopus subject areas

  • Organic Chemistry

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