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

Research output: Contribution to journalJournal articleResearchpeer-review

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, Darryl Pickering

(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.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume44
Issue number26
Pages (from-to)4501-4
Number of pages3
ISSN0022-2623
Publication statusPublished - 2001

Bibliographical note

Keywords: Alanine; Animals; Brain; Cell Death; Cell Line; Electrophysiology; Excitatory Amino Acid Agonists; Ligands; Mice; Models, Molecular; Neurons; Oocytes; Pyrimidines; Pyrimidinones; Radioligand Assay; Rats; Receptors, AMPA; Recombinant Proteins; Stereoisomerism; Xenopus laevis

ID: 20122679