2. Academic Validation
  3. 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

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

  • J Med Chem. 2001 Dec 20;44(26):4501-4. doi: 10.1021/jm015552m.
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

Affiliation

  • 1 Dipartimento Farmaco Chimico Tecnologico (DFCT), Universita' degli Studi di Siena, via Aldo Moro, 53100 Siena, Italy. campiani@unisi.it
PMID: 11741469 DOI: 10.1021/jm015552m
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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