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 journal › Journal article › Research › peer-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
Pickering, Darryl S
Schousboe, Arne
A Cagnotto
E Fumagalli
T Mennini
Pickering, Darryl S

(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 language	English
Journal	Journal of Medicinal Chemistry
Volume	44
Issue number	26
Pages (from-to)	4501-4
Number of pages	3
ISSN	0022-2623
Publication status	Published - 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