Literature DB >> 11741469

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 Campiani1, 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.   

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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Year:  2001        PMID: 11741469     DOI: 10.1021/jm015552m

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  5 in total

Review 1.  Glutamate receptor ion channels: structure, regulation, and function.

Authors:  Stephen F Traynelis; Lonnie P Wollmuth; Chris J McBain; Frank S Menniti; Katie M Vance; Kevin K Ogden; Kasper B Hansen; Hongjie Yuan; Scott J Myers; Ray Dingledine
Journal:  Pharmacol Rev       Date:  2010-09       Impact factor: 25.468

2.  Altered sensitivity to excitotoxic cell death and glutamate receptor expression between two commonly studied mouse strains.

Authors:  Rozzy Finn; Attila D Kovács; David A Pearce
Journal:  J Neurosci Res       Date:  2010-09       Impact factor: 4.164

3.  Altered sensitivity of cerebellar granule cells to glutamate receptor overactivation in the Cln3(Δex7/8)-knock-in mouse model of juvenile neuronal ceroid lipofuscinosis.

Authors:  Rozzy Finn; Attila D Kovács; David A Pearce
Journal:  Neurochem Int       Date:  2011-02-17       Impact factor: 3.921

4.  Altered glutamate receptor function in the cerebellum of the Ppt1-/- mouse, a murine model of infantile neuronal ceroid lipofuscinosis.

Authors:  Rozzy Finn; Attila D Kovács; David A Pearce
Journal:  J Neurosci Res       Date:  2011-10-04       Impact factor: 4.164

Review 5.  Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.

Authors:  Kasper B Hansen; Lonnie P Wollmuth; Derek Bowie; Hiro Furukawa; Frank S Menniti; Alexander I Sobolevsky; Geoffrey T Swanson; Sharon A Swanger; Ingo H Greger; Terunaga Nakagawa; Chris J McBain; Vasanthi Jayaraman; Chian-Ming Low; Mark L Dell'Acqua; Jeffrey S Diamond; Chad R Camp; Riley E Perszyk; Hongjie Yuan; Stephen F Traynelis
Journal:  Pharmacol Rev       Date:  2021-10       Impact factor: 18.923

  5 in total

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