389888-02-2 Usage
Uses
(S)-CPW 399 is a subtype-selective weakly desensitising AMPA agonist.
Biological Activity
Novel subtype-selective and weakly desensitizing AMPA receptor partial agonist (K i values are 44, 109, 223, 1890 and 2090 nM at GluR5, GluR1, GluR2, GluR3 and GluR4 receptors respectively). Exhibits potent agonist activity at GluR1 and GluR2 subunit-containing AMPA receptors (EC 50 values are 24.9 and 13.9 μM respectively) and is excitotoxic in vitro .
references
[1]. campiani g, morelli e, nacci v, et al. 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, 44(26): 4501-4504.[2]. sinclair c, reavy h, grieve a, et al. inherent desensitisation-preventing properties of a novel, subtype-selective ampa receptor agonist, (s)-cpw 399, as a possible explanation for its excitotoxic action in cultured cerebellar granule cells. neurochem int, 2003, 42(6): 499-510.[3]. salonen v, kallinen s, lopez-picon fr, et al. ampa/kainate receptor-mediated up-regulation of gabaa receptor delta subunit mrna expression in cultured rat cerebellar granule cells is dependent on nmda receptor activation. brain res, 2006, 1087(1): 33-40.[4]. butini s, pickering ds, morelli e, et al. 1h-cyclopentapyrimidine-2,4(1h,3h)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and selective iglur5 modulators. j med chem, 2008, 51(20): 6614-6618.
Check Digit Verification of cas no
The CAS Registry Mumber 389888-02-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,8,9,8,8 and 8 respectively; the second part has 2 digits, 0 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 389888-02:
(8*3)+(7*8)+(6*9)+(5*8)+(4*8)+(3*8)+(2*0)+(1*2)=232
232 % 10 = 2
So 389888-02-2 is a valid CAS Registry Number.
389888-02-2Relevant articles and documents
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
Campiani,Morelli,Nacci,Fattorusso,Ramunno,Novellino,Greenwood,Liljefors,Griffiths,Sinclair,Reavy,Kristensen,Pickering,Schousboe,Cagnotto,Fumagalli,Mennini
, p. 4501 - 4504 (2007/10/03)
(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.