Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties

G Campiani; E Morelli; V Nacci; C Fattorusso; A Ramunno; E Novellino; J Greenwood; T Liljefors; Roger Griffiths; C Sinclair; H Reavy; AS Kristensen; DS Pickering; A Schousboe; A Cagnotto; E Fumagalli; T Mennini

doi:10.1021/jm015552m

Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties

G Campiani, E Morelli, V Nacci, C Fattorusso, A Ramunno, E Novellino, J Greenwood, T Liljefors, Roger Griffiths, C Sinclair, H Reavy, AS Kristensen, DS Pickering, A Schousboe, A Cagnotto, E Fumagalli, T Mennini

Research output: Contribution to journal › Article › peer-review

30 Citations (Scopus)

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 [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.

Original language	English
Pages (from-to)	4501-4504
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	44
DOIs	https://doi.org/10.1021/jm015552m
Publication status	Published - 20 Dec 2001

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Campiani, G., Morelli, E., Nacci, V., Fattorusso, C., Ramunno, A., Novellino, E., Greenwood, J., Liljefors, T., Griffiths, R., Sinclair, C., Reavy, H., Kristensen, AS., Pickering, DS., Schousboe, A., Cagnotto, A., Fumagalli, E., & Mennini, T. (2001). Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties. Journal of Medicinal Chemistry, 44, 4501-4504. https://doi.org/10.1021/jm015552m

@article{f22929fd46474ec2bcbe8b01d583a049,

title = "Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties",

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 [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.",

keywords = "CHANNELS",

author = "G Campiani and E Morelli and V Nacci and C Fattorusso and A Ramunno and E Novellino and J Greenwood and T Liljefors and Roger Griffiths and C Sinclair and H Reavy and AS Kristensen and DS Pickering and A Schousboe and A Cagnotto and E Fumagalli and T Mennini",

note = "This paper represents an output from the multidisciplinary input by 3 transnational groups funded by a CEC Biotech Programme award. Briefly, input comprises: chemical synthesis (Italy); electrophysiology (Denmark); biochemical neuropharmacotoxicology (Scotland, St Andrews). The paper output very much reflects an example of an equal, discipline-based symbiotic contribution by each group.",

year = "2001",

month = dec,

day = "20",

doi = "10.1021/jm015552m",

language = "English",

volume = "44",

pages = "4501--4504",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society (ACS)",

}

Campiani, G, Morelli, E, Nacci, V, Fattorusso, C, Ramunno, A, Novellino, E, Greenwood, J, Liljefors, T, Griffiths, R, Sinclair, C, Reavy, H, Kristensen, AS, Pickering, DS, Schousboe, A, Cagnotto, A, Fumagalli, E & Mennini, T 2001, 'Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties', Journal of Medicinal Chemistry, vol. 44, pp. 4501-4504. https://doi.org/10.1021/jm015552m

Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties. / Campiani, G; Morelli, E; Nacci, V et al.
In: Journal of Medicinal Chemistry, Vol. 44, 20.12.2001, p. 4501-4504.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties

AU - Campiani, G

AU - Morelli, E

AU - Nacci, V

AU - Fattorusso, C

AU - Ramunno, A

AU - Novellino, E

AU - Greenwood, J

AU - Liljefors, T

AU - Griffiths, Roger

AU - Sinclair, C

AU - Reavy, H

AU - Kristensen, AS

AU - Pickering, DS

AU - Schousboe, A

AU - Cagnotto, A

AU - Fumagalli, E

AU - Mennini, T

N1 - This paper represents an output from the multidisciplinary input by 3 transnational groups funded by a CEC Biotech Programme award. Briefly, input comprises: chemical synthesis (Italy); electrophysiology (Denmark); biochemical neuropharmacotoxicology (Scotland, St Andrews). The paper output very much reflects an example of an equal, discipline-based symbiotic contribution by each group.

PY - 2001/12/20

Y1 - 2001/12/20

N2 - (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.

AB - (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.

KW - CHANNELS

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U2 - 10.1021/jm015552m

DO - 10.1021/jm015552m

M3 - Article

SN - 0022-2623

VL - 44

SP - 4501

EP - 4504

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

ER -

Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399, as a novel, potent and subtype-selective agonist of AMPA receptors with densensitization preventing properties

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