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 Campiani; 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; Darryl Pickering

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 Campiani, 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, Darryl Pickering

27 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 [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

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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, A. S., Pickering, D. S., Schousboe, A., Cagnotto, A., Fumagalli, E., Mennini, T., & Pickering, D. (2001). 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. Journal of Medicinal Chemistry, 44(26), 4501-4.

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, G; Morelli, E; Nacci, V et al.

In: Journal of Medicinal Chemistry, Vol. 44, No. 26, 2001, p. 4501-4.

Research output: Contribution to journal › Journal article › Research › peer-review

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 & Pickering, D 2001, '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', Journal of Medicinal Chemistry, vol. 44, no. 26, pp. 4501-4.

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title = "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",

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.",

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 R Griffiths and C Sinclair and H Reavy and Kristensen, {A S} and Pickering, {D S} and A Schousboe and A Cagnotto and E Fumagalli and T Mennini and Darryl Pickering",

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",

year = "2001",

language = "English",

volume = "44",

pages = "4501--4",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "26",

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TY - JOUR

T1 - 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

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, R

AU - Sinclair, C

AU - Reavy, H

AU - Kristensen, A S

AU - Pickering, D S

AU - Schousboe, A

AU - Cagnotto, A

AU - Fumagalli, E

AU - Mennini, T

AU - Pickering, Darryl

N1 - 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

PY - 2001

Y1 - 2001

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 [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.

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 [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.

M3 - Journal article

C2 - 11741469

SN - 0022-2623

VL - 44

SP - 4501

EP - 4504

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 26

ER -

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

Abstract

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