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 journalJournal articleResearchpeer-review

Standard

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; 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, Darryl.

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

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

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.

APA

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.

Vancouver

Campiani G, Morelli E, Nacci V, Fattorusso C, Ramunno A, Novellino E 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. Journal of Medicinal Chemistry. 2001;44(26):4501-4.

Author

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, Darryl. / 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. In: Journal of Medicinal Chemistry. 2001 ; Vol. 44, No. 26. pp. 4501-4.

Bibtex

@article{54c353b06e8f11df928f000ea68e967b,
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",

}

RIS

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

VL - 44

SP - 4501

EP - 4504

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 26

ER -

ID: 20122679