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13 results on '"Bison, Silvia"'

1. A novel process driving Alzheimer's disease validated in a mouse model: Therapeutic potential

Author

Greenfield, Susan A., primary, Cole, Gregory M., additional, Coen, Clive W., additional, Frautschy, Sally, additional, Singh, Ram P., additional, Mekkittikul, Marisa, additional, Garcia‐Ratés, Sara, additional, Morrill, Paul, additional, Hollings, Owen, additional, Passmore, Matt, additional, Hasan, Sibah, additional, Carty, Nikisha, additional, Bison, Silvia, additional, Piccoli, Laura, additional, Carletti, Renzo, additional, Tacconi, Stephano, additional, Chalidou, Anna, additional, Pedercini, Matthew, additional, Kroecher, Tim, additional, Astner, Hubert, additional, and Gerrard, Philip A., additional

Published
2022
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2. A novel process driving Alzheimer's disease validated in a mousemodel: Therapeutic potential.

Author

Greenfield, Susan A., Cole, Gregory M., Coen, Clive W., Frautschy, Sally, Singh, Ram P., Mekkittikul, Marisa, Garcia-Ratés, Sara, Morrill, Paul, Hollings, Owen, Passmore, Matt, Hasan, Sibah, Carty, Nikisha, Bison, Silvia, Piccoli, Laura, Carletti, Renzo, Tacconi, Stephano, Chalidou, Anna, Pedercini, Matthew, Kroecher, Tim, and Astner, Hubert

Subjects
ALZHEIMER'S disease, NICOTINIC receptors, PEPTIDES, TRANSGENIC mice, BRAIN diseases
Abstract

Introduction: The neuronal mechanism driving Alzheimer's disease (AD) is incompletely understood. Methods: Immunohistochemistry, pharmacology, biochemistry, and behavioral testing are employed in two pathological contexts--AD and a transgenic mouse model--to investigate T14, a 14mer peptide, as a key signaling molecule in the neuropathology. Results: T14 increases in AD brains as the disease progresses and is conspicuous in 5XFAD mice, where its immunoreactivity corresponds to that seen in AD: neurons immunoreactive for T14 in proximity to T14-immunoreactive plaques. NBP14 is a cyclized version of T14, which dose-dependently displaces binding of its linear counterpart to alpha-7 nicotinic receptors in AD brains. In 5XFAD mice, intranasal NBP14 for 14 weeks decreases brain amyloid and restores novel object recognition to that in wild-types. Discussion: These findings indicate that the T14 system, for which the signaling pathway is described here, contributes to the neuropathological process and that NBP14 warrants consideration for its therapeutic potential. [ABSTRACT FROM AUTHOR]

Published
2022
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5. Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/DReceptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045)

Author

Bromidge, Steven M., Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J., Granci, Enrica, Leslie, Colin P., Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M., Worby, Angela, Zonzini, Laura, and Zucchelli, Valeria

Abstract

Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of fused tricyclic benzoxazines which are potent 5-HT1A/B/Dreceptor antagonists with and without concomitant human serotonin transporter (hSerT) activity. Optimizing against multiple parameters in parallel identified 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045) as a potent 5-HT1A/B/Dreceptor antagonist with a high degree of selectivity over human ether-à-go-go related gene (hERG) potassium channels, favorable pharmacokinetics, and excellent activity in vivo in rodent pharmacodynamic (PD) models. On the basis of its outstanding overall profile, this compound was progressed as a clinical candidate with the ultimate aim to assess its potential as a faster acting antidepressant/anxiolytic with reduced side-effect burden.

Published
2024
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7. The Efficacy of Sodium Channel Blockers to Prevent Phencyclidine-Induced Cognitive Dysfunction in the Rat: Potential for Novel Treatments for Schizophrenia

Author

Large, Charles H., primary, Bison, Silvia, additional, Sartori, Ilaria, additional, Read, Kevin D., additional, Gozzi, Alessandro, additional, Quarta, Davide, additional, Antolini, Marinella, additional, Hollands, Emma, additional, Gill, Catherine H., additional, Gunthorpe, Martin J., additional, Idris, Nagi, additional, Neill, Jo C., additional, and Alvaro, Giuseppe S., additional

Published
2011
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8. Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D Receptor Antagonist

Author

Leslie, Colin P., primary, Biagetti, Matteo, additional, Bison, Silvia, additional, Bromidge, Steven M., additional, Di Fabio, Romano, additional, Donati, Daniele, additional, Falchi, Alessandro, additional, Garnier, Martine J., additional, Jaxa-Chamiec, Albert, additional, Manchee, Gary, additional, Merlo, Giancarlo, additional, Pizzi, Domenica A., additional, Stasi, Luigi P., additional, Tibasco, Jessica, additional, Vong, Antonio, additional, Ward, Simon E., additional, and Zonzini, Laura, additional

Published
2010
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9. Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045)

Author

Bromidge, Steven M., primary, Arban, Roberto, additional, Bertani, Barbara, additional, Bison, Silvia, additional, Borriello, Manuela, additional, Cavanni, Paolo, additional, Dal Forno, Giovanna, additional, Di-Fabio, Romano, additional, Donati, Daniele, additional, Fontana, Stefano, additional, Gianotti, Massimo, additional, Gordon, Laurie J., additional, Granci, Enrica, additional, Leslie, Colin P., additional, Moccia, Luca, additional, Pasquarello, Alessandra, additional, Sartori, Ilaria, additional, Sava, Anna, additional, Watson, Jeannette M., additional, Worby, Angela, additional, Zonzini, Laura, additional, and Zucchelli, Valeria, additional

Published
2010
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11. Discovery of 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, Selective, and Orally Active 5-HT1A/B/D Receptor Antagonist.

Author

Leslie, Colin P., Biagetti, Matteo, Bison, Silvia, Bromidge, Steven M., Di Fabio, Romano, Donati, Daniele, Falchi, Alessandro, Garnier, Martine J., Jaxa-Chamiec, Albert, Manchee, Gary, Merlo, Giancarlo, Pizzi, Domenica A., Stasi, Luigi P., Tibasco, Jessica, Vong, Antonio, Ward, Simon E., and Zonzini, Laura

Published
2010
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12. Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).

Author

Bromidge, Steven M., Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J., Granci, Enrica, Leslie, Colin P., Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M., and Worby, Angela

Published
2010
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