Search Results - "Aldegheri, Laura"
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Pharmacological characterisation of MDI-222, a novel AMPA receptor positive allosteric modulator with an improved safety profile
Published in Journal of psychopharmacology (Oxford) (01-01-2020)“…Purpose: There is considerable interest in positive allosteric modulators (PAMs) of the α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionate (AMPA) subtype of…”
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Identification of positive modulators of TRPM5 channel from a high-throughput screen using a fluorescent membrane potential assay
Published in SLAS discovery (01-01-2022)“…Transient Receptor Potential Melastatin 5 (TRPM5) is an intracellular calcium-activated cation-selective ion channel expressed in a variety of cell types…”
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From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents
Published in Journal of medicinal chemistry (13-05-2021)“…Transient receptor potential cation channel subfamily M member 5 (TRPM5) is a nonselective monovalent cation channel activated by intracellular Ca2+ increase…”
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A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons
Published in The Journal of pharmacology and experimental therapeutics (01-09-2015)“…Kv3.1 and Kv3.2 high voltage-activated potassium channels, which display fast activation and deactivation kinetics, are known to make a crucial contribution to…”
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Characterization of a New Hemoprotein in the YeastSaccharomyces cerevisiae
Published in The Journal of biological chemistry (19-02-1999)“…The Saccharomyces cerevisiae gene YNL234w encodes a 426-amino acid-long protein that shares significant similarities with the globin family. Compared with…”
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Integration of Lead Optimization with Crystallography for a Membrane-Bound Ion Channel Target: Discovery of a New Class of AMPA Receptor Positive Allosteric Modulators
Published in Journal of medicinal chemistry (13-01-2011)“…A novel series of AMPAR positive modulators is described that were identified by high throughput screening. The molecules of the series have been optimized…”
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Discovery of N-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a Novel Clinical AMPA Receptor Positive Modulator
Published in Journal of medicinal chemistry (12-08-2010)“…A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical…”
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N-Substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators
Published in Bioorganic & medicinal chemistry letters (01-12-2010)“…This work describes the synthesis and biological activity of a series of pyrrolidine and tetrahydrofuran analogues as AMPA receptor positive modulators. Ar =…”
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Characterization of the Reverse Use Dependent Block of Voltage Gated Sodium Channels
Published in Biophysical journal (01-01-2010)Get full text
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Optimisation of an integrated approach for cardiac safety profiling of novel compounds
Published in Journal of pharmacological and toxicological methods (01-07-2013)Get full text
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Pharmacological properties of rat α7 nicotinic receptors expressed in native and recombinant cell systems
Published in European journal of pharmacology (12-06-2002)“…The pharmacological properties of the rat α7 nicotinic acetylcholine receptor endogenously expressed in PC12 cells and recombinantly expressed in GH4C1 cells…”
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Pharmacological properties of rat alpha 7 nicotinic receptors expressed in native and recombinant cell systems
Published in European journal of pharmacology (12-06-2002)“…The pharmacological properties of the rat alpha7 nicotinic acetylcholine receptor endogenously expressed in PC12 cells and recombinantly expressed in GH4C1…”
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The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3
Published in Neuroscience letters (31-07-2003)“…The effects of fluoxetine (Prozac™) on the activity of human small-conductance calcium-activated potassium (SK) channels were investigated utilizing a…”
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14
Characterization of a new hemoprotein in the yeast Saccharomyces cerevisiae
Published in The Journal of biological chemistry (19-02-1999)“…The Saccharomyces cerevisiae gene YNL234w encodes a 426-amino acid-long protein that shares significant similarities with the globin family. Compared with…”
Get full text
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