about
Promotion of non-rapid eye movement sleep and activation of reticular thalamic neurons by a novel MT2 melatonin receptor ligandTherapeutic uses of melatonin and melatonin derivatives: a patent review (2012 - 2014).Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands.N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands.Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders.Recent advances in the development of melatonin MT(1) and MT(2) receptor agonists.Melatonin receptor agonists: new options for insomnia and depression treatment.Pharmacokinetic and pharmacodynamic evaluation of ramelteon : an insomnia therapy.Synthesis and characterization of new bivalent agents as melatonin- and histamine H3-ligands.Description of the constitutive activity of cloned human melatonin receptors hMT(1) and hMT(2) and discovery of inverse agonists.MT1-selective melatonin receptor ligands: synthesis, pharmacological evaluation, and molecular dynamics investigation of N-{[(3-O-substituted)anilino]alkyl}amides.Toward the definition of stereochemical requirements for MT2-selective antagonists and partial agonists by studying 4-phenyl-2-propionamidotetralin derivatives.Reassessing the melatonin pharmacophore--enantiomeric resolution, pharmacological activity, structure analysis, and molecular modeling of a constrained chiral melatonin analogue.Bivalent ligand approach on N-{2-[(3-methoxyphenyl)methylamino]ethyl}acetamide: synthesis, binding affinity and intrinsic activity for MT(1) and MT(2) melatonin receptors.Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists.2-N-acylaminoalkylindoles: design and quantitative structure-activity relationship studies leading to MT2-selective melatonin antagonists.2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.Synthesis and biological activity of new melatonin dimeric derivatives.Synthesis, pharmacological characterization and QSAR studies on 2-substituted indole melatonin receptor ligands.Synthesis of 2-substituted tryptophans via a C3- to C2-alkyl migration.A novel one-pot approach of hexahydropyrrolo[2,3-b]indole nucleus by a cascade addition/cyclization strategy: synthesis of (+/-)-esermethole.Diastereo- and enantioselective hydrogenation of a challenging enamide derived from 4-phenyl-2-tetralone: an appealing shortcut towards enantiopure cis-2-aminotetraline derivatives.N-(Anilinoethyl)amides: design and synthesis of metabolically stable, selective melatonin receptor ligands.Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.Conformation by NMR of two tetralin-based receptor ligands.Synthesis and structure-activity relationships of a series of pyrrole cannabinoid receptor agonists.Indole-based analogs of melatonin: in vitro antioxidant and cytoprotective activities.Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.Synthesis and conformational study of 3,4-carbocyclic bridged indole melatonin and serotonin analogues.An improved synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT): a selective MT(2) melatonin receptor antagonist.Synthesis, antioxidant activity and structure-activity relationships for a new series of 2-(N-acylaminoethyl)indoles with melatonin-like cytoprotective activity.1-Aminocylopropane-1-carboxylic acid derivatives as ligands at the glycine-binding site of the N-methyl-D-aspartate receptor.Melatonin, selective and non-selective MT1/MT2 receptors agonists: differential effects on the 24-h vigilance states.Anxiolytic effects of the melatonin MT(2) receptor partial agonist UCM765: comparison with melatonin and diazepam.3-(2-Carbamoylvinyl)-4,5-dimethylpyrrole-2-carboxylic acids as ligands at the NMDA glycine-binding site: a study on the 2-carbamoylvinyl chain modification.Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study.2-Bromomelatonin: synthesis and characterization of a potent melatonin agonist.1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues.Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study.
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P50
description
hulumtues
@sq
researcher
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wetenschapper
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հետազոտող
@hy
name
Gilberto Spadoni
@ast
Gilberto Spadoni
@en
Gilberto Spadoni
@es
Gilberto Spadoni
@nl
Gilberto Spadoni
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type
label
Gilberto Spadoni
@ast
Gilberto Spadoni
@en
Gilberto Spadoni
@es
Gilberto Spadoni
@nl
Gilberto Spadoni
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prefLabel
Gilberto Spadoni
@ast
Gilberto Spadoni
@en
Gilberto Spadoni
@es
Gilberto Spadoni
@nl
Gilberto Spadoni
@sl
P106
P1153
7004564996
P21
P31
P496
0000-0001-7253-6902