Search Results - "Bedini, Annalida"
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Selective melatonin MT2 receptor ligands relieve neuropathic pain through modulation of brainstem descending antinociceptive pathways
Published in Pain (Amsterdam) (01-02-2015)“…Neuropathic pain is an important public health problem for which only a few treatments are available. Preclinical studies show that melatonin (MLT), a…”
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Synthesis of Tryptamine Derivatives via a Direct, One-Pot Reductive Alkylation of Indoles
Published in Journal of organic chemistry (20-07-2012)“…An efficient, one-pot reductive alkylation of indoles with N-protected aminoethyl acetals in the presence of TES/TFA is reported. It represents the first…”
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Homology models of melatonin receptors: challenges and recent advances
Published in International Journal of Molecular Sciences (12-04-2013)“…Melatonin exerts many of its actions through the activation of two G protein-coupled receptors (GPCRs), named MT1 and MT2. So far, a number of different MT1…”
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Melatonin MT1 and MT2 Receptors Exhibit Distinct Effects in the Modulation of Body Temperature across the Light/Dark Cycle
Published in International journal of molecular sciences (17-05-2019)“…Melatonin (MLT) is a neurohormone that regulates many physiological functions including sleep, pain, thermoregulation, and circadian rhythms. MLT acts mainly…”
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Chiral Recognition of Flexible Melatonin Receptor Ligands Induced by Conformational Equilibria
Published in Molecules (Basel, Switzerland) (04-09-2020)“…-anilinoethylamides are a class of melatoninergic agents with the aniline portion mimicking the indole ring of the natural ligand and the ethylamide chain…”
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Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders
Published in Current topics in medicinal chemistry (01-07-2008)“…Melatonin (N-acetyl-5-methoxytryptamine) is synthesized and released by the pineal gland following a circadian rhythm characterized by high levels during the…”
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Synthesis and characterization of new bivalent agents as melatonin- and histamine H3-ligands
Published in International journal of molecular sciences (12-09-2014)“…Melatonin is an endogenous molecule involved in many pathophysiological processes. In addition to the control of circadian rhythms, its antioxidant and…”
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Analysis of Structure−Activity Relationships for MT2 Selective Antagonists by Melatonin MT1 and MT2 Receptor Models
Published in Journal of medicinal chemistry (16-06-2005)“…Three-dimensional homology models of human MT1 and MT2 melatonin receptors were built with the aim to investigate the structure−activity relationships (SARs)…”
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Indole-based analogs of melatonin: in vitro antioxidant and cytoprotective activities
Published in Journal of pineal research (01-03-2004)“…: The known neuroprotective actions of melatonin could be due to its antioxidant or radical scavenging activity, or they could be due to specific interactions…”
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Iridium-Catalyzed Direct Synthesis of Tryptamine Derivatives from Indoles: Exploiting N‑Protected β‑Amino Alcohols as Alkylating Agents
Published in Journal of organic chemistry (20-03-2015)“…The selective C3-alkylation of indoles with N-protected ethanolamines involving the “borrowing hydrogen” strategy is described. This method provides convenient…”
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Combined targeting of fatty acid amide hydrolase and melatonin receptors promotes neuroprotection and stimulates inflammation resolution in rats
Published in British journal of pharmacology (01-05-2023)“…Background and Purpose Devising novel strategies to therapeutically favour inflammation resolution and provide neuroprotection is an unmet clinical need…”
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MT2 selective melatonin receptor antagonists: design and structure-activity relationships
Published in ARKIVOC (19-04-2006)Get full text
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Dysfunction of serotonergic activity and emotional responses across the light‐dark cycle in mice lacking melatonin MT2 receptors
Published in Journal of pineal research (01-08-2020)“…Melatonin (MLT) levels fluctuate according to the external light/dark cycle in both diurnal and nocturnal mammals. We previously demonstrated that…”
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Industrial and academic approaches to the search for alternative melatonin receptor ligands: An historical survey
Published in Journal of pineal research (01-05-2024)“…The search for melatonin receptor agonists formed the main part of melatonin medicinal chemistry programs for the last three decades. In this short review, we…”
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Design, Synthesis, and Biological Activity of Hydrogen Peroxide Responsive Arylboronate Melatonin Hybrids
Published in Chemical research in toxicology (22-01-2019)“…Stimulus-responsive cleavage reactions have found broad use to direct drug release at a particular target disease area. Increased levels of reactive oxygen…”
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Therapeutic uses of melatonin and melatonin derivatives: a patent review (2012 - 2014)
Published in Expert opinion on therapeutic patents (01-04-2015)“…Melatonin is a neurohormone involved in the regulation of circadian rhythms, with potent antioxidant activity. It has a wide functional repertoire, with…”
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Binding and unbinding of potent melatonin receptor ligands: Mechanistic simulations and experimental evidence
Published in Journal of pineal research (01-03-2024)“…The labeled ligand commonly employed in competition binding studies for melatonin receptor ligands, 2‐[125I]iodomelatonin, showed slow dissociation with…”
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In silico drug discovery of melatonin receptor ligands with therapeutic potential
Published in Expert opinion on drug discovery (03-04-2022)“…The neurohormone melatonin ( -acetyl-5-methoxytryptamine) regulates circadian rhythms exerting a variety of effects in the central nervous system and in…”
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2-Arylmelatonin analogues: Probing the 2-phenyl binding pocket of melatonin MT1 and MT2 receptors
Published in European journal of medicinal chemistry (05-12-2022)“…In crystal structures of melatonin MT1 and MT2 receptors, a lipophilic subpocket has been characterized which accommodates the phenyl ring of the potent…”
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