Search Results - "Rios, Cristobal de los"
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Ischemic brain injury: New insights on the protective role of melatonin
Published in Free radical biology & medicine (01-03-2017)“…Stroke represents one of the most common causes of brain's vulnerability for many millions of people worldwide. The plethora of physiopathological events…”
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(±)-BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3β Inhibition with Calcium Channel Antagonism and Antiaggregating Properties for Alzheimer’s Disease
Published in ACS chemical neuroscience (21-04-2021)“…Multitarget-directed ligands (MTDLs) are considered a promising therapeutic strategy to address the multifactorial nature of Alzheimer’s disease (AD). Novel…”
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Novel Purine Derivative ITH15004 Facilitates Exocytosis through a Mitochondrial Calcium-Mediated Mechanism
Published in International journal of molecular sciences (01-01-2022)“…Upon depolarization of chromaffin cells (CCs), a prompt release of catecholamines occurs. This event is triggered by a subplasmalemmal high-Ca microdomain…”
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Evaluation of the neuroprotective efficacy of the gramine derivative ITH12657 against NMDA-induced excitotoxicity in the rat retina
Published in Frontiers in neuroanatomy (13-02-2024)“…The aim of this study was to investigate, the neuroprotective effects of a new Gramine derivative named: ITH12657, in a model of retinal excitotoxicity induced…”
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Identification of tetracyclic lactams as NMDA receptor antagonists with potential application in neurological disorders
Published in European journal of medicinal chemistry (15-05-2020)“…N-Methyl-d-aspartate receptors (NMDARs) are crucial for the normal function of the central nervous system (CNS), and fundamental in memory and learning-related…”
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The Neuroprotector Benzothiazepine CGP37157 Extends Lifespan in C. elegans Worms
Published in Frontiers in aging neuroscience (17-01-2019)“…The benzothiazepine CGP37157 has shown neuroprotective effects in several models of excitotoxicity involving dysregulation of intracellular Ca homeostasis…”
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New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties
Published in Bioorganic & medicinal chemistry (15-08-2008)“…In this communication, we describe the synthesis and biological evaluation of tacripyrimedones 1– 5, a series of new tacrine-1,4-dihydropyridine hybrids…”
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Synthesis, Pharmacological Assessment, and Molecular Modeling of Acetylcholinesterase/Butyrylcholinesterase Inhibitors: Effect against Amyloid-β-Induced Neurotoxicity
Published in ACS chemical neuroscience (17-04-2013)“…The synthesis, molecular modeling, and pharmacological analysis of phenoxyalkylamino-4-phenylnicotinates (2–7), phenoxyalkoxybenzylidenemalononitriles (12,…”
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Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[ b][1,8]naphthyridine-3-carboxylate
Published in Bioorganic & medicinal chemistry letters (01-05-2010)“…In silico analysis of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[ b][1,8]naphthyridine-3-carboxylate ( 2) predicts that this molecule should be…”
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New multipotent tetracyclic tacrines with neuroprotective activity
Published in Bioorganic & medicinal chemistry (15-12-2006)“…The synthesis and the biological evaluation (neuroprotection, voltage dependent calcium channel blockade, AChE/BuChE inhibitory activity and propidium binding)…”
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Dual Role of the P2X7 Receptor in Dendritic Outgrowth during Physiological and Pathological Brain Development
Published in The Journal of neuroscience (15-02-2023)“…At high levels, extracellular ATP operates as a "danger" molecule under pathologic conditions through purinergic receptors, including the ionotropic P2X7…”
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New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H 3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition
Published in Journal of medicinal chemistry (26-12-2019)“…New tritarget small molecules combining Ca channels blockade, cholinesterase, and H3 receptor inhibition were obtained by multicomponent synthesis. Compound…”
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Study of the single or combined action of three different neuroprotection strategies in an acute hypertension model in mice
Published in Acta ophthalmologica (Oxford, England) (01-01-2024)“…Aims/Purpose: To study the neuroprotective effects of a TrkB receptor activator (DHF), a calcium channel blocker that prevents Ca2+ toxic influx (ITH12657)…”
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Synthesis, biological evaluation and molecular modelling of diversely functionalized heterocyclic derivatives as inhibitors of acetylcholinesterase/butyrylcholinesterase and modulators of Ca2+ channels and nicotinic receptors
Published in Bioorganic & medicinal chemistry (01-05-2004)“…The synthesis and the biological activity of compounds 5-40 as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as…”
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P2X7R and TNFR1 antagonism neuroprotects rodent retinal ganglion cells in a sepsis model
Published in Acta ophthalmologica (Oxford, England) (01-12-2022)“…Purpose: i/ To analyse the time course of retinal ganglion cell death (RGCs) after systemic injection of LPS in mice. ii/ To analyse the neuroprotective effect…”
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Tetrabenazine Facilitates Exocytosis by Enhancing Calcium-Induced Calcium Release through Ryanodine Receptors
Published in The Journal of pharmacology and experimental therapeutics (01-10-2019)“…Vesicular monoamine transporter-2 is expressed in the presynaptic secretory vesicles membrane in the brain. Its blockade by tetrabenazine (TBZ) causes…”
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Therapeutic concentrations of varenicline increases exocytotic release of catecholamines from human and rat adrenal chromaffin cells in the presence of nicotine
Published in Neuropharmacology (01-09-2021)“…Cardiovascular side effects of varenicline and a case report of a hypertensive crisis in a varenicline-prescribed patient with pheochromocytoma have been…”
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Cholinergic and neuroprotective drugs for the treatment of Alzheimer and neuronal vascular diseases. II. Synthesis, biological assessment, and molecular modelling of new tacrine analogues from highly substituted 2-aminopyridine-3-carbonitriles
Published in Bioorganic & medicinal chemistry (01-01-2011)“…The structures of tacrine, the 2-aminopyridine-3,5-dicarbonitrile precursors, and the new tacrine analogues. The synthesis, biological assessment, and…”
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Synthesis, Biological Evaluation, and Molecular Modeling of Donepezil and N-[(5-(Benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine Hybrids as New Multipotent Cholinesterase/Monoamine Oxidase Inhibitors for the Treatment of Alzheimer’s Disease
Published in Journal of medicinal chemistry (22-12-2011)“…A new family of multitarget molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase…”
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1,8-Naphthyridine derivatives as cholinesterases inhibitors and cell Ca2+ regulators, a multitarget strategy for Alzheimer's disease
Published in Current topics in medicinal chemistry (01-11-2011)“…The synthesis and the pharmacological evaluation of 1,8-naphthyridine derivatives and related compounds as inhibitors of acetylcholinesterase (AChE) and…”
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