Search results for " melatonin"

Synthesis and Characterization of New Bivalent Agents as Melatonin- and Histamine H3-Ligands

2014

Melatonin is an endogenous molecule involved in many pathophysiological processes. In addition to the control of circadian rhythms, its antioxidant and neuroprotective properties have been widely described. Thus far, different bivalent compounds composed by a melatonin molecule linked to another neuroprotective agent were synthesized and tested for their ability to block neurodegenerative processes in vitro and in vivo. To identify a novel class of potential neuroprotective compounds, we prepared a series of bivalent ligands, in which a prototypic melatonergic ligand is connected to an imidazole-based H3 receptor antagonist through a flexible linker. Four imidazolyl-alkyloxy-anilinoethylami…

Efficient synthesis of hexahydroindenopyridines and their potential as melatoninergic ligands.

2014

Hexahydroindenopyridine (HHIP) is an interesting tricyclic piperidine nucleus that is structurally related to melatonin, a serotonin-derived neurohormone. Melatonin receptor ligands have applications in several cellular, neuroendocrine and neurophysiological disorders, including depression and/or insomnia. We report herein an efficient two-step method to prepare new HHIP via enamine C-alkylation-cyclization. The influence of substituents on the benzene ring and the nitrogen atom on melatoninergic receptors has been studied. Among the 25 synthesized HHIPs, some of them containing methylenedioxy (series 2) and 8-chloro-7-methoxy substituents (series 4) on the benzene ring revealed affinity fo…

Effects of daylight and artificial light on melatonin suppression in educational environment.

2012

An analysis of the characteristics of daylight in a scholastic environment was carried out by comparing SPDs and CCTs of the natural source (sky) during typical winter days with contemporaneous measurements of spectral irradiances and CCTs detected at the eyes level. Data obtained from these measurements together with those detected with artificial light, were used to evaluate the effects on melatonin suppression during the day according to the procedure proposed by Rea et al [2]. Despite illuminances on desks under natural and artificial light corresponded to the EN 12464-1 Standard requirements, the irradiances detected at eye's level, which are essential for melatonin suppression, do not…

Localization and interactions of melatonin in dry cholesterol/lecithin mixed reversed micelles used as cell membrane models

2005

The state of melatonin confined in dry cholesterol/lecithin mixed reversed micelles dispersed in CCl4 was investigated using 1H-NMR and FT-IR spectroscopies as a function of the melatonin to lecithin molar ratio (R(MLT)) and of the cholesterol to lecithin molar ratio (R(CHL)). An analysis of experimental results leads to the hypothesis that, independent of R(MLT) and as a consequence of anisotropic melatonin/lecithin, melatonin/cholesterol and cholesterol/lecithin interactions, melatonin is totally solubilized in reversed micelles. Melatonin is mainly located in and oriented in the nanodomain constituted by the hydrophilic groups of cholesterol and lecithin. A competition of melatonin and c…

Orientation and molecular contacts of melatonin confined into AOT and lecithin reversed micellar systems

2008

Abstract The state of increasing amounts of melatonin (MLT) confined in dry AOT or lecithin reversed micelles dispersed in CCl 4 has been investigated by UV–vis and 1 H NMR spectroscopies. The experimental results are consistent with MLT totally entrapped in reversed micelles, as a consequence of specific melatonin/surfactant interaction; the main driving force of the MLT solubilization in the core of reversed micelles is the establishment of H-bonding between the MLT NH groups (both indolic and amidic) and the head group of surfactants. The short contacts deduced from intermolecular NOEs are accounted for by favourable interactions between the surfactant's polar head and the H7–NH–H2 fragm…

Il trattamento dell’insonnia in eta’ evolutiva: report clinico e revisione della letteratura

2014

Síntesis de Protoberberinas y Ciclopentil-isoquinoleínas Dopaminérgicas, y Síntesis de Indenopiridinas Melatoninérgicas

2015

Resumen – Discusión de los resultados. En la presente Tesis Doctoral se han desarrollado diversas rutas de síntesis para la obtención de alcaloides isoquinoleínicos, con diferentes esqueletos, y de hexahidroindenopiridinas. Además se han realizado sus correspondientes ensayos farmacológicos, sobre distintas dianas biológicas basándonos en los resultados obtenidos previamente con este tipo de alcaloides de síntesis y/o aislados de la naturaleza, y de moléculas estructuralmente similares. Se ha observado, a lo largo de muchos años, que las IQ son uno de los metabolitos secundarios activos (MSA) más abundantes y de mayor interés farmacológico de los aislados en especies de la familia de las An…