Fluoxetine: a case history of its discovery and preclinical development

Introduction: Depression is a multifactorial mood disorder with a high prevalence worldwide. Until now, treatments for depression have focused on the inhibition of monoaminergic reuptake sites, which augment the bioavailability of monoamines in the CNS. Advances in drug discovery have widened the therapeutic options with the synthesis of so-called selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine. Areas covered: The aim of this case history is to describe and discuss the pharmacokinetic and pharmacodynamic profiles of fluoxetine, including its acute effects and the adaptive changes induced after long-term treatment. Furthermore, the authors review the effect of fluoxetine on neuroplasticity and adult neurogenesis. In addition, the article summarises the preclinical behavioural data available on fluoxetine’s effects on depressive-like behaviour, anxiety and cognition as well as its effects on other diseases. Finally, the article describes the seminal studies validating the antidepressant effects of fluoxetine. Expert opinion: Fluoxetine is the first selective SSRI that has a recognised clinical efficacy and safety profile. Since its discovery, other molecules that mimic its mechanism of action have been developed, commencing a new age in the treatment of depression. Fluoxetine has also demonstrated utility in the treatment of other disorders for which its prescription has now been approved

Soil and leaf mineral element contents in mediterranean vineyards: bioaccumulation and potential soil pollution

The study reported here concerns the geochemical distributions of macro- and trace elements (including potentially toxic elements, PTEs) in the vineyard soils of Alcubillas, which is one of the oldest, albeit not world-renowned, wine-growing areas in La Mancha (Central Spain). Soil and leaf samples were analyzed by X-ray fluorescence spectrometry to ascertain the levels of various elements in the soil and the plant. The potential toxicity of the elements was assessed with regard to the development of the vineyard. Despite the fact that fertilizers and pesticides are employed in the vineyards in this area, the results showed that the levels of trace elements in the soil samples did not exceed the reference values according the pedogeochemical values for the region and Spain. This finding suggests that the study area is not polluted, and therefore, there are hardly any traces of anthropogenic contamination. The Biological Absorption Coefficient (BAC) was calculated to assess the assimilation of various elements from the soil to the leaves, and differences were found in the element absorption capacity of the vines. Some elements were not taken up by Vitis vinifera despite elements like Zr and Rb being present in relatively high concentrations in the soil. The production in these soils does not represent a threat to human health or the ecosystem, because the farmers in this area are extremely careful to preserve the environment and they only farm to achieve moderate yields of grapes per hectar

Cambios de cobertura/uso del suelo en una porción de la Zona de Transición Mexicana de Montaña

La Porción Surponiente del Estado de México (PSEM) se ubica en la Zona de Transición Mexicana de Montaña. Las comunidades forestales que predominan en este territorio son bosques de pino (Pinus spp.), encino (Quercus spp.), mixtos (Pinus spp. - Quercus spp. y Quercus spp. - Pinus spp.), mesófilo de montaña y tropical caducifolio, los cuales están siendo modificados por la influencia de procesos antropogénicos. Este estudio presenta el análisis de los cambios de cobertura y uso del suelo ocurridos entre 1989 y 2009 en la PSEM, a través de la interpretación de imágenes de satélite (Landsat TM), que en complemento con la aplicación del algoritmo máxima verosimilitud permitieron la construcción de mapas temáticos de uso de suelo y vegetación, los cuales fueron evaluados para conocer su confiabilidad temática. A partir de la sobreposición de estos mapas se elaboró una matriz de cambios que comprende la superficie de las coberturas y usos del suelo para cada año y con base en esta se determinaron las tasas de cambio. Los resultados obtenidos demuestran que la cobertura del bosque disminuyó considerablemente, es decir, se eliminaron 19 262 ha, las cuales fueron ocupadas por las categorías cuerpos de agua (105 ha), agropecuario (19 113 ha), asentamientos humanos (39 ha) y agricultura tecnificada controlada (5 ha). La superficie deforestada es resultado del establecimiento y la práctica de actividades relacionadas con la agricultura y ganadería

FPGA Implementation for Real-Time Background Subtraction Based on Horprasert Model

Background subtraction is considered the first processing stage in video surveillance systems, and consists of determining objects in movement in a scene captured by a static camera. It is an intensive task with a high computational cost. This work proposes an embedded novel architecture on FPGA which is able to extract the background on resource-limited environments and offers low degradation (produced because of the hardware-friendly model modification). In addition, the original model is extended in order to detect shadows and improve the quality of the segmentation of the moving objects. We have analyzed the resource consumption and performance in Spartan3 Xilinx FPGAs and compared to others works available on the literature, showing that the current architecture is a good trade-off in terms of accuracy, performance and resources utilization. With less than a 65% of the resources utilization of a XC3SD3400 Spartan-3A low-cost family FPGA, the system achieves a frequency of 66.5 MHz reaching 32.8 fps with resolution 1,024 × 1,024 pixels, and an estimated power consumption of 5.76 W

A morphological approach to evaluating the nature of vineyard soils in semiarid Mediterranean environment

La Mancha (Central Spain) is one of the most extensive vineyard regions in the world, and ‘Valdepeñas’ is a representative Protected Denomination of Origin (PDO) in this region. However, what are their main soil types? what kind of horizons are the most common? and what is the role of the geomorphological positions in their pedodiversity? After describing and sampling 90 soil profiles in this area, Alfisols, Inceptisols and Entisols were mainly identified in Soil Taxonomy terms; in other words, Luvisols, Cambisols, Regosols, Leptosols and a highly significant proportion of Calcisols according to FAO-UNESCO-ISSS. The accumulation of carbonate, the thickness of which varies from a diffuse or powdery form to crusted forms, appear sometimes like polycyclic. The presence of red soils, with or without a calcic or petrocalcic horizon, indicates the most representative edaphic stages in this region. Consequently, the morphological signature is calcic or petrocalcic, followed by argillic and/or cambic horizons, under ochric horizons. It can be concluded that the nature of soils in Valdepeñas can be considered a differential factor to bear in mind for quality viticultural production. Highlights: There are unknown conceptual zones in support production of wine. A comprehensive study in a local case was performed due to its traditional production of vineyards. This study highlights the importance and uniqueness of the calcic and petrocalcic horizons. A disconnect exists between some tradicional viticultural zones with low reputation and the real value of their soil

The 72-Hour WEBT Microvariability Observation of Blazar S5 0716+714 in 2009

Context. The international whole earth blazar telescope (WEBT) consortium planned and carried out three days of intensive micro-variability observations of S5 0716+714 from February 22, 2009 to February 25, 2009. This object was chosen due to its bright apparent magnitude range, its high declination, and its very large duty cycle for micro-variations. Aims. We report here on the long continuous optical micro-variability light curve of 0716+714 obtained during the multi-site observing campaign during which the Blazar showed almost constant variability over a 0.5 magnitude range. The resulting light curve is presented here for the first time. Observations from participating observatories were corrected for instrumental differences and combined to construct the overall smoothed light curve. Methods. Thirty-six observatories in sixteen countries participated in this continuous monitoring program and twenty of them submitted data for compilation into a continuous light curve. The light curve was analyzed using several techniques including Fourier transform, Wavelet and noise analysis techniques. Those results led us to model the light curve by attributing the variations to a series of synchrotron pulses. Results. We have interpreted the observed microvariations in this extended light curve in terms of a new model consisting of individual stochastic pulses due to cells in a turbulent jet which are energized by a passing shock and cool by means of synchrotron emission. We obtained an excellent fit to the 72-hour light curve with the synchrotron pulse model

Novel rhodium on carbon catalysts for the oxidation of benzyl alcohol to benzaldehyde: A study of the modification of metal/support interactions by acid pre-treatments

Rhodium nanoparticles or rhodium organometallic complexes are mainly used in catalysis for reduction or hydroformylation reactions. In this work instead, we explored the capabilities of Rh nanoparticles as an oxidation catalyst, applied to the oxidation of benzyl alcohol to benzaldehyde under very mild conditions (100 °C, and atmospheric pressure) as a model reaction. Here we report the preparation of novel Rh/C catalysts by using an impregnation protocol, with particular emphasis on the pre-treatment of the carbon supports by using HNO3 and HCl, as well as the characterization of these materials by using an array of methods involving TEM, XPS and XRPD. Our preparation method led to a wide Rh particle size distribution ranging from 20 to 100 nm, and we estimate an upper limit diameter of Rh nanoparticles for their activity towards benzyl alcohol oxidation to be ca. 30 nm. Furthermore, a HNO3 pre-treatment of the activated carbon support was able to induce a smaller and narrower particle size distribution of Rh nanoparticles, whereas a HCl pre-treatment had no effect or sintered the Rh nanoparticles. We rationalise these results by HNO3 as an acid able to create new nucleation sites for Rh on the carbon surface, with the final effect of smaller nanoparticles, whereas for HCl the effect of sintering was most likely due to site blocking of the nucleation sites over the carbon surface. The roles of acid centres on the carbon surfaces for the oxidation reaction was also investigated, and the larger their amounts the larger the amounts of by-products. However, by treatment with HNO3 we were able to convert neutral or basic carbons into supports capable to enhance the catalytic activity of Rh, and yet minimised detrimental effects on the selectivity of the oxidation to benzaldehyde