Dual target ligands with 4-tert-butylphenoxy scaffold as histamine H3 receptor antagonists and monoamine oxidase B inhibitors

Dual target ligands are a promising concept for the treatment of Parkinson’s disease (PD). A combination of monoamine oxidase B (MAO B) inhibition with histamine H3 receptor (H3R) antagonism could have positive effects on dopamine regulation. Thus, a series of twenty-seven 4-tert-butylphenoxyalkoxyamines were designed as potential dual-target ligands for PD based on the structure of 1-(3-(4-tert-butylphenoxy)propyl)piperidine (DL76). Probed modifications included the introduction of different cyclic amines and elongation of the alkyl chain. Synthesized compounds were investigated for human H3R (hH3R) affinity and human MAO B (hMAO B) inhibitory activity. Most compounds showed good hH3R affinities with Ki values below 400 nM, and some of them showed potent inhibitory activity for hMAO B with IC50 values below 50 nM. However, the most balanced activity against both biological targets showed DL76 (hH3R: Ki = 38 nM and hMAO B: IC50 = 48 nM). Thus, DL76 was chosen for further studies, revealing the nontoxic nature of DL76 in HEK293 and neuroblastoma SH-SY5Ycells. However, no neuroprotective effect was observed for DL76 in hydrogen peroxide-treated neuroblastoma SH-SY5Y cells. Furthermore, in vivo studies showed antiparkinsonian activity of DL76 in haloperidol-induced catalepsy (Cross Leg Position Test) at a dose of 50 mg/kg body weight

The significance of animals behavior in predicting earthquakes

Earthquake, the sudden ground shaking, is the natural disaster, responsible for substantial damages and loss of many human lives every year. Therefore, it is vital to develop effective earthquake early warning (EEW) system. There are at least several potential predictive signs – physical phenomena, which precede an earthquake (e.g. changes in electromagnetic field, gases emission, air ionization and many others) On the basis of historical records and contemporary observations, some scientists suggest that animals behaviour which presumably changes shortly before the earthquake, could be also treated as a part of warning system. However, there is some scepticism in the Western civilization concerning this issue. This paper is an attempt to discuss the problem with presentation of physical stimuli role in earthquake heralding and animals capacity to respond to them. This discussion is based on analysis of scientific research and also on anecdotal observations. As a conclusion it seems that looking forward for guarded but not unfavourable approach to this issue is needed

The effect of roads and railways infrastructure on the wildlife

Transport, roads and railways have a wide variety of ecological effects on the natural environment and wildlife. The most important direct impact is massive death toll, particularly road killing of animals as a result of collisions. Habitat fragmentation due to the roads and railways building is also significant with its far-off results (edge effect, decrease of habitat size, genetic diversity, etc). Moreover, the railway is barrier that impedes the migration of hoofed mammals. The construction of culverts and tunnels is probably the best method for species protection, particularly in the case of mammals. Some animal species however, as bats or amphibians, are more susceptible to the obstacles caused by the transportation infrastructure, thus they become seriously endangered. Then the effects of pollution of the area surrounding roads, like noise, unnecessary light, chemicals which is the separate and increasing drawback not extensively discussed in this paper. The methods of mitigation problems caused by roads/railways infrastructure do not seem to be satisfactory

Behaviorism and behvior: philosophy and behavioral methods

Behawior i behawioryzm to pojęcia często używane zamiennie, co jest błędem. Celem niniejszego artykułu jest szczegółowe wyjaśnienie obydwu pojęć oraz wskazanie związku między nimi. Zarówno pojęcie "behawior", jak i "behawioryzm" odnoszą się do zachowania. Behawior jest złożonym systemem zachowań zwierzęcia w odpowiedzi na sygnały docierające ze środowiska zewnętrznego lub z wnętrza organizmu, zaś behawioryzm odnosi się do bardzo silnie rozwiniętego kierunku w psychologii, opierającego się na przyczynowo- skutkowej obserwacji zachowania ograniczającej się do eksperymentalnej i obiektywnie mierzalnej analizy. Wyróżniamy behawioryzm metodologiczny (Watsona) oraz radykalny (Skinnera), a także behawioryzm filozoficzny, określany także mianem logicznego. Nauka zajmująca się behawiorem to etologia. Opisuje ona różne formy zachowań, zarówno tych wrodzonych jak i nabytych, poprzez obserwację przede wszystkim w warunkach naturalnych, ale i eksperymentalnych. Behawior możemy podzielić na: stereotypowy (wrodzony), instynktowy (motywowany) oraz nabyty.Behavior and behaviorism are concepts often used interchangeably, which is wrong. The aim of this article is a detailed explanation of both concepts and relationship between them. Both terms "behavior" and "behaviorism" refer to the behavior. However, the first means a system of complex behavior of an animal in the response to signals from external environment or from the body interior. While the other one refers to the very strongly developed branch of psychology based on cause-and- effect behavioral observations limited to the experimental and objectively measurable analysis. There are distinguished methodological behaviorism (Watson), radical behaviorism (Skinner), and philosophical behaviorism, also called logical. Science concerned with the behavior, named ethology, describes various forms of inborn and acquired behavior observed primarily in nature, and also in an experimental space

Individual differences in police dog handlers

The Polish adaptation of the NEO-FFI inventory (see Costa & McCrea, 1989; 1992b; Zawadzki et al. 2007) was used in the present study to assess the personality of dog handlers. For diagnosis of the emotional intelligence, the Polish scale Popular Questionnaire of Emotional Intelligence was used (Jaworowska & Matczak, 2005). There were 601 participants out of the total estimated number of 1408 police dog handlers in Poland. The results were compared with normalization tests for the measures used. The personality profile and emotional intelligence of dog handlers differ significantly from general population. Described in the NEO-FFI terms, police dog handlers are characterized by very low neuroticism, slightly above average extraversion, slightly below average openness to experience, a little above average agreeableness, and very high conscientiousness. In terms of emotional intelligence, they demonstrate higher control and understanding of emotions. It seems that the results obtained in the study may become relevant for the recruitment and training of police officers

Structural Quality and Magnetotransport Properties of Epitaxial Layers of the (Ga,Mn)(Bi,As) Dilute Magnetic Semiconductor

Structural analysis of epitaxial layers of the (Ga,Mn)(Bi,As) quaternary dilute magnetic semiconductor (DMS), together with investigations of their magnetotransport properties, has been thoroughly performed. The obtained results are compared with those for the reference (Ga,Mn)As layers, grown under similar conditions, with the aim to reveal an impact of Bi incorporation on the properties of this DMS material. Incorporation of Bi into GaAs strongly enhances the spin-orbit coupling strength in this semiconductor, and the same has been expected for the (Ga,Mn)(Bi,As) alloy. In turn, importantly for specific spintronic applications, strong spin-orbit coupling in ferromagnetic systems opens a possibility of directly controlling the direction of magnetization by the electric current. Our investigations, performed with high-resolution X-ray diffractometry and transmission electron microscopy, demonstrate that the (Ga,Mn)(Bi,As) layers of high structural quality and smooth interfaces can be grown by means of the low-temperature molecular-beam epitaxy method, despite a large difference between the sizes of Bi and As atoms. Depending on the applied buffer layer, the DMS layers can be grown under either compressive or tensile misfit strain, which influences their magnetic properties. It is shown that even small 1% Bi content in the layers strongly affects their magnetoelectric properties, such as the coercive field and anisotropic magnetoresistance

Stress hormone level and the welfare of captive European bison (Bison bonasus): the effects of visitor pressure and the social structure of herds

Abstract Background Captive European bison (Bison bonasus) play an active role in conservation measures for this species; this includes education, which may conflict with these animals’ welfare. The effect of the presence of visitors on the welfare of captive animals can be negative, positive or neutral. However, the response of a given species to visitors is difficult to predict, since even closely related species display varying levels of tolerance to captivity. The aim of the study was to compare immunoreactive fecal cortisol levels (regarded as an indicator of the level of physiological stress) in groups of captive European bison that differed in terms of their social structure and the level of visitor pressure. The second aim was to determine if there was a correlation between intestinal parasitic burden and immunoreactive fecal cortisol levels. Results Immunoreactive fecal cortisol levels were not influenced by sex or age. However, study site and the interaction between study site and visitor pressure were statistically significant. European bison in one enclosure presented higher levels of immunoreactive fecal cortisol on weekdays than at weekends. In the other two study sites, the levels did not differ between weekdays and weekends. No correlation was found between parasitological infestation and immunoreactive fecal cortisol levels. Conclusions Measurement of fecal cortisol metabolites could be a valuable method for further research into the welfare of European bison in captivity. More subtle factors such as individual animal characteristics, feeding systems, and the arrangement of enclosures can be of great importance in terms of the effect of visitors on animals. The results of this study can be used in guidelines for the management of European bison populations