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31.
Biotransformation of 4‐fluoro‐N‐(1‐{2‐[(propan‐2‐yl)phenoxy]ethyl}‐8‐azabicyclo[3.2.1]octan‐3‐yl)‐benzenesulfonamide,a novel potent 5‐HT7 receptor antagonist with antidepressant‐like and anxiolytic properties: In vitro and in silico approach 下载免费PDF全文
Karolina Słoczyńska Katarzyna Wójcik‐Pszczoła Vittorio Canale Paweł Żmudzki Paweł Zajdel Elżbieta Pękala 《Journal of biochemical and molecular toxicology》2018,32(5)
The aim of the study was to investigate the metabolism of 4‐fluoro‐N‐(1‐{2‐[(propan‐2‐yl)phenoxy]ethyl}‐8‐azabicyclo[3.2.1]octan‐3‐yl)‐benzenesulfonamide (PZ‐1150), a novel 5‐HT7 receptor antagonist with antidepressant‐like and anxiolytic properties, by the following three ways: in vitro with microsomes; in vitro employing Cunninghamella echinulata, and in silico using MetaSite. Biotransformation of PZ‐1150 with microsomes resulted in five metabolites, while transformation with C. echinulata afforded two metabolites. In both models, the predominant metabolite occurred due to hydroxylation of benzene ring. In silico data coincide with in vitro experiments, as three MetaSite metabolites matched compounds identified in microsomal samples. In human liver microsomes PZ‐1150 exhibited in vitro half‐life of 64 min, with microsomal intrinsic clearance of 54.1 μL/min/mg and intrinsic clearance of 48.7 mL/min/kg. Therefore, PZ‐1150 is predicted to be a high‐clearance agent. The study demonstrated the applicability of using microsomal model coupled with microbial model to elucidate the metabolic pathways of compounds and comparison with in silico metabolite predictions. 相似文献
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Habitat fragmentation has often been implicated in the decline of many species. For habitat specialists and/or sedentary species, loss of habitat can result in population isolation and lead to negative genetic effects. However, factors other than fragmentation can often be important and also need to be considered when assessing the genetic structure of a species. We genotyped individuals from 13 populations of the cooperatively breeding Brown‐headed Nuthatch Sitta pusilla in Florida to test three alternative hypotheses regarding the effects that habitat fragmentation might have on genetic structure. A map of potential habitat developed from recent satellite imagery suggested that Brown‐headed Nuthatch populations in southern Florida occupied smaller and more isolated habitat patches (i.e. were more fragmented) than populations in northern Florida. We also genotyped individuals from a small, isolated Brown‐headed Nuthatch population on Grand Bahama Island. We found that populations associated with more fragmented habitat in southern Florida had lower allelic richness than populations in northern Florida (P = 0.02), although there were no differences in heterozygosity. Although pairwise estimates of FST were low overall, values among southern populations were generally higher than northern populations. Population assignment tests identified K = 3 clusters corresponding to a northern cluster, a southern cluster and a unique population in southeast Florida; using sampling localities as prior information revealed K = 7 clusters, with greater structure only among southern Florida populations. The Bahamas population showed moderate to high differentiation compared with Florida populations. Overall, our results suggest that fragmentation could affect gene flow in Brown‐headed Nuthatch populations and is likely to become more pronounced over time. 相似文献
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Everton Tizo‐Pedroso Kleber Del‐Claro 《Ethology : formerly Zeitschrift fur Tierpsychologie》2011,117(6):498-507
Division of labor is a strategy that maximizes the foraging and reproductive success of eusocial insects. Although some arachnids exhibit colony structure and social organization similar to that of hymenopterans, temporal polyethism has only been demonstrated in few species. The social organization of cooperative pseudoscorpions Paratemnoides nidificator is similar to that of social spiders, but it involves a clear division of labor. Work allocation was experimentally investigated in colonies composed of only one developmental stage (young or adults) or by one sex (males or females), through laboratory manipulation. During 44 h of observation, more than 14 000 behavioral repetitions were quantified, distributed in 95 different types of behavioral acts, and grouped in 10 behavioral categories. The results showed that reproductive colonies of P. nidificator are maintained by gender‐ and age‐based activities. Males and non‐reproductive females performed the external cleaning of the colony and prey capture. Reproductive females take care of the juveniles and build reproductive silk chambers. Nymphs build most of the molt chambers and perform internal cleaning. In the absence of nymphs, male colonies survived 1–2 mo, while female colonies survived 3–4 mo. In nymph colonies, work is readjusted so that all maintenance tasks are executed. This is the first study clearly demonstrating division of tasks in arachnids. It suggests that specialization is an adaptative and evolutionarily old trait in this species. Unlike cooperative spiders, P. nidificator possesses physiological (e.g. reproduction, ecdysis, lifespan) and behavioral (e.g. behavioral synchrony or self‐organization) characteristics that allow task specialization. 相似文献
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F. Teixeira‐de Mello I. Gonzalez‐Bergonzoni F. Viana C. Saizar 《Zeitschrift fur angewandte Ichthyologie》2011,27(6):1413-1415
This study provides data on the length–weight relationship (LWR) for 26 species of neotropical fishes. Specimens were collected between 2008 and 2009 from a dam‐enclosed section of the middle Negro River (Uruguay). This study represents the first reference on length–weight relationships for 17 species, and also provides new maximum sizes for eight species. 相似文献
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Rafael Ruiz‐de‐Castañeda Ana Isabel Vela Elisa Lobato Víctor Briones Juan Moreno 《Journal of Field Ornithology》2011,82(2):215-224
ABSTRACT Bacteria grow on avian eggshells and thus can potentially cause diseases in developing embryos. Little is known about culturable bacteria colonizing avian eggshells in free‐living birds, with most studies restricted to poultry. Our objective was to examine the culturable bacterial array growing on eggshells during incubation that could negatively affect hatching success of Pied Flycatchers (Ficedula hypoleuca) in a temperate montane habitat in central Spain. Cloacal culturable bacteria of females were also analyzed because bacteria can be vertically transmitted from females to eggs. We used fecal samples as surrogates of cloacal samples due to the small size of sampled birds. We found that eggshells and female cloacae of Pied Flycatchers harbored 24 and 40 bacterial families and species, respectively, but only a few in each clutch and each cloaca. Rod‐shaped gram‐negative bacteria and bacteria in the family Pseudomonadaceae were the most common bacteria on eggshells during early and late incubation and in female cloacae. Although based on small sample sizes, we found that females with rod‐shaped gram‐negative bacteria in their cloacae laid eggs that also had these bacteria, providing possible evidence for vertical transmission. We found no evidence for vertical transmission of Pseudomonadaceae, suggesting a possible environmental source for these bacteria. The prevalence of bacterial morphological types and major taxonomical categories on eggshells did not vary from early to late stages of incubation, providing support for the hypothesis that incubation may have bacteriostatic effects on bacterial proliferation on eggshells. Despite being primary egg invaders in poultry, we detected no effects of culturable Pseudomonadaceae or Pseudomonas luteola on hatching success. Our study represents the first to examine the culturable bacteria growing on the eggshells of a wild bird in a temperate habitat and additional studies based on culture‐independent techniques are required to confirm our results. 相似文献
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