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We observed the reduced expression of the
2022-05-23
We observed the reduced expression of the GluN2a subunit in the temporal and entorhinal cortexes and ventral hippocampus, which may result in the predominance of GluN2b-containing NMDA receptors during the latent period. Previously, using the same model, we revealed the reduction of the GluN2a/GluN2
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Some other neuroinflammatory neuroendocrine and
2022-05-23
Some other neuroinflammatory, neuroendocrine, and neurotrophic pathway but not the ghrelin/GHSR pathway may mediate the CUMS-induced depression- and anxiety-like behaivors. The endogeous ghrelin/GHSR pathway activated by chronic mild stress may plays a role in homeostasis. With respect to the mechan
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In order to test the influence
2022-05-23
In order to test the influence of the initial depolarization, experiments were performed, where the degree of chloride substitution was varied, either by adding n-Ringer to Adaptaquin incubated in a sucrose Ringer or by suspending the cells directly in Ringers identical to the final composition in
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Experiments show that CSD propagation
2022-05-23
Experiments show that CSD propagation can be slowed or interrupted by pre-existing lesions or areas of high astrocytic density (Chen et al., 2006), and reduced expression of astrocytic gap junctions significantly increases the size of ischemic infarcts (Nakase et al., 2003). By decreasing the gap ju
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All data were analyzed using SAS software version SAS Instit
2022-05-23
All data were analyzed using SAS software (version 9.3, SAS Institute Inc., Cary, NC). Because of very low FFAR1 protein detection (at the detection limit or no signal) in 3 H-BHB cows, quantification was not possible within a linear range and therefore these animals were omitted from the statistica
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We next determined the selectivity profile of
2022-05-23
We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty imidazoline receptors receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affini
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Ligand selectivity may directly be related to
2022-05-23
Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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DAMPs are endogenous danger signals that can
2022-05-23
DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious ML133 HCl during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our current data indi
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In the current study we report
2022-05-23
In the current study, we report the properties of P. anserina mutants carrying mutations in a gene encoding the bi-functional enzyme 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (PFK-2/FBPase-2). This enzyme catalyzes two opposite reactions (Pilkis et al., 1995, Rider et al., 2004): synthesi
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br Conclusions In summary our results demonstrate that in sh
2022-05-23
Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical 3965 have a dual effect, and a decrease of the 5-HT2A express
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Unfortunately the approved drugs suffer from failure in
2022-05-23
Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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The diseases of ocular surface and
2022-05-21
The diseases of ocular surface and the cornea are very common in ophthalmological practice and as a result there is a continuous, need for novel therapeutic options. Here, we demonstrated a corneal distribution of GPR35, a potential molecular target for new drugs (; ). The search for the expression
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Recently a G protein coupled receptor
2022-05-21
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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Spatial working memory improved in the Balb c
2022-05-21
Spatial working memory improved in the Balb/c strain at a dose of VU0410120 (i.e., 30mg/kg) that disrupted spatial working memory in the Swiss Webster comparator strain. Consistent with a recent PET study in rhesus macaques suggesting a relationship between the extent of the dose-dependent occupancy
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In this study we present
2022-05-21
In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g
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