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To maintain low Glu concentrations in the synaptic cleft
2022-02-10

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino Phos-tag Acrylamide mg is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astroc
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The classical genomic effects of GR come about
2022-02-09

The classical genomic effects of GR come about through ligand-bound GR homodimerizing in the nucleus and via direct binding to GREs on the target genes, bringing about transcriptional activation or repression. Examples of target genes up-regulated by activated GR include genes encoding β2-adrenergic
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The mechanisms underlying the inhibitory effects of n
2022-02-09

The mechanisms underlying the inhibitory effects of n-3 FAs on neoplasia have not been completely elucidated. Until recently, the emphasis has been on the ability of n-3 FAs to compete for the pathways that lead to the synthesis of pro-inflammatory eicosanoids from arachidonic acid, an n-6 FA, there
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C prevents the glutamate and
2022-02-09

C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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Starting from the hypothesis that the linker
2022-02-09

Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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br Trifluoromethylketones This group of compounds was demons
2022-02-09

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Ivacaftor benzenesulfonate synthesis in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthi
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The combination of niacin with a selective
2022-02-09

The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su
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To facilitate the development of novel diagnostic and therap
2022-02-09

To facilitate the development of novel diagnostic and therapeutic interventions in NASH, a plethora of animal models have been used to identify molecular targets that are involved in the onset and progression of NASH. In view of recent advances in the understanding of the pathogenesis of NASH and pr
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br Computational details and modeling All calculations were
2022-02-09

Computational details and modeling All calculations were performed using the density functional B3LYP [34] method, implemented in Gaussian03 program [35]. The structures of reactants, transition states, intermediates, and products were optimized using the 6-31+G(d) basis set for the H, C, N, O an
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br Transporter based brain targeting nano DDS Drug delivery
2022-02-08

Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the liothyronine sodium from harmful substances. Since only selected, neutral, lipophilic
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br Discussion Our results indicate
2022-02-08

Discussion Our results indicate that marked changes in the relative distribution of AMPA receptors in microsomal and synaptic fractions occur during the postnatal period, and that these changes are correlated with changes in different populations of AMPA binding sites. At early postnatal ages (PN
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br Material and methods br Results br Discussion Accumulatin
2022-02-08

Material and methods Results Discussion Accumulating evidence suggests that the hippocampus is sensitive to noise-induced hearing loss and other forms of sensory deprivation, which deprives the hippocampus of sensory information required for its normal operations such as spatial navigation
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br Fipronil resistance associated with A S
2022-02-08

Fipronil resistance associated with A2′S and A2′G mutations Fipronil is a second-generation NCA (Fig. 1), and A2′S and A2′G mutations provide a low level of cross-resistance to fipronil (Cole et al., 1995, Gao et al., 2007). As shown in Table 1, the A2′S Acetaminophen confers high resistance to
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br Materials and methods br
2022-02-08

Materials and methods Chemical synthesis Declaration of interest Acknowledgements This research was supported by a grant from the National Institute for General Medicine to K.W.M. (GM 58448) and by the Department of Anesthesia, Critical Care & Pain Medicine at Massachusetts General Hospi
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In conclusion we have shown that the brain
2022-02-08

In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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