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Milligan et al demonstrated the
2022-02-15

Milligan et al. [31] demonstrated the important role of TNF-α, IL-6 and IL-1β in the development of mechanical hyperalgesia induced by intrathecal injection of gp120. Because of this work, we decide to produce and purify gp120 to develop biological systems to study pain and behavior in rodents. Intr
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To verify the feasibility of the proposed
2022-02-15

To verify the feasibility of the proposed method, EIS is firstly adopted to study the modification processes of the electrode. As shown in Fig. 1A, the nyquist plot of bare gold electrode exhibits a straight line, which indicates a fast charge transfer process (curve a). After modified with probe a,
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Azaperone In this study we present the synthesis and
2022-02-15

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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To ensure the induction of CYP enzymes
2022-02-15

To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme
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Reactivation of memory engram neurons
2022-02-15

Reactivation of memory engram neurons underlies memory retrieval. Neurons activated during memory formation are reactivated during the memory test 24, 25, 32. The reactivation is observed in the cerebral cortex as well as in the hippocampus and amygdala 33, 34. The ratio of the reactivation correlat
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Betahistine N methyl pyridyl ethylamine
2022-02-15

Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 aldehyde dehydrogenase inhibitor agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease
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Based on pharmacophore modeling a good HDAC
2022-02-15

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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In an effort to further improve the intrinsic
2022-02-15

In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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The frequency of GSTM and GSTT null
2022-02-15

The frequency of GSTM1 and GSTT1 null genotypes vary in different populations. For example, Hiragi et al. (2007) reported a frequency of 17–35% for the GSTM1 null genotype and 22–44% for the GSTT1 null genotype in Brazilians of African descent (Hiragi et al., 2007). Chen, Liu, and Relling (1996) rep
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One of the main clinical
2022-02-14

One of the main clinical issues of ABCB1, together with its impact on intestinal absorption, concerns its location at the BBB. Indeed, ABCB1 has been identified in the luminal side of endothelial cells and in the abluminal side of astrocyte endfeet processes of the CNS microvasculature [[36], [37],
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Our study has some limitations that should be considered whe
2022-02-14

Our study has some limitations that should be considered when the results are interpreted. First, we did not measure the protein levels of Bax and Bcl2, due to time and budget limitations. Although simultaneous measurements of both mRNA and protein levels are complementary for a better understanding
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br Acknowledgments br Introduction When human
2022-02-14

Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact nmda receptor suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltage-dependent catio
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br Results and discussion br Conclusions As
2022-02-14

Results and discussion Conclusions As described above, the SAR study based on compound 1 led to the identification of compound 4 as an ideal inhibitor. An enzyme level investigation showed that 4 is a more potent and selective FGFRs tyrosine kinase inhibitor than is Ponatinib. In addition, the
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Recent research has focused on
2022-02-14

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty Cy5.5 NHS ester receptor receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it contr
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The RAS RAF MEK ERK pathway also known as
2022-02-14

The RAS/RAF/MEK/ERK pathway (also known as the MAPK/ERK pathway) is one of the most important signaling pathways in PDAC. Activation of the MAPK/ERK pathway promotes PDAC growth and apoptosis resistance in response to gemcitabine [43,44]. We previously demonstrated that inhibition of GPX4 can overco
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