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br Acknowledgment br Introduction Positive and
2021-10-20
Acknowledgment Introduction Positive and negative reinforcement are known as the two pivotal components in various models of drug dependence. Compulsive drug seeking behavior results from both the euphoric effects of drug use (positive reinforcement) and the unpleasant withdrawal signs followi
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KU-57788 Tight junctions regulate the transfer of ions as we
2021-10-20
Tight junctions regulate the transfer of ions as well as small molecules across endothelial barriers (Li et al., 2015). We also investigated whether resistin affects tight junctions, which play an important role in the conformation of polarized endothelial barriers (Matsuzaki et al., 2010). A previo
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Numerical models of blood regulation
2021-10-19
Numerical models of blood regulation provide insight into the interaction of the cellular-level and macro-scale phenomena studied in silico, a term referring to computer simulations of the dynamics of complex biological systems as opposed to in vivo or in vitro experimental studies. These in silico
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Recently the classical view of the compartmentalization of t
2021-10-19
Recently, the classical view of the compartmentalization of the plant isoprenoid metabolism has been re-evaluated, following the demonstration of the partial peroxisomal localization of the mevalonic icrt (MVA) pathway, generally regarded as cytosolic. Using GFP-tagging approaches, the last two enz
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Recent studies in our laboratory demonstrated that several
2021-10-19
Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his
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Fig summarizes the results for M concentration
2021-10-19
Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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Histamine in the central nervous system is produced
2021-10-19
Histamine in the central nervous system is produced mainly in the tuberomammillary nucleus and is implicated in learning and memory as well as sleep and wakefulness, feeding and drinking, and neuroendocrine regulation . For instance, treatment with antihistamines not only produces drowsiness but als
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G P also plays a critical role in regulating
2021-10-19
G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon
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Activity of compound in rat
2021-10-19
Activity of compound 10 in rat 103 9 receptor tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as
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We show that pharmacological inactivation
2021-10-19
We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase
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Nitecapone Having identified initial leads and
2021-10-19
Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Nitecapone derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl, chloro a
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G protein coupled receptors GPCRs constitute a large family
2021-10-19
G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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ML-090 The GPR gene was included
2021-10-19
The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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The diseases of ocular surface and the cornea
2021-10-19
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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br Materials and methods br Results br Discussion ENU mutage
2021-10-19
Materials and methods Results Discussion ENU mutagenesis is a powerful approach to identify novel genes or integrin signaling pathway to dissect the molecular basis of mammalian immune system (Siggs, 2014). T cells are critical components in the host defense against pathogens, and their act
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