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br Biologically active non peptide galanin receptor ligands
2021-11-24
Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas
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In this review we will highlight how the functional
2021-11-24
In this review we will highlight how the functional impact of GABA receptors activation in thalamic neurons far exceeds the traditional “shunting” effect and shapes the whole thalamic network excitability. We will show how GABA released during either tonic or burst firing of GABAergic thalamic neuro
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In recent years many studies have demonstrated that
2021-11-24
In recent years, many studies have demonstrated that the release of endogenous FPR ligands can influence severe diseases associated with inflammation, including systemic inflammatory response syndrome (SIRS)20, 21 and cancers, such as glioblastoma as well as gastric and colorectal cancer 22, 23, 24.
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Both anxiety like behavior and sucrose preference intake wer
2021-11-24
Both anxiety-like behavior and sucrose preference/intake were reduced in GPR40/FFAR1 KO male mice, while social behavior was normal in KO mice. These findings indicate that brain GPR40/FFAR1 is involved in the modulation of anxiety- and depression-like behavior in rodents. Previous studies have demo
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br Introduction The term autophagy was coined by Christian
2021-11-24
Introduction The term “autophagy” was coined by Christian de Duve in 1963 to describe the process of removing and degrading intracellular components such as unused proteins and damaged organelles through lysosomes [1,2]. Autophagy has been divided into three main types, namely, macroautophagy, mi
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Phosphorylation of the p Rel A dimer the most
2021-11-24
Phosphorylation of the p50-Rel A dimer, the most common form of NF-κB, leads to ubiquitination of IκB proteins (Fig. 2). Poly-ubiquitination of IκB proteins identifies them for rapid degradation by 26S proteasomes, thereby allowing NF-κB dimers to undergo nuclear translocation and activate the trans
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To enhance the impact of GD
2021-11-24
To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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Figure shows the network of the persons with
2021-11-24
Figure 2 shows the network of the 47 persons with diagnosed HIV and their 192 contacts. Of the contacts, 149 (78%) were first-generation contacts and 43 (22%) were second-generation contacts. Color and shape combinations used for network nodes (i.e., persons) allow one to simultaneously discern past
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Whether histamine receptor distribution is altered in canine
2021-11-24
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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Glutathione transferases GST have been discovered in many
2021-11-23
Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To da
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Recently a G protein coupled receptor GPR a was identified
2021-11-23
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Mechanistic studies have suggested that the benefits of niacin therapy may result from the activation of GPR109a located on adipocytes. Recent experiments have shown that niacin activation of GPR109a re
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A high throughput screening campaign of the Lilly corporate
2021-11-23
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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Results indicated that superfusion of orexin alone glutamate
2021-11-23
Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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br Acknowledgements br Introduction Benzodiazepine BZ treatm
2021-11-23
Acknowledgements Introduction Benzodiazepine (BZ) treatment is widely used for quick and efficient anxiolytic and sedative responses. However, when the use is extended to longer periods, adverse effects emerge. These include tolerance to the initial drug effect, dependence as revealed by withd
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More recently NMR techniques have been used to monitor K
2021-11-23
More recently, NMR techniques have been used to monitor K+ () fluxes in isolated rat hearts. These reveal an increased rate of passive efflux of from Langendorff-perfused hearts at 20°C compared to 36°C or 10°C (Gruwel, Kuzio, Xiang, Deslauriers, & Kupriyanov, 1998). Similar experiments assessed th
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