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To shed more light on the binding of benzophenanthridine
2022-06-29
To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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To date glycine receptors have been found in
2022-06-29
To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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Entry into CNS is tightly regulated
2022-06-29
Entry into CNS is tightly regulated by highly dynamic barriers, namely, the BBB, the blood-CSF barrier, and the arachnoid epithelium (Abbott et al., 2010; Yasuda et al., 2013). Similar barriers also exist within the CNS including the ependymal barrier as well as the cellular membrane barriers of the
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ICH induced striatal lesion produced a reduction of
2022-06-29
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino tlr signaling transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ische
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Ion dependence of mGluRs activity
2022-06-29
Ion dependence of mGluRs activity has been previously reported, notably to Ca2+ and Cl− (Kuang and Hampson, 2006). While mGlu1 and mGlu3 receptors were demonstrated to be sensitive to Ca2+, Cl− modulation was reported for all mGluRs, with a lesser extent for the mGlu2 receptor (DiRaddo et al., 2014;
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To further implicate the role of
2022-06-29
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 Apoptosis Inhibitor was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-t
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br Acknowledgements This work was supported by grants of
2022-06-29
Acknowledgements This work was supported by grants of the Argentine National Research Council (CONICET, PIP 0662). The authors express their appreciation to the Transmission Electron Microscopy Service (MET) of the Faculty of Veterinary Medicine of the National University of La Plata (Argentina)
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br Histamine H R Many of the highlight H R
2022-06-28
Histamine H3R Many of the highlight H3R ligands have been described as suitable pharmacological tools for in vitro or in vivo studies and are designated here. The number of ligands and structural categories is huge, and a number of inclusive reviews of the SAR and properties of H3R ligands have b
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br Dual acting HR antagonists While the present medicinal
2022-06-28
Dual-acting HR antagonists While the present medicinal chemistry efforts are mainly focused on selective ligands targeting GPCRs, and particularly on H1R, H3R and H4R selective antagonists/agonists, there were and, also, still are several efforts to develop dual acting H1R/H2R, H1R/H3R and H3R/H4
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Another important outcome of reducing
2022-06-28
Another important outcome of reducing hypothalamic HIF in DIO was the increase in gliosis and hypothalamic inflammation. Both experimental and human studies have shown that hypothalamic inflammation plays an important role in obesity by inducing resistance to anorexigenic signals, such as insulin an
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CTGF is an established YAP
2022-06-28
CTGF is an established YAP/TAZ target gene which plays a central role in tissue remodeling. Downregulation of CTGF mediates collagen loss in chronologically-aged human skin whereas persistent activation of CTGF can result in excessive deposition of collagen and fibrotic disorders [63]. The authors f
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To prevent toxicity of free hemoglobin as
2022-06-28
To prevent toxicity of free hemoglobin as well as its degradation metabolites heme and free iron, several scavenger proteins and degradation enzymes protect the body. Haptoglobin (Hp) is the most well described hemoglobin scavenging protein that binds free hemoglobin and transports it to macrophages
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86002 sale Nazar and colleagues reported a normal HER
2022-06-28
Nazar and colleagues reported a normal HER2 gene number in 13 primary and 2 recurrent ethmoid sinus adenocarcinomas, without any histological and immunohistochemical characterization, so a comparison with the present findings is impossible [14]. More recently, 552 head and neck carcinomas have been
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Furthermore the absolute lack of E allele expression
2022-06-28
Furthermore, the absolute lack of E2 allele expression in both chronic and SVR cases, supports the protective role of the E2 allele against HCV infection at a time of exposure. However this hypothesis could not be entirely proved by this study due to lack of healthy individuals participation. Simila
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Given the role that activation of GC C has in
2022-06-28
Given the role that activation of GC-C has in stimulating fluid secretion in the intestine, attempts have been made to exploit this pathway to relieve symptoms of chronic constipation. Currently, an orally administered synthetic ST mimic, linaclotide [29], has been successfully shown to alleviate co
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