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Several studies have shown that regulation of glutamate
2022-04-14
Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu
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br Methods GLUT DS was diagnosed either when analysis
2022-04-14
Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF YC 1 receptor below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percentile and
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GS-4997 cAMP is a key secondary
2022-04-14
cAMP is a key secondary messenger which transduces extracellular signals at glucagon receptors to intracellular effector molecules. cAMP-protein kinase A (PKA) pathway increases the gene expression of enzymes including phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6-phosphatase (G6Pase) whic
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Contradictory results have been described regarding the role
2022-04-14
Contradictory results have been described regarding the role of the Shh pathway during vertebrate skeletal myogenesis. Different studies have shown that Shh can increase or inhibit myoblasts proliferation and terminal muscle differentiation, depending on the experimental model [[1], [2], [3], [4], [
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br Conclusions We concluded that the inhibitory
2022-04-13
Conclusions We concluded that the inhibitory effects of propofol on fMMYALF-induced neutrophil activation are mediated by competition with FPR1, which inhibits receptor-mediated downstream signaling and inflammatory responses such as oxidative burst, elastase release, and chemotactic migration (F
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br Redox cancer therapy The understandin http www apexbt
2022-04-13
Redox cancer therapy The understanding of ROS mechanisms supported the development of two parallel anticancer strategies based on ROS modulation, the use of antioxidants for cancer prevention and the use of ROS inducers to exacerbate oxidative stress to lead cancer Adenine HCl sale to death [27]
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br Importance of iron and lipoxygenase in ferroptosis What
2022-04-13
Importance of iron and lipoxygenase in ferroptosis What remains to be somewhat controversial is the role of iron and lipoxygenases (LOX) in the death process, specifically in lipid peroxidation. So far, iron chelators have been repeatedly shown to halt ferroptosis (hence its name) induced by chem
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Other N substituted carboxamide oxy pyridine derivatives a
2022-04-13
Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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Glutathione transferases GST have been
2022-04-12
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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Abn CBD induced changes reduced microglial cell density cell
2022-04-12
Abn-CBD induced changes (reduced microglial cell density, LXR-623 mg size and a lower density of ramification) in the microglial morphology that could be compatible with a blockade of the neuroinflammation provoked by MPTPp. The absence of GPR55 transcripts in microglial cells in striatum and the s
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br Niacin has long been used for the
2022-04-12
Niacin () () has long been used for the treatment of lipid disorders and for the prevention of cardiovascular disease, the leading cause of death in the U.S., as a result of its ability to raise high-density lipoprotein (HDL) levels. Recent mechanistic investigations have shown that niacin may exe
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The saturated carbocyclic derivatives pyrazoles M and M
2022-04-12
The saturated carbocyclic derivatives, pyrazoles (2.5μM and 5.2μM) and (9.0μM and 2.5μM), provided little improvement in potency when compared to the linear alkyl derivatives, whereas the C5-phenyl derivative (0.31μM and 0.43μM) showed promise as a scaffold for further structural modifications.
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GPR A a G protein coupled receptor located mainly
2022-04-12
GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic Miltefosine synthesis [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to
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br FXR Agonists Azepinol b indole hEC
2022-04-12
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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Some studies show that testosterone may
2022-04-12
Some studies show that testosterone may be involved in regulating cell proliferation and its stimulating effect has been proved in castrated rats (Wainwright et al., 2011), but not in mice and meadow voles (Ormerod and Galea, 2003; Benice and Raber, 2010). However, the seasonal difference in cell pr
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