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br Brief overview of the glutamate system and
2021-12-30

Brief overview of the glutamate system and rationale for targeting the glycine site of NMDARs In the central nervous system (CNS), glutamate is the major excitatory neurotransmitter and works in concert with gamma-aminobutyric endothelin receptor antagonists (GABA), the primary inhibitory neurot
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However Gingrich and Hen reported that absence of the
2021-12-30

However, Gingrich and Hen reported that absence of the gene at all stages of ontogenesis of mice may interfere with the normal developmental program and/or the organism may undergo changes in other systems to compensate for gene absence (46). In addition, potentially altered maternal behavior of GP
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Up to now the research about the
2021-12-30

Up to now, the research about the effect of PAs on inhibiting carbohydrase activity in vitro or reducing blood sugar level in vivo was mainly reported in PAs from grape seeds, Lepisanthes alata (Malay cherry) leaves, sorghum, pomegranate, cranberry and persimmon (Banerji and Banerjee, 2016, Barrett
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br Multiple sclerosis MS is an immune
2021-12-29

Multiple sclerosis MS is an immune-mediated disease of the human CNS with a pathological signature featuring immunocyte infiltration, altered cytokine production, oligodendroglial degeneration, astrogliosis, microglial activation, multifocal demyelination and axonal degeneration (Schipper, 2004b)
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Finally our data found that the EBV dUTPase protein
2021-12-29

Finally, our data found that the EBV dUTPase protein modulates tryptophan, serotonin, and DA metabolism and use in vitro and in vivo. The EBV dUTPase may alter kynurenine catabolism in microglia in vitro, suggesting that there is an increase synthesis of quinolinic acid. Quinolinic acid, an agonist
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With the administration of OM fatty
2021-12-29

With the administration of OM3 fatty acids, it has previously been shown that the activation of GPR120 is linked to the secretion and circulating levels of the adipokine adiponectin [123] promoting anti-inflammation (downregulation of NF-κB) and insulin sensitivity [124]. Interestingly, Nrf2 also de
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Recently a G protein coupled receptor
2021-12-29

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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But some experiments did not support the
2021-12-28

But some experiments did not support the antinociceptive role of GalR2 in peripheral locations beyond the DRG. The partial saphenous nerve ligation and the complete Freund's adjuvant model in the rats demonstrated that close intra-arterial infusion of galanin, but not galanin (2–11), reduced cooling
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In conclusion our results show
2021-12-28

In conclusion, our results show that multiple receptor populations can be expressed when α4, β3 and δ mRNAs are injected into Xenopus oocytes and include β3 homomeric; α4β3; and β3δ receptors. The previously unidentified β3δ can be differentiated pharmacologically from either β3, α4β3 and α4β3δ rece
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Developmental studies have reported that some subunits of
2021-12-28

Developmental studies have reported that some subunits of GABAA receptors like α2 and α3 are predominantly expressed during in-utero development, and then substituted for α1 around birth in the rat hippocampus (Brooks-Kayal et al., 2001; Fritschy et al., 1994; Golshani et al., 1997; Kapur and Macdon
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Activation of FXR or TGR has overlapping but also
2021-12-28

Activation of FXR or TGR5 has overlapping but also differing effects on metabolic regulation and inflammation [1]. In this report, we demonstrate that in addition to preventing the progression of obesity, NAFLD, and atherosclerosis, activation of BA receptors can also promote regression of these com
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In addition to the robust intracellular calcium mobilisation
2021-12-28

In addition to the robust intracellular calcium mobilisation, DHA and TUG-891 also induced MMP-9 granules release and superoxide production, supporting a key role of calcium in bovine neutrophil defense responses (Burgos et al., 2011). Pisani et al. (Pisani et al., 2009) described a reduction of bas
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In conclusion a series of new
2021-12-28

In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed
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br Results br Discussion The present
2021-12-28

Results Discussion The present findings outline a novel regulatory mechanism for fasting-induced ketogenesis, which involves histamine release from mast HhAntag into the hepatic portal system, H1 receptor-mediated stimulation of liver OEA biosynthesis, and recruitment of the nuclear receptor P
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alkaline phosphatase inhibitor Synthesis of these hydrazide
2021-12-28

Synthesis of these hydrazide inhibitors is outlined in , . Condensation of Boc-carbazate with desired aldehyde resulted in hydrazone of type which were reduced to alkylated hydrazides using NaBH and toluenesulfonic acid. The resulting alkylated hydrazides were acylated with alkaline phosphatase i
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