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Compared with the tetrazole derivative the potency
2021-10-16
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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Introduction Although G protein coupled receptor GPR was con
2021-10-16
Introduction Although G-protein-coupled receptor 55 (GPR55) was considered a cannabinoid receptor, it differs phylogenetically from cannabinoid type 1 (CB1) and type 2 (CB2) receptors as it lacks the classic cannabinoid-binding pocket (Baker et al., 2006). GPR55 is sensitive to an array of cannabin
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br Acknowledgments br Introduction Manipulating target prote
2021-10-16
Acknowledgments Introduction Manipulating target protein expression via either induction or suppression of gene expression is a powerful technology that has been widely used in the recent past in the field of neurobiology, both to study the pathophysiological significance of a target gene and
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br Introduction Depression is a prevalent and disabling
2021-10-16
Introduction Depression is a prevalent and disabling psychiatric illness that affects millions of individuals worldwide, resulting in enormous personal suffering and public health costs [1]. Traditional antidepressants such as monoamine oxidase inhibitors (MAOIs) and selective serotonin reuptake
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It was previously proposed that glucagon acts in the
2021-10-16
It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the auda synthesis via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the l
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The first phase of insulin secretion is due to calcium
2021-10-15
The first phase of insulin secretion is due to calcium signaling because of glucose sensing, increased cytoplasmic ATP levels, cellular depolarization, calcium influx and activation of calcium sensing molecules that eventually causes the fusion of the insulin granules to plasma membrane (exocytosis)
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The glycolytic activator phosphofructo kinase fructose bisph
2021-10-15
The glycolytic activator 6-phosphofructo-2-kinase/fructose 2,6-bisphosphatase 3 (PFKFB3) is well-known as a downstream substrate of hypoxia-inducible factor 1α (HIF-1α) signaling pathway [5,6]. Tumor hypoxia has long been associated with increased malignancy, poor prognosis and drug resistance. HIF-
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Omecamtiv mecarbil br Disp Mediated Hh Membrane Recycling
2021-10-15
Disp-Mediated Hh Membrane Recycling Due to its cholesterol modification, Drosophila Hh enriches on sphingolipid-rich apical membranes of polarized epithelial Omecamtiv mecarbil 33., 38., 39.. Genetic studies examining Hh release from wing imaginal disc epithelia suggest that Hh must be endocytos
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gstp1-1 br Intracellular trafficking with concurrent signali
2021-10-15
Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g
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In our studies the EC values for long
2021-10-15
In our studies, the EC50 values for long-chain unsaturated fatty acids added to the short form of human GPR120 receptor (BC101175), were higher than the EC50 values previously reported (Hirasawa et al., 2005) for the long form of GPR120 (NM_181745), which was co-expressed with Gα16 protein.(Table 2)
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Another group of secreted proteins that determine
2021-10-15
Another group of secreted proteins that determine the virulence of V. dahliae are effectors and microbe associated molecular patterns (MAMP) that regulate plant immunity [10]. So far, there is only one AGI5198 receptor gene Ave1 cloned in V. dahliae, yet it does not exist in race 2 strains such as V
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br Methods and materials br Results Overall
2021-10-15
Methods and materials Results Overall, free glutamate intakes in US children and adults are shown in Table 1. The sample-weighted mean intake of crude free glutamate was 258 mg/d for children and 322 mg/d for adults. Furthermore, the corresponding energy-adjusted value was 136 mg/1000 kcal and
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In summary activated A AR exacerbated
2021-10-15
In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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Transient forebrain ischemia in rodents induces a reduction
2021-10-15
Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the beta-Nicotinamide mononucleotide mg region most vulnerable to ischemia-induced dama
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Single cell reverse transcriptase PCR on A
2021-10-14
Single-cell reverse transcriptase-PCR on A. mellifera antennal lobe (AL) cells showed the expression of RDL as well as another GABA receptor like subunit, LCCH3 (Dupuis et al., 2010). Based on whole cell patch-clamp electrophysiology it was concluded that the predominant GABA receptors in AL cells a
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