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Because of its excellent GPR
2022-05-17
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, vorapaxar was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel
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br Conflict of interest br Funding br
2022-05-16
Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino Dexmedetomidine derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-me
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Bergmann glia cells BGCs are the
2022-05-16
Bergmann glia phenylephrine hydrochloride (BGCs) are the most abundant glia cells in the cerebellum, comprising more than 90% of the cerebellar glia. These cells span the entire cerebellar molecular layer and encapsulate neuronal somata, dendrites and axons. BGC are involved in neurotransmitter upt
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The unique mechanism of EAAT anion channel gating results
2022-05-16
The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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Apoptosis a form of programmed cell death
2022-05-16
Apoptosis, a form of programmed cell death, is a critical component in maintaining homeostasis and growth in all tissues and plays a significant role in immunity and cytotoxicity [54,55]. Although GR are expressed in all immune cells, the physiological outcomes of GR activation are highly cell type-
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GIPR genes were not found in any of
2022-05-16
GIPR genes were not found in any of the available bird genome as well as the genomes of several species of fish (Tables S3 and S4). The genomic neighborhoods surrounding the GIPR genes in species that have them was generally conserved (see Fig. 8), and like GLP2R, those fish that did have a Gipr gen
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Decreases in LS mean h WMG versus placebo were
2022-05-16
Decreases in LS mean 24-h WMG versus placebo were observed with both the 10mg q.d. a.m. (−18.8mg/dL) and 6mg q.d. p.m. (−25.0mg/dL) MK-3577 ‘partial blockade’ regimens, but was not assessed for the 25mg b.i.d regimen. Decreases in FPG versus placebo were observed for both the 10mg q.d. a.m. (−7.2mg/
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The findings in mice were
2022-05-16
The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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The waiting time for first
2022-05-16
The waiting time for first arrival of 2-Palmitoylglycerol into the dense fraction of 3–4 min at the normal chloride conductance, and about 30 min with inhibition to about 10% of the normal value, signifies that the Gardos channels in the activated cells become maximally or near maximally activated,
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Galactosidase Gal EC is an enzyme exoglycosidase and the
2022-05-16
α-Galactosidase (α-Gal, EC 3.2.1.22) is an enzyme exoglycosidase, and the main role of this enzyme is the enzymolysis of α-galactoside. After this hydrolysis, galactosylation of cyclodextrins by the α-galactosidase occurs, thus forming α-galactosyl-cyclodextrin. This branched CD is easy to dissolve
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Cellular inhibition is caused by the hyperpolarization of th
2022-05-16
Cellular inhibition is caused by the hyperpolarization of the cell and is mediated by both synaptic and extrasynaptic GABAARs. Synaptic GABAARs are sensitive to high concentrations of GABA released at the synapse and mediate phasic inhibition. In contrast, extrasynaptic GABAARs mediate tonic inhibit
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The intestinal epithelium is the first line of
2022-05-16
The intestinal epithelium is the first line of defense against pathogens and noxious agents and exerts a range of physiological activities, including digestion and ru listings mg of nutrients. The intestinal wall consists of a series of finger shaped protrusions called villi and invaginations known
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During the course of our optimization of the diarylsulfonami
2022-05-16
During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic somatostatin receptor and compound in
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br Materials and methods br Results and discussion br Conclu
2022-05-16
Materials and methods Results and discussion Conclusions Acknowledgments The authors are grateful to Dr. N. Prevete for providing the human AGS shCTR and AGS shFPR2 cells. This work was supported by POR Campania FSE 2007-2013 Project CREME and Ministry of Health, Italy, RF-2011-02349269.
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We used a culture model of
2022-05-16
We used a culture model of human erythropoiesis that recapitulates all developmental stages [24] to screen a focused set of lncRNAs for potential contribution to this program. We found induction of lncRNA Fas-antisense 1 (Fas-AS1 or Saf) during RBC maturation and demonstrate that essential erythroid
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