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As part of our discovery efforts searching for
2022-05-04
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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br Advanced Glycation Endproducts As glucose levels
2022-05-04
Advanced Glycation Endproducts As glucose levels rise within sensory neurons as a result of hyperglycemia, normal metabolic pathways become overwhelmed and excess glucose is shunted into other ancillary pathways that, under these conditions, become damaging. One consequence of hyperglycemia is th
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While the S site has been implicated in binding it
2022-05-04
While the S2 site has been implicated in binding, it Tunicamycin is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. However, there are n
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benfotiamine australia Fatty acids have been repeatedly
2022-05-04
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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Fourthly the distribution sites after i c v
2022-05-04
Fourthly, the distribution sites after i.c.v. injection of FAM-ghrelin(1–7)-NH2 were explored in mice using the technologies of fluorescence labeling. The green fluorescence of FAM-ghrelin(1–7)-NH2 was strongly distributed in these structures of lateral ventricle, lateral septal nucleus, dorsal part
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br Conclusions br Introduction Bioinformatics analysis shows
2022-05-04
Conclusions Introduction Bioinformatics analysis shows that there are about 300,000 G-rich sequences in human genome if searching with the consensus sequence (G3+N1-7G3+N1-7G3+N1-7G3+) [1], and their localizations are non-random. These G-rich sequences always localize in functional regions, su
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To date the underlying mechanism of ropivacaine
2022-04-29
To date, the underlying mechanism of ropivacaine in inducing neurotoxicity remains unclear. Cell death was intimately involved in local-anesthetic neurotoxicity [6,18]. Two classic signaling pathways triggered cell death: the extrinsic pathway and the intrinsic pathway [12]. Our study demonstrated t
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Methods br Results br Discussion SV exocytosis from
2022-04-29
Methods Results Discussion SV exocytosis from excitatory boutons is more sensitive to inhibition by isoflurane than exocytosis from inhibitory boutons,4, 31 but the mechanism(s) of this synaptic selectivity is unknown. Although P/Q-type VGCCs contributed quantitatively more to SV exocytosis t
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br Materials and methods br Results
2022-04-29
Materials and methods Results Discussion In this study, we demonstrated that, at the level of hREECs, blockade of the ETA receptor partially inhibited the effect of NPY on the secretion of ET-1. This suggests that the secreted ET-1 by NPY contributes, in part, to its own secretion via activ
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br Role of catecholamines in HIV associated neuroinflammatio
2022-04-29
Role of catecholamines in HIV-associated neuroinflammation Concluding remarks However, more research is needed to determine the precise mechanisms responsible for the immunomodulatory effects of catecholamines, including the involvement of specific receptors and signaling pathways in immune ce
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The finding that a peptide consisting
2022-04-29
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino Methscopolamine synthesis ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor
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The finding of histamine action on ASICs also raises the
2022-04-29
The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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Several lines of evidence suggest that thermosensation in AF
2022-04-29
Several lines of evidence suggest that thermosensation in AFD is unlikely to be mediated by thermosensitive ion channels. AFD exhibits a steep temperature dependence with a reported Q of >1015 for temperature-evoked current, implying a strong amplification step in the thermotransduction process (Ram
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Renal disease is characterized by
2022-04-29
Renal disease is characterized by aberrant fibrotic remodeling of renal tissue, elevated apoptosis in kidney tissue, and eventual organ failure. In addition, patients with renal disease are more likely to suffer from systemic hypertension due to oxidative damage (reviewed in Ref. [18]). Treatment of
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br NO GC pathway and implications for glaucoma Direct
2022-04-29
NO-GC-1 pathway and implications for glaucoma Direct in vivo measurement of NO in the eye is not yet feasible. However, measurement of nitrate and nitrite levels are routinely used as markers for the activity of NOS and the production of NO radicals [98]. Several studies in human glaucoma patient
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