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It is well known that histamine functions not
2021-10-19
It is well known that histamine functions not only as an inflammation mediator but also as an aminergic neurotransmitter or neuromodulator. Histaminergic neurons [27], [28] and histamine receptor subtypes (H1R [29] and H3R [30]) are widely existed in mammalian central olfactory system. Histamine reg
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The fibulins are a newly abundantly in
2021-10-19
The fibulins are a newly abundantly in the basement membrane of blood vessels. Among them, fibulin-1 is essential for elastin polymerization. Tropoelastin cannot be assembled into mature elastin fibrils without the functional fibulin-1. In adult blood vessels, pronounced fibulin 1 deposition can be
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In the H NMR spectrum
2021-10-19
In the 1H NMR spectrum two pairs of doublet resonances arising from the protons in the aromatic moiety of the two diastereoisomers can be readily observed around 7.5–7.6 ppm. These resonances can be used to detect and quantify the two diastereoisomers. From the results presented in Fig. 1A it can be
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br Acknowledgments This research was partially supported by
2021-10-19
Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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pde inhibitor Acute in vivo experiments were
2021-10-19
Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding pde inhibitor control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg produ
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It is important to clarify whether the decrease in
2021-10-19
It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U
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br Regulation of Glu transporters The pivotal role of
2021-10-19
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino FDA-approved Drug Library calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These inc
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A oligomers increased ubiquitination of GLT in
2021-10-19
Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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Most of the above mechanisms are implicated in
2021-10-18
Most of the above mechanisms are implicated in attenuation of myocardial I/R injury. However, the role of GalR2 receptor activation in cardioprotection remains unclear because of the lack of receptor subtype selectivity of peptides G2 and G3. It has been shown that Ala5-galanin (2–11) (G4) has a hig
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The orientation of the immobilized enzyme may
2021-10-18
The orientation of the immobilized enzyme may affect its activity and stability and therefore the final biocatalyst performance. Since proteins present areas more prone to unfolding in their surface or near to it [36], the immobilization through these areas may improve the final biocatalyst stabilit
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The suboptimal trypsin selectivity profile
2021-10-18
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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Although drug monitoring is not
2021-10-18
Although drug monitoring is not usually requested, there are some cases where measurement of DOACs in 73122 australia is useful, and of special help for managing patients at risk. These cases include the control of adherence to a therapeutic protocol, surveillance of drug accumulation risk in long
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br Hedgehog pathway The Hedgehog pathway
2021-10-18
Hedgehog pathway The Hedgehog pathway (Fig. 1) derives its name from Hh gene mutant Drosophila, which presents a spiked phenotype resembling the animal “hedgehog” [13]. The Hh proteins control embryonic development in vertebrates, where the signaling mechanisms mediated by the proteins are multip
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LY2606368 HCl br For some time it was known that
2021-10-18
For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor LY2606368 HCl in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on the r
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TGR is a class A
2021-10-18
TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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