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While NR upregulation in the spinal cord
2021-09-28

While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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Further explorations at the ortho and meta positions
2021-09-28

Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp
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Glucose uptake a critical metabolic control point
2021-09-28

Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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The genes for the receptors
2021-09-28

The genes for the receptors for peptides similar to glucagon are dispersed on three human chromosomes, with two on chromosome 17 (GCGR and GLP2R) and one each on chromosomes 6 (GLP1R) and 19 (GIPR) (see Table S1). The exon–intron gene structures of these genes are similar, as are the genes for other
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Sometime ago we have described diamino triazines as histamin
2021-09-27

Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by glutamate receptor and zymosan. In this work we describe n
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br Conclusion The histamine H receptor has been the
2021-09-27

Conclusion The histamine H3 receptor has been the focus of a great deal of research over the past four decades and in this context, substantial progress has been made in developing H3R-related ligands. The involvement of H3Rs in many neurological disorders has been documented by several lines of
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An interference of fluorescence derived from biological samp
2021-09-27

An interference of fluorescence derived from biological samples is also an important Sodium Nitroprusside to be addressed in the fluorescent analysis for biological samples. Advanced glycation endproducts (AGEs) are representative endogenous fluorescent substances that are widely distributed in var
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Racemic protein crystallography has been proven to be a
2021-09-27

Racemic protein crystallography has been proven to be a powerful technique for crystallizing proteins , , , , . The structures of many difficult-to-crystallize peptides/proteins of different sizes were resolved by the racemic protein crystallography combined with the protein chemical synthesis , , ,
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SynaptoRedTM C2 sale br Conclusion br Conflict of interest b
2021-09-27

Conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements Introduction Free fatty acids (FFAs) are essential nutrients that contribute to various cellular functio
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As part of our discovery
2021-09-27

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 fragmen
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br Expression of GlyT in the spinal cord
2021-09-27

Expression of GlyT in the spinal cord in response to neuropathic pain Twelve days after sham injury or CCI, GlyT1 and GlyT2 mRNA expression in rat spinal cord was analyzed using qPCR. Here, no significant changes in expression of the transporters in our CCI model of neuropathic pain compared with
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The LBD experiences a large scale conformational transition
2021-09-27

The LBD experiences a large-scale conformational transition between open and closed states upon agonist binding within the cleft separating the two lobes of the domain. The upper lobe (Lobe 1, also called D1) is connected to the ATD, and the lower lobe (Lobe 2, also called D2) is connected to the TM
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Through the analysis of various synthetic GPR agonists
2021-09-27

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic aa2414 motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering TAK-8
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Fidaxomicin Limitations of our study are the following
2021-09-26

Limitations of our study are the following: we did not measure central energy metabolism in parallel, so we can only hypothesize that GLUT1 hypermethylation may be associated with alterations in central glucose metabolism. We did not measure GLUT1/GLUT4 gene expression or glucose uptake, so that we
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One may carefully evaluate the concept pancreas derived GLP
2021-09-26

One may carefully evaluate the concept ‘pancreas derived GLP-1′ as this may dependent on the specificity of the cytidine used in immunohistochemistry or radiommunoassays. If either a side-viewing antibody or a C-terminal wrapping antibody raised against GLP-1 is applied one may also identify N-termi
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