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Dual H H receptor antagonists developed by GlaxoSmithKline h
2022-05-10
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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Distribution of histamine receptors in the intestines varies
2022-05-10
Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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br Conflict of interest br
2022-05-10
Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent
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br Hedgehog pathway in embryonic development It is now
2022-05-10
Hedgehog pathway in embryonic development It is now well established that the Hedgehog pathway solves a role as one of the essential signaling mechanisms for the modulation of cellular growth and differentiation during embryogenesis. Operating through time- and position-dependent mechanisms, this
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br Acknowledgements This work was financially supported by
2022-05-10
Acknowledgements This work was financially supported by the National Natural Science Foundation of China (Grant No. 81803033) and the “Double First-Class” University project (CPU2018GF02). Introduction Atrial fibrillation (AF) is the most common progressive cardiac rhythm disorder. Studies ha
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sirtuin Stability of DBS over the day
2022-05-10
Stability of DBS over the 60-day time points was encouraging, with a maximum of 0.1 log10 IU/mL degradation from the day 1 value (Supplementary Fig. 1 and Supplementary Table 3). Discussion This study evaluated the sensitivity and specificity of the Aptima HCV Dx assay for HCV RNA detection from
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Moreover we have demonstrated that internalization and subce
2022-05-10
Moreover, we have demonstrated that internalization and subcellular trafficking of NPRA, using IF staining (IFS) and co-IP of plasma membrane, endosomal, lysosomal, and recycling endosome markers to follow intracellular trafficking and signaling by confocal IF microscopy (CIF) and immunoblotting (IB
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br Discussion In the present paper it
2022-05-10
Discussion In the present paper it was shown for the first time that the conjugation of ethacrynic alltrans and glutathione catalyzed by GSTP1-1 stereospecifically forms one of the diastereoisomers of the glutathione conjugate (EASG). Chemical conjugation results in formation of a mixture of bot
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Further SAR was explored with the imidazole series to
2022-05-10
Further SAR was explored with the imidazole series to achieve better enzyme inhibition activity (). In comparison to published earlier, replacing the amide with sulfonamide and reverse sulfonamide maintained the GSNOR inhibitory activity. It is clear that exchanging the phenyl ring (, and ) by t
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br GPR a G protein coupled receptor GPCR was
2022-05-10
GPR35, a G protein-coupled receptor (GPCR), was discovered and classified as an orphan GPCR in 1998 and deorphanized in 2006 by the discovery of kynurenic ion channels as the endogenous agonist. Since its discovery, limited references on the GPR35 receptor have appeared, due in part to a scarcity
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No compounds in this series showed any appreciable activity
2022-05-10
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma
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br The glycine transporter GlyT was originally
2022-05-10
The glycine transporter 1 (GlyT1) was originally identified as a member of the solute carrier family 6 of sodium- and chloride-dependent neurotransmitter transporters . GlyT1 is expressed in the central nervous system and in peripheral tissues; mainly in erythroid cells, from erythroblasts in the
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br Materials and Methods br Results All of the studied
2022-05-10
Materials and Methods Results All of the studied transporter genes were expressed at detectable levels in all the analyzed samples at mRNA level by means of applied rt-PCR method (CTRizatriptan Benzoate was observed for ABCC4, ABCC1, ABCG2, SLC22A3, and SLC22A18 (less than 10% of mean expressi
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Prior to cellular uptake studies of
2022-05-10
Prior to cellular uptake studies of LDC000067 , docking simulation was performed (A). The result suggested this complex was capable of binding in the cavity of an outward open XylE. The orientation of the sugar moiety in the docked complex was similar to that of the glucose unit bound in the crysta
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The simple carrier model for GLUT transport activity propose
2022-05-10
The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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