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On the other hand we have previously demonstrated
2022-07-26
On the other hand, we have previously demonstrated that gelsemine displaced the H3-strychnine from membrane fractions of rat spinal cord homogenates. In addition, spinal gelsemine antinociception was blocked by intrathecal injection of the specific glycine receptor antagonist strychnine or gene sile
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br Experimental procedures br Results br
2022-07-26
Experimental procedures Results Discussion Although the presence and localization of the GlyR subunits have been determined in the adult retina, the proportion of each GlyR subunit has not been assessed in the adult or in the developing retina. In the present study, we carried out the absol
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br Conflicts of interest br Funding This work
2022-07-26
Conflicts of interest Funding This work was supported by the National Natural Science Foundation of China (No.81670558; 81800542), and the Science & Technology Development Fund of Tianjin Education Commission for Higher Education (No.2017KJ221). Acknowledgements Introduction Free fatty
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Herein we report the discovery of AM AM maintains
2022-07-26
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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During the tests in vitro
2022-07-25
During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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Some previous findings indicate that
2022-07-25
Some previous findings indicate that GALP has an influence on AVP and OT secretion from the posterior pituitary gland. Cunningham et al. (2004) noted that the expression of GALP mRNA was increased in the neurohypophysis of lactating rats compared to non-lactating rats, whereas GALP mRNA expression i
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In the course of our
2022-07-25
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric Maraviroc type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the process
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It is noted that knee swelling was milder
2022-07-22
It is noted that knee swelling was milder and the intensity of IL-4 staining (MFI) in the vehicle-treated group was lower in the second (Fig. 7a and d) than the first (Figs. 1a and 3f) AIA experiment. The variation in joint swelling between the two studies is most likely due to the models being perf
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Compared to a large database of NSCLC
2022-07-22
Compared to a large database of NSCLC samples matched for disease type, many of the frequently altered genes were similar to those seen in this series of FGFR fusion-positive samples; however, there were notable exceptions. As expected, alterations in known NSCLC drivers (KRAS and EGFR) were signifi
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Polyunsaturated fatty acids PUFAs represent
2022-07-22
Polyunsaturated fatty acids (PUFAs) represent a class of lipids that contain two or more carbon double (unsaturated) bonds (CC) and classified as n-3, n-6 and n-9 fatty acids. PUFAs including n-3 such as docosahexaenoic 2-D08 (DHA), eicosapentaenoic acid (EPA) and n-6 such as arachidonic acid (AA)
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KP372-1 Potential roles for S P in angiogenesis cancer
2022-07-22
Potential roles for S1P in angiogenesis, cancer, and autoimmune diseases such as RA have been reported [73]. In RA synoviocytes, S1P has been shown to enhance expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) in response to the pro-inflammatory cytokines, TNF-α and interleukin (IL)-
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EZH can also interact with Ten Eleven Translocation gene fam
2022-07-22
EZH2 can also interact with Ten-Eleven Translocation gene family members (TET1, TET2, and TET3), which convert 5-methylcytosine (5 mC) to 5-hydroxymethylcytosine (5hmC), to cause changes in patterns of histone methylation and DNA methylation [52]. Huang et al. found that the expression levels of all
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Multi targeting agents are of major interest in modern
2022-07-22
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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The repurposing of well characterized and well tolerated
2022-07-22
The repurposing of well-characterized and well-tolerated drugs in order to treat illnesses for which they were not originally intended has emerged as an attractive alternative to a long and costly process of drug development. Repositioning antihistaminergic ligands seems a promising idea given that
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Over recent decades there were
2022-07-22
Over recent decades, there were three breakthroughs of high intensity heavy-ion acceleration [6]. The first is the invention of radio frequency quadrupole (RFQ) type accelerator, which could accelerate more than dozens of milli-ampere ion beams and is a good solution to space-charge-effect of heavy-
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