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Compared with the tetrazole derivative the potency of analog
2022-08-24
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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New follicular wave emergence is associated closely with
2022-08-24
New follicular wave emergence is associated closely with the stage of the estrous Talarozole (Sirois and Fortune, 1988). As indicated by results from the present experiment, cows that had regression of the largest follicle on Day 0 of treatment onset had follicle wave characteristics that were cons
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We started our investigation by evaluating the
2022-08-24
We started our investigation by evaluating the impact of changes to the piperidine moiety of (). As demonstrated with morpholine and piperazine , attenuation of nitrogen basicity resulted in complete loss of activity, suggesting that a basic heterocyclic nitrogen is important for potent inhibition
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We next compared the enhancing effects
2022-08-24
We next compared the enhancing effects of 100nM zinc on currents produced by a low concentration of glycine with zinc effects on the same currents produced by the partial agonist taurine. In this experiment, zinc was co-applied with concentrations of glycine or taurine producing 5–10% of the maximal
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Ironically another series of studies examining
2022-08-24
Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th
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A number of anti diabetic drugs are available that
2022-08-24
A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore
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Apramycin Sulfate Congenital Gcgr mice exhibit increased hep
2022-08-23
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific Apramycin Sulfate impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405
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alizarin The current gold standard for diagnosing BAM or BAD
2022-08-23
The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) alizarin (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated taurocholic acid and m
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In this study we intended to explore
2022-08-23
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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br Materials and methods br Results
2022-08-23
Materials and methods Results The immunoblot analysis demonstrated the presence of similar immunoreactivity by liver FBPase in hepatic and renal extracts. These results indicate that FBPase is present in a similar amount in both tissues. Moreover, the analysis revealed that the antibody detect
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The anti platelet functions of
2022-08-23
The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagat
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br Materials and methods br Results br
2022-08-23
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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An important aspect of macrophage biology
2022-08-22
An important aspect of macrophage biology, highly influenced by HO-1 activity, is macrophage polarization. The broadest classification, based on the in vitro stimulation, surface marker expression, and inflammatory cytokines production, describes macrophages as classically activated, proinflammatory
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GSK can function in regulating insulin signaling and glucose
2022-08-22
GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin
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Abn CBD induced changes reduced microglial
2022-08-22
Abn-CBD induced changes (reduced microglial cell density, CP 154526 receptor size and a lower density of ramification) in the microglial morphology that could be compatible with a blockade of the neuroinflammation provoked by MPTPp. The absence of GPR55 transcripts in microglial cells in striatum an
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