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The experiments indicate that a
2021-11-30
The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in BTB06584 preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but not in vessels pre
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Many investigators have noted structural similarities betwee
2021-11-30
Many investigators have noted structural similarities between certain flavonoids and benzodiazepines, such as diazepam, that are the most widely studied positive modulators of GABAA receptors. Benzodiazepines can act on these receptors via ‘two distinct and separable mechanisms’ (Walters, Hadley, Mo
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Free fatty acids FFAs which
2021-11-30
Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty A-1210477 receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these FFAs. Short c
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br Conclusions Our in vitro and in vivo data
2021-11-30
Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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The urea derivatives a e were obtained
2021-11-30
The urea derivatives 7a–e were obtained from 1-(3-phenoxybenzyl)-piperazine (6) by reaction of isocyanate, or triphosgene and subsequent reaction of produced carbamoyl chloride with the amine RH as shown in Scheme 2. The imidazole urea 7g was prepared by reaction of 6 with 1,1′-carbonyldiimidazole.
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The first phase of insulin secretion is
2021-11-30
The first phase of insulin secretion is due to calcium signaling because of glucose sensing, increased cytoplasmic ATP levels, cellular depolarization, calcium influx and activation of calcium sensing molecules that eventually causes the fusion of the insulin granules to plasma membrane (exocytosis)
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The biochemical cell culture activities and properties of bi
2021-11-30
The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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Utilization of fascinating properties such as
2021-11-30
Utilization of fascinating properties, such as localized surface plasmon resonance (LSPR), high fluorescent quantum yield, biocompatible nature, chromogenic and electrocatalytic functionality of several nanomaterials for histamine sensing is also quite evident where the nanomaterials have served as
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br Statistical analysis The mean standard deviation median r
2021-11-30
Statistical analysis The mean, standard deviation, median, range, frequency, and percentage were used for data description. The chi-square (x2) test was used for analyses the differences in categorical variables in the 2-way table. Overall survival (OS) was defined as the time interval between t
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Carbon monoxide another key product from the breakdown
2021-11-30
Carbon monoxide, another key product from the breakdown of heme by HO-1, also plays an important role in the vasculature. Like NO, CO is endogenously derived from the endothelium [68] and can weakly activate sGC by binding to its heme moiety [69]. CO was found to have vasodepressor activity in rats
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The present study chose the fdh
2021-11-30
The present study chose the fdh gene, the homolog of mammalian GSNOR, to generate UAS-fdh and fdh double-stranded RNA interference (ds-RNAi) transgenic Drosophila. These transgenic models were used to study the effect of GSNOR activity modulation on visual learning and memory and to explore the poss
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Pharmacologic approaches of inhibiting GSNOR activity have r
2021-11-30
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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Lean mass is representative of the muscle tissue
2021-11-29
Lean mass is representative of the muscle tissue mass equivalent of all the body parts containing water, excluding fat, bone minerals, and such substances which do not contribute to the NMR signal, such as hair, claws, etc. (ECHO-MRI (Houston, TX) user's manual). It was interesting that in the Bob-C
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Active compounds and were further tested and EC and pEC
2021-11-29
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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Here we reported series of carbohydrate
2021-11-29
Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of pepstatin and their polyol structures give them many unique biological properties as we have described earlier. More int
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