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The pharmacokinetics of was obtained in mouse
2022-06-02

The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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SBI-0206965 A linker length of and atoms was
2022-06-02

A linker length of 4 and 5 atoms was found to be optimal ( and ) compared to the only weakly active compounds with longer linkers ( and ) or the inactive compounds with shorter linker chains (–). In a next step incorporation of hetero-atoms in the linker was explored (). An amide linker as in and di
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The importance of FXR FGF signaling in
2022-06-02

The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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In the latent inhibition model a conditioned stimulus
2022-06-01

In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group
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Regarding the causative diseases of ES
2022-06-01

Regarding the causative diseases of ES, patients with unknown cause and those with encephalitis had significantly higher CSF levels of 2-Deoxyadenosine 5-diphosphate against GluN2B-NT2 and GluN2B-CT than the disease controls, but patients with genetic disorder and those with cortical dysplasia show
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As cardiovascular disease accounts for the majority
2022-06-01

As cardiovascular disease accounts for the majority of deaths in subjects with T2D, it is imperative that we better characterize the cardiovascular risks and benefits of the various therapies we prescribe to these individuals to control their glycemia. Indeed, the potential to identify subsets of di
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Due to the versatility of
2022-06-01

Due to the versatility of the ghrelin system and its multiple functions, dysregulation in some of the components of the ghrelin system, such as ghrelin, GOAT, and GHSR, might lead to pathogenesis of many endocrine-related diseases, including obesity, short stature, cancer, inflammatory, and cardiova
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bardoxolone receptor In this study an galactosidase gene Gal
2022-06-01

In this study, an α-galactosidase gene, GalA, from a Aspergillus oryzae strain RIB40 [14] was artificially synthesized. To produce high levels of secretory expression in Pichia and facilitate its industrial application, we systematically investigated the gene dosages and the role of the ERSAs, namel
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Methscopolamine Developmental studies have reported that som
2022-06-01

Developmental studies have reported that some subunits of GABAA receptors like α2 and α3 are predominantly expressed during in-utero development, and then substituted for α1 around birth in the rat hippocampus (Brooks-Kayal et al., 2001; Fritschy et al., 1994; Golshani et al., 1997; Kapur and Macdon
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The effect of GC on Fgf was not directly dependent
2022-06-01

The effect of GC on Fgf21 was not directly dependent on ileal Fgf15 because basal Fgf21 Amfenac Sodium Monohydrate was similar in Fgf15+/+ and Fgf15−/− mice. Moreover, GC treatment induced similar Fgf21 up-regulation in both strains. Fxr activation has been reported to increase Fgf21 expression and
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In this study we have investigated
2022-06-01

In this study, we have investigated the expression of FXR and TGR5 in CCA tissues in two independent cohorts of patients and determined their association with tumor clinicopathological parameters. The expression of both BA receptors was also evaluated in CCA human cells and normal human cholangiocyt
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br Medium to long chain fatty acids
2022-06-01

Medium- to long-chain fatty acids Medium- to long-chain fatty acids impart a wide range of physiological effects. Medium-chain and long-chain fatty acids have 6–12 carbons and >12 carbons, respectively. As the energy source, these fatty acids are supplied primarily by food intake, biosynthesis, a
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Endothelial cells receive a variety of
2022-06-01

Endothelial cells receive a variety of information from the environment which finally guides them through all phases of neovascularization. Angiogenic signals enhance the proliferation of endothelial cells, upregulated resistance to apoptosis, alterations within proteolytic balance, reorganization o
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keap1 nrf2 br Role of ferroptosis in
2022-06-01

Role of ferroptosis in PD Pathological progression of PD displays features that may facilitate ferroptosis induction such as elevated iron in the SNpc [49], [57], [88], [122], depleted GSH [194] and lipid peroxidation [51]. Iron chelation has been shown to mitigate the motor impairment in mouse m
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Several observations about structure activity relationships
2022-06-01

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic vx 809 australia class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether l
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