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In the present study we conducted
2021-09-08

In the present study, we conducted a search for other possible endogenous ligands for GPR35. We focused on lysophospholipids because of the homology (30%) between GPR35 and GPR55 whose endogenous ligand is lysophosphatidylinositol (LPI) [9], especially 2-arachidonoyl LPI [10]. Notably, the GPR35 gen
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The compounds described in this
2021-09-08

The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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br Results and discussion br Conclusion In summary
2021-09-08

Results and discussion Conclusion In summary, starting from our previous lead vitamin k3 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivatives showed good
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832 582 4016 Na K ATPase adenosine triphosphate
2021-09-08

Na+/K+-ATPase, 832 582 4016 and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased as from 2
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In the gastrointestinal GI tract CART expression has
2021-09-08

In the gastrointestinal (GI) tract CART expression has been described in the enteric nervous system in rats (Ekblad et al., 2003), pigs (Wierup et al., 2007), sheep (Arciszewski et al., 2009), guinea pigs (Ellis and Mawe, 2003) and humans (Kasacka et al., 2012). Less is known about CART expression i
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To directly address whether pharmacological
2021-09-08

To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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The observed CORT induced increase in Cx phosphorylation at
2021-09-08

The observed CORT-induced increase in Cx43 phosphorylation at S368 may also contribute to GJIC disruption. Gap junction channel permeability is modulated through connexin phosphorylation (Moreno and Lau, 2007). Specifically, the phosphorylation of Cx43 on S368 has been previously shown to decrease i
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Some clinical reports have suggested that
2021-09-08

Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]
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The synthesis of compounds and were achieved
2021-09-08

The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanedi
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Studies on FXR knockout mice
2021-09-08

Studies on FXR knockout mice demonstrated that FXR activity is necessary to maintain a proper integrity of intestinal tight junction [18]. HF diet-induced bowel dysfunction impaired FXR activity and affected fecal BA profile. Generally, it augmented the concentration of secondary BAs in the colon e.
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Compound and several additional FPR antagonists identified h
2021-09-08

Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 ITE and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutrophils and tra
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Recently we indicated that cell motility was
2021-09-08

Recently, we indicated that cell motility was regulated by the different induction of GPR120 and GPR40 in liver epithelial WB-F344 Annexin V-Cy3 Apoptosis Kit Plus treated with chemical agents. The cell motility of WB-F344 cells was stimulated by phorbol ester 12-O-tetradecanoylphorbol-13-acetate (
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Neuropathic pain NP is a chronic pain caused
2021-09-07

Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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Migration chemotaxis and trafficking of leukocytes including
2021-09-07

Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial CPI-203 australia (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cells
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Here we show that Hippo
2021-09-07

Here, we show that Hippo signaling components are expressed during epicardium formation. To determine the significance of Yap and Taz in the developing epicardium, we generated epicardium-specific Yap/Taz double-knockout mice. Genetic deletion of Yap and Taz using Sema3d mice leads to embryonic leth
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