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We have expanded these studies by doing EEG recording
2022-05-16

We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA Senexin A or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist
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Additionally to their peripheral effects
2022-05-16

Additionally to their peripheral effects, evidence indicate a role for ETs in the central nervous system (Mosqueda-Garcı́a et al., 1993). Indeed, using Northern blot analysis and in situ hybridization it has been shown the presence of immunoreactive ET of non-vascular origin and of neuronal location
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Distribution of histamine receptors in the
2022-05-16

Distribution of histamine receptors in the intestines varies among species, but our findings are similar to those previously reported in humans and guinea pigs (Thurmond, 2010, Thurmond, 2015). H1 receptors were located mainly in the gastric mucosa, smooth muscle, and lymphoid tissue, corresponding
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br Conflicts of interest br Significance p
2022-05-16

Conflicts of interest Significance p53 is required for the induction of cell senescence to limit the proliferation of polyploid cells. We found that Hippo signal deficiency or Yap activation in mouse livers result in polyploid formation and polyploid cell growth. The combined loss of Hippo sig
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ICG-001 In this study we present the first data on the
2022-05-16

In this study, we present the first data on the kinetic properties of the hexokinase of T. equiperdum, which we compare with similar data available for pleomorphic T. brucei (Seed and Baquero, 1965, Nwagwu and Opperdoes, 1982, Hara et al., 1997, Morris et al., 2006, Chambers et al., 2008b, Chambers
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The overall response rate to afatinib is comparable to a
2022-05-16

The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an
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br Patients and methods br Results
2022-05-13

Patients and methods Results Discussion The positivity of serum anti-HBc is the most commonly used marker to confirm the history of HBV infection. Quantification of serum anti-HBc has been explored as a marker of HBV-induced hepatitis and the adaptive immune response against HBV infection a
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br Mutagenesis and Receptor Modeling Studies br Signal Trans
2022-05-13

Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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Lactate as administered in these models is
2022-05-13

Lactate as administered in these models is metabolized rapidly and it appears that transient engagement of GPR81 with lactate serum concentrations in the range of moderate exercise physiology, as measured here at 3–4 mmol/L, are sufficient to suppress tissue macrophage NF-κB activation in our models
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The GPR gene was included in our survey because of
2022-05-13

The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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br Experimental br Acknowledgments This research was
2022-05-13

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa
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In summary through medicinal chemistry
2022-05-13

In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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Similar to GPR A activation of G protein coupled
2022-05-13

Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic Rifabutin australia receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al.,
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Myosmine mg It is essential to maintain
2022-05-13

It is essential to maintain genome integrity and stability which is assaulted by oxidative stress. To perform this function, all human cells have well developed repair systems. Base excision repair (BER) system is the most effective pathway responsible to revert back lesions caused by oxidative stre
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The ion conduction pathway reported herein accounts for all
2022-05-13

The ion conduction pathway reported herein accounts for all known functional properties of EAAT/GltPh anion channels. Simulations reveal unitary current amplitudes and ion selectivities (Figures 3C and 3D) that resemble experimental results (Melzer et al., 2003, Wadiche and Kavanaugh, 1998). The cal
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