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Continuing studies of endocannabinoid ligands
2022-05-27

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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br Materials and methods br Results and discussion
2022-05-26

Materials and methods Results and discussion Conflict of interest Introduction In the presence of continuous and excessive levels of nutrients, adipocytes become hypertrophic and release several pro-inflammatory adipocytokines such as interleukin-6 (IL-6), monocyte chemoattractant protei
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A number of synthetic GPR
2022-05-26

A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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br Material and methods br Results br Discussion Organisms
2022-05-26

Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In α-Naphthoflavone to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver [19]. T
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The unique ability of R PabI
2022-05-26

The unique ability of R.PabI to specifically excise DL-Menthol from a palindromic sequence is based on a novel structural architecture that is distinct not only from other DNA glycosylases but also from other proteins [88]. In the absence of DNA, R.PabI forms a dimer with a central, highly twisted
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Based on our finding that
2022-05-26

Based on our finding that TFA modulates GlyR function and reports that TFA-bound Caspase Inhibitor Set I synthesis can differ markedly from those synthesized without TFA, we retested a previously published dodecapeptide (D12-116) that also enhanced GlyR function but this time as a chloride salt (Tip
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br Materials and methods br
2022-05-26

Materials and methods Results Discussion Quercetin is a relatively abundant bioactive flavonoid with a wide variety of documented physiological effects, which has gained popularity as a nutritional supplement [40]. There is increasing interest in quercetin's anticancer properties (for recen
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Another consistent observation in our
2022-05-26

Another consistent observation in our studies was the lower plasma catecholamine concentrations in the exercised GHSR-null mice, suggesting a diminished sympathoadrenal response. A proper sympathoadrenal response is essential for increasing substrate utilization during exercise [81]. Thus, the reduc
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GHSR A s have high levels
2022-05-26

GHSR-1A's have high levels of constitutive activity and recent investigations show that constitutively active GHSR-1As in the absence of ligand (ghrelin) binding can have effects on feeding and energy balance (Mear et al., 2013, Petersen et al., 2009). Furthermore, GHSR-1As are capable of dimerizing
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The first GSM was identified from the
2022-05-26

The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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A way to identify what subunit
2022-05-26

A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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The GABA A receptors containing
2022-05-26

The GABA-A receptors containing the δ subunit are crucial for the mediation of non-synaptic inhibition in the dentate gyrus; thus, the decreased expression of the δ subunit may suggest a decrease in the inhibitory tone and an increase in the neuronal excitability. Moreover, the GABA-A receptors cont
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br Acknowledgements Research was funded by the Natural Scien
2022-05-26

Acknowledgements Research was funded by the Natural Sciences and Engineering Council of Canada (NSERC) (Grant #210290) SGF. The funding body played no role in the design or execution of the study. The authors declare no conflict of interest. Introduction HBO2 therapy is the use of 100% oxygen
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Knock out mice of FXR
2022-05-26

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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Stimulation of FPR by bacterial N formyl peptides
2022-05-26

Stimulation of FPR by bacterial N-formyl peptides induces basophil and mast ion channels release of immunogenic compounds such as histamine [21], [31]. Furthermore, we demonstrated that histamine plays a role in F-MITs-induced sepsis-like symptoms since cimetidine, a histamine H2-receptor antagonis
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