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The pharmacokinetics of was obtained in mouse rat and
2022-03-22

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) indicat
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We also explored various nitrogen substituents with an aim t
2022-03-22

We also explored various nitrogen substituents with an aim toward modulating sterics and basicity within the ABH series. No glycine uptake inhibition was detected with non-basic bicycles (data not shown). Isopropyl was the best compromise between desired on-target effect and clearance, however, eff
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br Acknowledgment br Introduction Positive and negative rein
2022-03-22

Acknowledgment Introduction Positive and negative reinforcement are known as the two pivotal components in various models of drug dependence. Compulsive drug seeking behavior results from both the euphoric effects of drug use (positive reinforcement) and the unpleasant withdrawal signs followi
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br Dysregulation of glutamate transporter expression and fun
2022-03-22

Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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br Experimental br Results br Discussion The use of Dex
2022-03-22

Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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We found that silymarin induced more improvement of renal
2022-03-22

We found that silymarin induced more improvement of renal functions compared to Rvs. Our results were in agreement with previous studies. The effect of silymarin has been tested in alloxan-induced diabetes mellitus models in rats. Alloxan produces reactive oxygen species which injure renal tissue. S
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A frequent complication of SIRS and
2022-03-22

A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal Nelfinavir Mesylate mg [3] M
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br Materials and methods br Acknowledgments We are grateful
2022-03-22

Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research
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Phloretin All of the abovementioned effects of PUFAs signal
2022-03-22

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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br Acknowledgements The authors have no ethical conflicts to
2022-03-22

Acknowledgements The authors have no ethical conflicts to disclose. The authors have no conflicts of interest to declare. This work was funded by the Research Council of Lithuania. Introduction This paper studies whether there is a causal influence of the risk-taking incentives provided by op
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There are several basic science studies
2022-03-22

There are several basic science studies that aim to investigate potential mechanisms behind the reduced incidence of MI in factor Xa inhibitor treated patients. Perzborn et al. reported that in-vitro addition of rivaroxaban reduced tissue-factor induced platelet aggregation (Perzborn, Heitmeier, & L
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Treatment with histamine had no
2022-03-22

Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 GNF 2 sale (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo A-I promoter a
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In various models histamine has been
2022-03-22

In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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Arena Pharmaceutical introduced a biaryl sulfone derivative
2022-03-22

Arena Pharmaceutical introduced a biaryl sulfone derivative with antagonistic activity at H3Rs known as APD-916, ((R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine), which was rationally designed from corresponding sulfonamides in order to yield compounds with short dura
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Yap and Taz may regulate
2022-03-22

Yap and Taz may regulate epicardial cell proliferation, EMT, and fate determination via multiple mechanisms. In this study, we provide evidence that Yap/Taz function in part by directly modulating Tbx18 and Wt1 expression. Members of the T-box family of transcription factors regulate a variety of de
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