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Molecular properties as well as metabolic stability
2022-01-20

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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br Acknowledgments This work was supported by the
2022-01-20

Acknowledgments This work was supported by the Slovak grant agency VEGA, Grant 2/0084/13. We would like to thank Dr. J. Bauer for careful reading of the manuscript. Introduction Glycine is an important neurotransmitter which regulates both Pancuronium dibromide inhibitory neurotransmission an
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br Experimental section br Acknowledgments MIN cells
2022-01-20

Experimental section Acknowledgments MIN6 G-1 were kindly provided by Dr. Junichi Miyazaki, Osaka University. This research was supported in part by the Ministry of Education, Culture, Sports, Science and Technology of Japan (JP16H05099 and JP18H04609 to K.H., and JP16H06574 to T.U.), SENTAN,
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br Experimental br Acknowledgments This project was
2022-01-20

Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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At present many methods have been applied for
2022-01-20

At present, many methods have been applied for multiple detection. For example, AT7519 Hydrochloride [[9], [10], [11]] is frequently used to detect multiple targets because of its exquisite sensitivity and specificity, but it is difficult to design experiments to test short-length oligonucleotides.
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br Materials and methods Patients charts were reviewed retro
2022-01-20

Materials and methods Patients’ charts were reviewed retrospectively, and 165 consecutive patients (82 with cancer and 83 without cancer) who either started edoxaban (Lixiana®, Daiichi-Sankyo, Tokyo, Japan) therapy for the treatment of VTE or were switched from other oral anticoagulants to edoxab
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summarizes FAAH inhibition data for a series of
2022-01-20

summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibition
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We examined the expression of notch in
2022-01-20

We examined the expression of notch-1 in the brains of mice following morphine or oxycodone tolerance. The results showed that notch-1 levels did not change following morphine or oxycodone tolerance, with or without the treatment of IRL-1620. This indicates the possibility that morphine or oxycodone
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Apoptosis is one of critical
2022-01-20

Apoptosis is one of critical toxic mechanisms of benzene metabolites. In this work, overexpression of HIF-1a could significantly reduce the increase in cell apoptosis caused by 40 μM BQ. At the meanwhile, anti-apoptotic protein Bcl-2 level was significantly elevated in HIF-1a overexpression cells th
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STAR Methods br Acknowledgments We thank C Hong R
2022-01-20

STAR★Methods Acknowledgments We thank C. Hong, R. Huang, and Z. Yu at the HHMI Janelia cryo-EM facility for help with microscope operation and data collection. We thank A. Müller, W. Kan, and W. Weis for help with the SEC-MALS analysis and M. Elazar and J. Glenn for the use of equipment. P. Love
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br Methods br Results br Discussion The
2022-01-19

Methods Results Discussion The aim of this study was to investigate whether serum lectin-binding activity is associated with development of HCC in HCV-positive individuals. Using ELISA-based assays of lectin-binding activity, we demonstrated that both age and gender influence the circulatin
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The first hypothesis better fertility in heifers that had
2022-01-19

The first hypothesis, better fertility in heifers that had CL at day 0, was clearly supported by our results. Heifers with a CL had over 60% P/AI compared to ∼50% in heifers without CL. These results are consistent with several other studies reporting that cycling heifers have greater fertility than
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Due to the high structural similarity
2022-01-19

Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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In this study we find that DH CBD induces analgesic
2022-01-19

In this study, we find that DH-CBD induces analgesic effects on inflammatory but not acute pain and the SL 0101-1 level of spinal α1 GlyRs increased after CFA paw injection. These results suggest that GlyR α1 is only involved in chronic pain. A possible explanation is that once the expression of α
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tiger br Results and discussion br Conclusion In conclusion
2022-01-19

Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thio
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