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br Development of calibrators and controls for DiXaIs
2022-08-19
Development of calibrators and controls for DiXaIs Method validation and comparison with reference technique (LC:MS) At this stage, anti-Factor Xa bioassays can be established for reliably measuring DiXaI concentrations in plasma, with the available appropriate drug specific calibrators and co
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br Conclusion We have demonstrated that ETB receptors negati
2022-08-19
Conclusion We have demonstrated that ETB receptors negatively regulate the expression of AT1 receptors in renal proximal tubule 98059 from WKY rats but not in SHRs. Short-term activation of the ETB receptor increases AT1 receptor phosphorylation in WKY cells but decreases it in SHR cells. We con
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Sometime ago we have described diamino triazines as
2022-08-19
Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by trans-AUCB and zymosan. In this work we describe new deri
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Aprotinin A second H R antagonist with
2022-08-19
A second H3R antagonist with benzamide-based structure from Johnson & Johnson is JNJ-31001074, known as Bavisant and under chemical IUPAC name of (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone. It is a compound with molecular weight 329.44, HBA four, and MLogP 1.52 encompass
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p-gp inhibitors Distribution of histamine receptors in the
2022-08-19
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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One of the possibilities of HO targeting is gene therapy
2022-08-19
One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing Deacetylase Inhibitor Cocktail but
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Based on pharmacophore modeling a good
2022-08-19
Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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br Hepatitis C virus HCV infection is a
2022-08-19
Hepatitis C virus (HCV) infection is a major cause of chronic liver disease that can lead to cirrhosis and hepatocellular carcinoma. It is estimated that nearly 200 million individuals worldwide are currently infected with HCV and it is the leading cause of liver transplants. The current standard
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Substitutions V L F V and Q
2022-08-19
Substitutions V36L, F43V and Q80H were identified in the present study. RAS V36L is associated with resistance to boceprevir [18]. In 2015, Brazilian clinical practice guidelines on the management of hepatitis C no longer included combined therapies with boceprevir or telaprevir as a treatment optio
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br Modulators of the GUCY C cGMP PDEs
2022-08-19
Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for
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Decreasing GSK activity has therapeutic benefits in animal m
2022-08-19
Decreasing GSK-3β activity has therapeutic benefits in animal model of colitis [45] and traumatic YM178 injury [46] and ischemia/reperfusion injury [47,48]. In brain, activation of GSK-3β promotes Aβ toxicity by elevating APP expression and its amyloidogenic cleavage, and by dysregulating Aβ clearan
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Much of the understanding of this system
2022-08-19
Much of the understanding of this system has come from several studies focussed on CB1. A significant amount of research has demonstrated that activation of the CB1 receptor by cannabinoid ligands stimulates food intake [10], reduces gastrointestinal motility [11], and increases lipogenesis [12] and
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br Declaration of interest br Acknowledgments br This work w
2022-08-19
Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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Fmoc-Phe-OPfp En el caso de la foliculitis
2022-08-19
En el caso de la foliculitis decalvante (FD), se ha publicado un estudio multicéntrico español de 82 pacientes en el que se concluye que el tratamiento que consigue una mayor efectividad (mejora en 15/15 pacientes tratados) y un mayor periodo de remisión postratamiento (7,2 meses) es la combinación
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There is sufficient evidence to indicate
2022-08-18
There is sufficient evidence to indicate that kisspeptin plays a role in regulating sheep reproduction. However, the molecular mechanism by which kisspeptin regulates GnRH Crystal Violet and reproduction has remained unclear. Therefore, in this study on GnRH in sheep, the promoter region of GnRH wa
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