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The H R antagonist cimetidine Tagamet became the first billi
2022-05-24
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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The measured ROcc values and mg kg respectively
2022-05-24
The measured ROcc50 values (4.8 and 42 mg/kg, respectively) were lower than those estimated from the mouse free guanylyl cyclase concentrations (0.4 and 9.3 mg/kg for the sigma-1 and histamine H3 receptor, respectively) or rat CSF levels (0.65 and 4.5 mg/kg, respectively). This discrepancy is almos
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It is important to highlight that glucose dependent generati
2022-05-24
It is important to highlight that glucose-dependent generation of OMP of high magnitudes occurs due to the voltage-gating properties of VDACs, because only small magnitudes of OMP were obtained when the VDAC voltage sensitivity was zero (Fig. 5). These results indicate a possible physiological role
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br Acknowledgements This work was supported by
2022-05-24
Acknowledgements This work was supported by NIH HL111674 (JHF), and the Antoinette E. (“Mimi”) & Herman Boehm Foundation (JK). The authors wish to acknowledge the valuable assistance of the Functional Genomics Core of the University of Colorado, Denver. Introduction The 21-gene recurrence sco
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br Introduction Local anesthetics LAs
2022-05-24
Introduction Local anesthetics (LAs) are a set of common medicines used for pain management in clinical settings. Up to now, LAs have been extensively used for peripheral nerve blocks, interventional spinal procedures, and epidural anesthesia [1]. In addition to their anesthetic and analgesic ef
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Significan http www apexbt com media diy images wb
2022-05-24
Significant DNA damage was observed in hemolymph of molluscs exposed to raw composite tannery effluent as evident from comet assay images. DNA damage was evaluated by the presence of tail resembling that of comet in single strand DNA. Break in DNA strand was reported in the liver and gill Lestaurtin
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Ras pathways are involved in the regulation of virulence
2022-05-24
Ras pathways are involved in the regulation of virulence in Cryptococcus neoformans [7] and Candida albicans [8,9]. To verify the importance of Ras in the survival response of the fungus in the host, a pathogenicity test of P. brasiliensis was performed before and after treatment with the Ras inhibi
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Chronic exposure of cells to cytotoxic drugs can result in
2022-05-24
Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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It is interesting to note that the long
2022-05-24
It is interesting to note that the long and short forms of GPR120 exist at different basal levels of phosphorylation, with the short form demonstrating a greater degree of constitutive activity [12]. Importantly, Burns and Moniri [12] showed that, upon activation, the long and short isoforms of GPR1
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br Acknowledgments br Free fatty acids
2022-05-23
Acknowledgments Free fatty acids (FFAs) are not only essential nutritional components, but they also function as signaling molecules. Recently, a G protein-coupled receptor (GPCR) de-orphanizing strategy successfully identified multiple receptors for FFAs, which function on the cell surface and
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Injury to oligodendrocyte progenitors caused
2022-05-23
Injury to oligodendrocyte progenitors caused in part by glutamate contributes to the pathogenesis of myelination disturbances in PVL [5]. In the immature human brain, the susceptibility of developing oligodendrocytes to hypoxia-ischemia correlates with their expression of glutamate receptors of the
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Importance of glucokinase in glucose
2022-05-23
Importance of glucokinase in glucose homeostasis and a possibility to change its activity using the activators define the scientific interest in the development of new allosteric activators of GK (Liu et al., 2012, Pfefferkorn et al., 2011, Waring et al., 2013, Behera et al., 2015). Activation of gl
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Congenital Gcgr mice exhibit increased hepatic Fgf expressio
2022-05-23
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific buy serotonin receptor impairs glucose control in these mice [6]. In addition, the FGF21 analog L
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Whether or not SMO and SMO dependent HH signaling play
2022-05-23
Whether or not SMO and SMO-dependent HH signaling play a role in hematopoiesis is a subject of strong controversy. Obviously, the effects of SMO deletion are highly contextual and dependent on the timing of deletion. transplanted murine Smo−/− fetal liver aristocort synthesis into sublethally irra
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The structural modelling studies gave a
2022-05-23
The structural modelling studies gave a view of arsenic mediated covalent modifications possible in Cx43. In order to look for the biochemical effects of Arsenic on Cx43 and Cx43 mediated GJIC formation, and in order to further decipher the mechanism involved in Arsenic induced decreases in expressi
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