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H together with T also forms a binding
2021-11-29

H109, together with T112, also forms a binding site for H+ (Chen et al., 2004; Harvey et al., 1999). H+-binding at this site also inhibits GlyR-mediated currents. Notably, the vicinity of neurons experiences changes in pH, to a mild extent in physiological conditions such as when neurons fire (Chesl
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Benidipine HCl Previous reports have showed that the express
2021-11-26

Previous reports have showed that the expression and localization of GLUT8 in mouse (Gómez et al., 2006; Kim and Moley, 2007), rat (Ibberson et al., 2002) and human (Schürmann et al., 2002). In this study, GLUT8 protein mainly localized in the spermatocytes, elongated and round spermatids in the adu
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To identify inhibitors of the Hh GLI signaling pathway from
2021-11-26

To identify inhibitors of the Hh/GLI signaling pathway from natural resources, we have recently reported the successful construction of a cell-based screening assay system for the Hh/GLI signaling pathway (Fig. 1). This is an assay using a GLI-dependent luciferase reporter in human keratinocyte cell
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racecadotril br Introduction The growth hormone secretagogue
2021-11-26

Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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The objective of this study is to
2021-11-26

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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br Acknowledgements br Introduction Muscle FBPase is
2021-11-26

Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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br Introduction Atrial fibrillation is the
2021-11-26

Introduction Atrial fibrillation is the most common cardiac arrhythmia (Benjamin et al., 1998). Pulmonary vein (PV) sleeves contain a mixture of working myocardium and potential arrhythmogenic pacemaker O6-Benzylguanine receptor behaving as an ectopic trigger of atrial fibrillation (Haissaguerre
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We notice that previous reports of arsenic exposure
2021-11-26

We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 AG-1024 increased H3K9ac after 24 h, when analyzed by methods of immunofluorescence and Weste
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A second H R antagonist
2021-11-26

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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YM 155 In order to determine which complex of
2021-11-26

In order to determine which complex of the electron transport chain is targeted by Authipyrin, a semi-intact assay was performed. The substrates of each complex were added separately in combination with Authipyrin or the respective control inhibitor. Seahorse XF plasma membrane permeabilizer (PMP) w
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br All platelet agonists acting through specific receptors
2021-11-26

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) o
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br Materials and methods br Results
2021-11-26

Materials and methods Results Discussion Main results obtained in this work are presented in Table 1 and can be summarized as follows: 1) AEA inhibits FcεRI receptor-induced degranulation with the participation of CB2 and GPR55 receptors by a PTX-insensitive mechanism; 2) AEA does not block
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br GPR is a class A GPCR
2021-11-26

GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine Gefitinib which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell si
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br Introduction High dose niacin or nicotinic
2021-11-26

Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic palovarotene form of niacin modulates plasma lipid profiles including decreasing cir
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br Discussion According to the generally
2021-11-25

Discussion According to the generally accepted notion which originated from the study of ATP-depleted Caspase-6 Fluorometric Assay Kit the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and the s
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