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As a continuation of our
2024-08-12
As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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The present in vitro pharmacological experiments
2024-08-12
The present in vitro pharmacological experiments revealed that the cholinergic up-regulation of VEGF expression in neurons and astrocytes was mainly mediated by nicotinic AChR and muscarinic AChR, respectively. In addition, neuronal VEGF expression was elevated by endogenous ACh in a manner that was
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Conclusion Twenty compounds with dinitrobenzoate
2024-08-12
Conclusion Twenty compounds with 3,5-dinitrobenzoate scaffold were synthesized and evaluated using cell-free and HWB assays for their 5-LOX inhibition activities. Compared to the parent compound, six compounds show significantly increased enzyme inhibition activities. The best compound, 3-tolyl 3,5
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Direct inhibition of LO activity
2024-08-12
Direct inhibition of 5-LO activity by BRP-187 is clearly evident in cell-free assays using PMNL homogenates and isolated human recombinant 5-LO as enzyme source. In such assays, pure FLAP inhibitors like MK886 are inactive [9], [10], [29], [44]. Wash-out experiments and studies using the nonionic de
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The present work has implications for our thinking
2024-08-12
The present work has implications for our thinking about the effects of antidepressant (e.g. SSRIs) use on maternal care in depressed mothers which consist of approximately 10–20% of all mothers (Gjerdingen and Yawn, 2007, Susser et al., 2016), and more than 40% of depressed mothers are prescribed w
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The mechanism by which Gas prevents inflammation has been re
2024-08-12
The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I
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br Introduction Stroke is a devastating
2024-08-12
Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti
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Stroke also known as a cerebrovascular accident or brain
2024-08-12
Stroke, also known as a cerebrovascular accident or L-Cysteinesulfinic acid sale attack, is one of the leading causes of death and disability worldwide (Haley et al., 2017; Hankey, 2017; Lie et al., 2017). According to the data released by the World Health Organization (WHO), stroke occurs every 5
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We have recently reported a regulatory effect
2024-08-09
We have recently reported a regulatory effect of quercetin on the AChE activity in the brainstem during the demyelination and remyelination process [17]. It has also been observed that there is a protective effect on lipid peroxidation and worsening of motor functions caused by loss of myelin in the
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Earlier studies showed that exposure of cells to IR
2024-08-09
Earlier studies showed that exposure of cells to IR caused ATM-dependent phosphorylation of 53BP1, as judged by electrophoretic mobility shift [24], [25], [26]. To date, the only known in vivo 53BP1 phosphorylation site(s) are Ser25 and possibly Ser29 [27]. In the course of our studies, we noticed t
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Why do glutamate and glycine bind to the
2024-08-09
Why do glutamate and glycine bind to the Macitentan in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lobes
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Apelin is a peptide hormone and an endogenous ligand
2024-08-09
Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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br Materials and methods br Results and
2024-08-09
Materials and methods Results and discussion Conclusion Funding This work was supported by the Canadian Institute of Health Research (CIHR) [grant number FDN-148413] to PS, the National Science and Engineering Research Council of Canada (NSERC) [grant number CRD-399680] to ÉM, and the FR
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br Experimental section br Acknowledgment S
2024-08-09
Experimental section Acknowledgment S.B.T. is grateful to the Deutsche Forschungsgemeinschaft (DFG), the Wilhelm Sander-Stiftung and Interdisciplinary Center for Molecular Materials (ICMM) for generous research support. M.M. greatly acknowledges the experimental support and the scientific cont
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br Antifungal resistance what is
2024-08-09
Antifungal resistance, what is in a name? Antifungal resistance is an emerging and hot topic in the field of medical mycology. Microbiological resistance is identified by determining minimal inhibitory concentrations (MICs) in vitro for a given antifungal and interpreting this value according to
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