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Extracellular adenosine acts as a local modulator
2023-03-01
Extracellular adenosine acts as a local modulator of cell function via four adenosine receptor subtypes (A1Rs A2AR, A2BR, and A3R) that are involved in numerous physiological and pathophysiological processes [31]. Each is encoded by a separate gene and has different functions, although with some ove
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AMPK modulates changes in lipid metabolism
2023-03-01
AMPK modulates changes in lipid metabolism via the regulation of fatty fusidic acid oxidation and cholesterol synthesis in the liver. The key enzymes involved include ACC and HMGCR [27,28]. Both participate in the rate-limiting steps of fatty acids and cholesterol synthesis and are inactivated on p
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Despite these efforts to prevent oxidative
2023-03-01
Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of
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Epithelial mesenchymal transition EMT is
2023-03-01
Epithelial-mesenchymal transition (EMT) is the process by which epithelial cells are trans-differentiated into motile mesenchymal cells. During EMT, epithelial cells reorganize their cortical trans-AUCB cytoskeleton, lose their junctions and apical-basal polarity, change cell shape, and reprogram g
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Introduction Myasthenia gravis MG is
2023-03-01
Introduction Myasthenia gravis (MG) is an autoimmune disorder characterized by muscle weakness, which is mainly due to autoantibodies reducing the number or function of postsynaptic Telaprevir receptors (AChRs) [1], [2]. Animal models have been developed to uncover the immunopathogenesis of MG. Exp
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Several studies have recently used optogenetics to selective
2023-03-01
Several studies have recently used optogenetics to selectively activate various cholinergic neurons (Jiang et al., 2014). However, most do not explicitly report direct release of GABA from cholinergic fibers, with the exception of our two studies described above (Saunders et al., 2015a, Saunders et
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As we previously observed in the NSFT Fukumoto et
2023-03-01
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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As mentioned above variation of the A ring was undertaken
2023-03-01
As mentioned above, variation of the A-ring was undertaken in order to improve microsomal stability and kinase selectivity relative to NSC 66811 synthesis (). 1-Imidazole-2-carboxamides with substitution at the 4-position (–) were mostly tolerated with 4-cyano-imidazole-2-carboxamide () having comp
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The subnuclear localizations of redox regulators
2023-02-25
The subnuclear localizations of redox regulators is also largely unknown. The potential role of thiol reductases as transcription regulators or DNA repair molecules may suggest an association to DNA. In this way, the presence of a zinc finger domain potentially involved in protein/DNA interactions o
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br Conflicts of interest br Introduction When it comes to
2023-02-25
Conflicts of interest Introduction When it comes to risk taking, surgeons and anesthesiologists show greater risk taking than other physicians. Surgical procedures carry several risks of which infection is one. Surgical site infections (SSI) are the most common hospital acquired infection and
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br Conclusions Extract of non germinated winter rape seeds
2023-02-25
Conclusions Extract of non-germinated winter rape seeds cv. Bellevue was screened for the aminopeptidase activity. It revealed broad substrate specificity, with the highest activity toward Phe-pNA. Also in the partially purified sample, phenylalanine was preferentially hydrolysed. PMSF, known ser
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Altogether the situations described above clearly impede
2023-02-25
Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) hav
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An alternative to the agonist
2023-02-25
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Venlafaxine hydroxydopamine OHDA is a selective catecholamin
2023-02-25
6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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Candesartan Moreover showed reduction in fibroblast
2023-02-25
Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (PCandesartan have recently shown only moderate efficacy (40% inhibition
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