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Further evidence for action mechanism was provided by
2024-08-16
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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We have previously shown that the
2024-08-16
We have previously shown that the human gonadotropins hLH and hCG trigger a partly irreversible stimulation of intracellular cyclic AMP accumulation in mouse Leydig Tumor Nicotinamide (MLTC) in contrast to all other tested mammalian LHs and CG (Klett et al., 2016). In order to get a better insight
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Very recently Niessen et al have
2024-08-16
Very recently, Niessen et al. have described the resensitizing effect of MB327 on nAChR performing solid-supported membrane (SSM)-based electrophysiological experiments (Niessen et al., 2016) using plasma membrane preparations obtained from Torpedo californica. These findings validated and underlin
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It has been reported that HT R
2024-08-16
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and
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Ro 08-2750 australia Several mechanisms have been suggested
2024-08-15
Several mechanisms have been suggested to account for the causal association of ICAM-1 induction and leukocyte adhesion with DR, including oxidative stress [16], NF-κB [17], PKC [18], and bioactive lipids [19]. Our previous studies highlighted the role of bioactive lipid metabolites derived from 12/
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Two critical determinants of receptor
2024-08-15
Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al
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Therefore the rational design of target compounds is
2024-08-15
Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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Introduction Antimicrobial resistance is a growing health th
2024-08-15
Introduction Antimicrobial resistance is a growing health threat worldwide that has been associated with incorrect prescription and overuse of prostaglandin agonist synthesis [1]. Considering that physicians play a central role in antibiotic usage, a better understanding of their prescribing behav
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The electrokinetic remediation technique is carried
2024-08-15
The electrokinetic remediation technique is carried out with a low-level direct current, and the pollutants in soil can be transported and removed by the electric field [19]. This works well even in soil with low permeability via electro-osmotic flow and electro-migration [20]. The electrokinetic pr
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AMPK is a cellular energy sensor
2024-08-15
AMPK is a cellular energy sensor that is phosphorylated in response to high intracellular ADP levels to increase GLUT4 translocation into the cell, and subsequently, increase intracellular glucose levels to provide substrate to replenish ATP levels [25]. In metabolic syndrome, sequestration of plasm
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aphidicolin Based upon these findings the S
2024-08-15
Based upon these findings, the 12S-lipoxygenase seems to increase membrane excitability by specifically inhibiting M-type K+ channels. The 12S-lipoxygenase is expressed in many parts of mammalian aphidicolin including the cerebrum, cerebellum, hypothalamus, basal ganglia, hippocampus, olfactory bul
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Inflammatory factors released by activated cells during
2024-08-15
Inflammatory factors released by activated cells during AD are very important for the disease progression. Not only several inflammatory cytokines, such as IL-1β, IL-18, and IL-33, but also anti-inflammatory ones, as IL-10 and IL-13, are upregulated in the brain of AD patients (Morimoto et al., 2011
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In the presence of detrimental conditions such as inflammati
2024-08-14
In the presence of detrimental conditions, such as inflammation, hypoxia, ischemia trauma or neoplastic milieu, the extracellular levels of adenosine increase massively, reaching micromolar range [51,52]. In these pathological contexts, adenosine accumulation stems from increased extracellular depho
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fusidic acid The theoretical calculations of ADME
2024-08-14
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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The first rationally designed dual mPGES
2024-08-14
The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic Hexa His tag - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synth
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