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The effects of opioids such as morphine
2022-09-22
The effects of opioids such as morphine are mediated through the opioid receptors. Opioid receptors are widely expressed both peripherally and in the CNS (Chen et al., 1993, Evans et al., 1992). The opioid agonist morphine has been shown to amplify the effect of the tubular cell-gp120 interaction on
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Among the compounds prepared at this
2022-09-22
Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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br RNA preparation cDNA synthesis and RT PCR Trizol
2022-09-22
RNA preparation, cDNA synthesis and RT-PCR Trizol reagent (Invitrogen, Carlsbad, CA, USA) was used to extract total RNA from tissues according to the manufacturer’s protocol and isolated RNA quantity was determined by UV spectrophotometry (Nanodrop, Thermo Scientific, USA) and RNA integrity was v
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In conclusion we have shown that
2022-09-21
In conclusion, we have shown that AKR1D1 regulates glucocorticoid availability and GR activation and therefore represents a key pre-receptor regulator of hormonal action in human liver. However, there are additional questions that need to be addressed including dissecting the broader role of AKR1D1
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The presented results speak for the direct effects
2022-09-21
The presented results speak for the direct effects of ghrelin on rat spermatozoa, which are accomplished by the activation of the GHSR-1a receptor. Thus, the results seem to be of physiological significance in vivo since ghrelin, the natural ligand of GHSR-1a, was found to be present in the seminal
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A model substance often used in the
2022-09-21
A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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Neovascularization upon IMQ treatment was observed to differ
2022-09-21
Neovascularization upon IMQ treatment was observed to different degrees in WT and GAL3-KO mice, whereas the increase in vascular endothelial growth factor mRNA levels was genotype independent. Because we observed lower levels of the cytokines IL-17A, IL-22, IL-23, and TNF-α in IMQ-treated skin of GA
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FFAs concentration response curves for increasing intracellu
2022-09-21
FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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bromophenol blue receptor In this study it was demonstrated
2022-09-21
In this study it was demonstrated that also in mice chronically exposed to CS, lung inflammation persists after SC and is associated with a progressive alveolar loss and remodeling of respiratory tract, characterized by the onset of bronchial and bronchiolar GCM and peribronchiolar fibrosis. Persist
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Piroxicam belongs to the oxicam family of
2022-09-21
Piroxicam belongs to the oxicam family of NSAIDs and a special attention has been drawn to this drug because of its multifunctional potential [5], [27], [28]. Chemically, piroxicam (4-hydroxy-2-methyl-N-2-pyrimidyl-2H-1,2-benzothiazine-3-carboxyamide) is an enolic M 1145 australia with a size compar
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Compound and several additional FPR antagonists identified
2022-09-21
Compound 10 and several additional FPR1 antagonists identified here specifically blocked fMLF-induced responses mediated via FPR1 in FPR1-HL60 EHT 1864 and human neutrophils, but not responses mediated via FPR2 or FPR3 (in human neutrophils and transfected HL60 cells) or Fpr1 (murine neutrophils and
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PK profiles of were evaluated
2022-09-21
PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 cell
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The site of paracetamol action remains
2022-09-21
The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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Here we employ a genetic approach to
2022-09-21
Here we employ a genetic approach to examine the potential interaction of Gli3 and Ezh2 with respect to anteroposterior limb bud polarity. Loss of Ezh2 in a Gli3 mutant background leads to synergistic loss of anterior identity, although the double mutant phenotype more closely resembles that of Ezh2
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A number of studies have reported
2022-09-20
A number of studies have reported that lncRNA may function as sponge to interact with miRNAs at posttranscriptional level, thereby regulating miRNA targeted genes (Tang et al., 2015, Han et al., 2015). For example, lncRNA Malat1 induces autophagy by regulating ULK2 via sponging miR-26b (Li et al., 2
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