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Recently Bristol Myers Squibb and Merck reported their GPR a
2022-01-20
Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic YM 90709 derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists w
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Although pharmacological studies from the end of the th
2022-01-20
Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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br Anandamide signaling and cardiovascular function The card
2022-01-20
Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate
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br Acknowledgment br Introduction Non
2022-01-20
Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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Tyr phosphorylation of AnxA was first reported to be
2022-01-20
Tyr23 phosphorylation of AnxA2 was first reported to be involved in endocytosis, particularly in the internalisation of the insulin receptor [20]. Phosphorylated Tyr23 seems to be necessary for the stable association of AnxA2 with endosomes, and for their early-stage transport [14]. The role of AnxA
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Introduction Histone is the core component of chromatin and
2022-01-20
Introduction Histone is the core component of chromatin and histone modification is one of the key mechanisms of epigenetic regulation (Bannister and Kouzarides, 2011). Amino psora residues on histone tails can be modified under different mechanisms including acetylation, methylation, phosphorylat
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br Materials and methods br Results Aberrant A has
2022-01-19
Materials and methods Results Aberrant Aβ has been suggested to be an initiating factor for glutamate excitotoxicity in AD pathology. To investigate whether Aβ1-42 alters glutamate uptake in astrocytes, neurons, and astrocyte-neuron co-cultures, we used synthetic Aβ1-42 peptide. Aβ1-42 has fas
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Here we studied the effects of BZ flurazepam FZ at
2022-01-19
Here we studied the effects of BZ flurazepam (FZ) at high doses in acute and chronic settings of tolerance and dependence in GluR-A−/− mice (Zamanillo et al., 1999). We used measurements in which the phenomenon of “learning while intoxicated” should play only a minor role in order to find out the si
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The NVC response in the
2022-01-19
The NVC response in the diseased or aging Exo1 may be altered, including changes in both the chemical mediators of NVC, ion channel behaviour, and the dynamics of the vascular system. For example, in Alzheimer’s disease the production of NO is shown to be inhibited (Lourenço et al., 2014), hyperten
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Our own search towards aryl imidazole derived GSMs
2022-01-19
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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The present in vitro experiments confirm previous
2022-01-19
The present in vitro experiments confirm previous suppositions (Ciosek, Gałecka, 2011, Izdebska, Ciosek, 2010) that Gal modulates AVP and OT release by acting at every level of the hypothalamo-neurohypophysial system. In fact, both 10−10 M and 10−8 M Gal diminished basal release of AVP and OT from t
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5402 br Material and methods br Results br Discussion Propof
2022-01-19
Material and methods Results Discussion Propofol is commonly used in operation rooms or intensive care units (ICUs) for critically ill patients. Various clinical trials have demonstrated that the antioxidant, anti-inflammatory, and free-radical-scavenging properties of propofol can provide
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br Conclusions Our in vitro and in vivo data
2022-01-19
Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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The effect of combined A and PD treatment on the
2022-01-19
The effect of combined A-192621 and PD 155080 treatment on the Z-YVAD-FMK during endotoxin infusion is quite different compared to either drug used alone (Wanecek et al., 1999). After administration of both antagonists in combination, cardiac index increased to baseline values within 30 min, and wa
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br Introduction Ovarian cancer patients have the highest mor
2022-01-19
Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is flavin adenine dinucleotide with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone meth
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