• 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,

• 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

• 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

• 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

• 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

• 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

• SGCs tightly ensheath the soma

  2022-01-18

  

  SGCs tightly ensheath the soma of DRG neurons (Costa and Moreira, 2015, Hanani, 2005, Takeda et al., 2009). Intimate associations between SGCs and neurons facilitate bidirectional regulation of SGC function and neuronal excitability. After nerve injury, neuronal hyperexcitability can result in SGC a

• In parallel we were also preparing and

  2022-01-18

  

  In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora

• br Introduction Methylglyoxal MG is a highly reactive dicarb

  2022-01-18

  

  Introduction Methylglyoxal (MG) is a highly reactive dicarbonyl metabolite formed in cells mainly by the spontaneous degradation of triose phosphates, glyceraldehyde-3-phosphate, and dihydroxyacetone phosphate (Rabbani and Thornalley, 2012). It exists in a wide range of organisms, including proto

• Because sleep and metabolism are intimately linked the

  2022-01-18

  

  Because sleep and metabolism are intimately linked, the authors next move to study whether Eaat2 also controls metabolic rate. First, we must ask how sleep and metabolism are connected at a functional level. The 17 alpha hydroxylase allocation hypothesis of sleep posits that organisms temporally pa

• br Experimental br Results br

  2022-01-18

  

  Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,

• The Hedgehog Hh pathway is

  2022-01-18

  

  The Hedgehog (Hh) pathway is linked to the development of several types of epithelial cancers (Rubin and de Sauvage, 2006). A paracrine mechanism has been implicated in CAF activation, with Hh ligands secreted by cancer cells activating the glioma-associated transcription factors (Gli) in surroundin

• The caseins are a family of milk phosphoproteins whose

  2022-01-18

  

  The caseins are a family of milk phosphoproteins whose biological function is to provide supersaturating concentrations of calcium, phosphates, and essential fura 2 to the neonate (Vonderhaar and Ziska, 1989). α- and β-caseins, the most abundant of the milk caseins, are described as calcium sensiti

• br Introduction The growth hormone secretagogue receptor

  2022-01-18

  

  Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt

• br Involvement of gap junctions and Panx in spinal

  2022-01-18

  

  Involvement of gap junctions and Panx1 in spinal cord processing of pain information Several studies indicated that GJs in the CNS contribute to pain. A common finding in such studies is that intrathecal administration of GJ blocker attenuates pain behavior. For example, intrathecal CBX attenuate

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