• Another small compound targeting IBAT has

  2022-01-26

  

  Another small compound targeting IBAT has been evaluated in Phase I clinical trial (EudraCT 2013-001175-21) [86]. The oral administration of A4250 to healthy subjects did not give rise to any serious adverse events, was well tolerated and had a similar safety profile as elobixibat; however, it cause

• Compounds were tested for GPR activity in a functional

  2022-01-26

  

  Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO kd025 transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity relat

• Tail group SAR of the imidazole derived analogs

  2022-01-26

  

  Tail group SAR of the imidazole derived analogs is shown in . The previous SAR study from the discovery of AMG 837 revealed that a simple un-substituted meta-biphenyl tail group was less favorable in terms of potency. Efforts to introduce polarity to the tail group were not successful. When a methyl

• br Introduction Adenosine triphosphate ATP is an organic

  2022-01-26

  

  Introduction Adenosine-5′-triphosphate (ATP) is an organic molecule (nucleoside triphosphate) which consists of adenine, ribose, and three phosphoric SB273005 residues. ATP serves as a temporary carrier of energy in all living cells, so it is a common substance in any organism. In the cells, new

• Overall this study provides compelling evidence that overexp

  2022-01-26

  

  Overall, this study provides compelling evidence that overexpression of catalase coupled with an enriched diet of OM3 fatty acids are metabolically beneficial. This combination was shown to increase adipose tissue expression of the GPR120/FFAR4, which by interacting with the Nrf2 pathway, resulted i

• In summary through medicinal chemistry design and

  2022-01-26

  

  In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on

• Historically a role for the prefrontal cortex

  2022-01-25

  

  Historically, a role for the prefrontal cortex in spatial working memory has been repeatedly claimed (for review, see Kolb, 1984). Older studies using traditional, non-fibre-sparing lesions (e.g. aspiration lesions) often resulted in spatial alternation deficits. In contrast, more recent studies emp

• GK allosteric activators validate the importance of GK from

  2022-01-25

  

  GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many

• A frequent complication of SIRS and sepsis

  2022-01-25

  

  A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal A-1210477 [3] Moreover, it

• Nitrocefin The central event eliciting insulin secretion is

  2022-01-25

  

  The central event eliciting insulin secretion is the production of ATP which leads to the inhibition of ATP-sensitive inwardly-rectifying K+ATP channels, a consecutive depolarization of the plasma membrane with opening of voltage-dependent Ca2+ channels and Ca2+ influx into the beta-cell. However, i

• br Conclusions Our in vitro and in

  2022-01-25

  

  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

• Production of reactive oxygen species ROS at the site

  2022-01-25

  

  Production of reactive oxygen species (ROS) at the site of pathogen attack following recognition of pathogen-associated molecular patterns (PAMPs) is regarded as one of the initial plant immune responses. ROS accumulation can induce a hypersensitive reaction in host plants, thereby causing programme

• In conclusions it is hypothesized that

  2022-01-25

  

  In conclusions, it is hypothesized that caffeine administration could lead to an increase in histamine neuronal activation or release of histamine [38] to induced locomotor stimulation via H1 receptor activation. In addition, the present study also propose that the spaced administration of caffeine

• Acknowledgement This work was supported by

  2022-01-25

  

  Acknowledgement This work was supported by grants from the National Natural Science Foundation of China (No.81802749), Shenzhen Healthcare Research Project (No.SZBC2017029), the Science and Technology Foundation of Shenzhen (JCYJ20170412155231633, JSGG20170414104216477), National Key Research and D

• There is increased awareness of HBV reactivation in

  2022-01-25

  

  There is increased awareness of HBV reactivation in chronic HCV/HBV co-infected patients treated with DAAs [1], [2]. The recent emergence of this adverse event of DAA therapy is due to the exclusion of HBV co-infected subjects from registration clinical trials evaluating the safety of these treatmen

15850 records 491/1057 page Previous Next First page 上5页 491492493494495 下5页 Last page