• LEE011 synthesis Acute in vivo experiments were performed

  2022-01-24

  

  Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding LEE011 synthesis control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 10mg/kg pr

• br Niacin has long been used

  2022-01-24

  

  Niacin () () has long been used for the treatment of lipid disorders and for the prevention of cardiovascular disease, the leading cause of death in the U.S., as a result of its ability to raise high-density lipoprotein (HDL) levels. Recent mechanistic investigations have shown that niacin may exe

• Our exploration of Domain focused on the role of

  2022-01-21

  

  Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be replaced

• In order to ensure that the decrease in

  2022-01-21

  

  In order to ensure that the decrease in ethanol and morphine intake was not due to a sedative effect of SNAP 37889, locomotor activity and motor learning were assessed through behavioural paradigms. Using the locomotor test, SNAP 37889 did not alter any parameters of locomotion; this lack of sedatio

• Interestingly the subcellular localization of FBPase in hepa

  2022-01-21

  

  Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Remoxipride hydrochloride reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our resu

• Occupying at least of brain

  2022-01-21

  

  Occupying at least 50% of Afatinib dimaleate volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of syna

• br Conclusions and perspectives br

  2022-01-21

  

  Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025

• The current study identified the presence and location

  2022-01-21

  

  The current study identified the presence and location of all four histamine receptors in the GI tract of 6 healthy adult dogs. Although no clinical signs of GI disease were noted, mild inflammation was noted in at least one section of the GI tract in all dogs based on WSAVA guidelines. Interpretati

• All the compounds and were

  2022-01-21

  

  All the compounds –, , , –, , – and – were assayed for their potential cytotoxicity at a single dose of 10 µM on Huh7 cells. Interestingly, all compounds proved to be non toxic, with the exception of and which exhibited high cellular toxicity and therefore were excluded from further experiments (a).

• Over the last years numerous studies gave insights into

  2022-01-21

  

  Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137

• The combination of niacin with a selective PGD receptor

  2022-01-20

  

  The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su

• For molecules with potential for therapeutic use high

  2022-01-20

  

  For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low

• br Conclusion These are exciting times

  2022-01-20

  

  Conclusion These are exciting times in EAAT research. The discovery and use of the GltPh and GltTk transporters as model systems for EAATs has provided detailed understanding of structure–function aspects of the transporters. Moreover, recent studies into the physiological functions of the transp

• To examine the possible role

  2022-01-20

  

  To examine the possible role of mGluRs in the LH/PFA in the hypercapnic ventilatory response, a nonspecific antagonist of mGluRs, MCPG, was microinjected into the LH/PFA. MCPG elicited a significantly increased hypercapnic ventilatory response in awake rats, but not during sleep, in the light and da

• br Introduction Hepatocyte injury initiates and facilitates

  2022-01-20

  

  Introduction Hepatocyte injury initiates and facilitates inflammation in the course of liver disease progression. Thus, understanding the regulatory basis for sensing and responding to damage-associated inflammatory processes in the liver’s parenchymal cells is a primary issue in liver pathophysi

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