• The third generation cephalosporin antibiotics can cross the

  2021-12-06

  

  The third-generation cephalosporin Voreloxin Hydrochloride can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when taken

• LPCs have been previously described as potential anti

  2021-12-06

  

  LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al

• Genetic disruption or pharmacologic inhibition of the hepati

  2021-12-06

  

  Genetic disruption or pharmacologic inhibition of the hepatic glucagon pathway has invariably been shown to increase pancreatic α cell mass. This has been observed in glucagon receptor (GCGR) knockout (Gcgr−/−) mice (Gelling et al., 2003), glucagon knockout mice (Hayashi et al., 2009), prohormone co

• Introduction Glucose dependent insulinotropic polypeptide GI

  2021-12-06

  

  Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G

• br Introduction G protein coupled receptors GPCRs represent

  2021-12-06

  

  Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign

• br Acknowledgments The research leading to these

  2021-12-06

  

  Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/

• According to Laplace s law loss of myogenic

  2021-12-04

  

  According to Laplace’s law, loss of myogenic response would increase wall stress and tension in downstream vessels and subsequently induce endothelial dysfunction and arterial stiffness [36]. Indeed, we found that arteries from FPR-1 KO mice presented with a leftward shift in the stress-strain curve

• Acknowledgments br Introduction Stress plays a key role in t

  2021-12-04

  

  Acknowledgments Introduction Stress plays a key role in the etiology and/or exacerbation of major depressive disorder characterized by loss of energy, feelings of hopelessness and anhedonia [1]. Ample evidence clearly suggests that endocannabinoids (eCBs) participate in stress-associated neurona

• Taken together the four HRs couple with several different

  2021-12-04

  

  Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc

• br Concluding Remarks and Future Perspectives Our

  2021-12-04

  

  Concluding Remarks and Future Perspectives Our understanding of substrate targeting mechanisms utilized by kinases has grown tremendously in the past few years, but challenges still remain in relating these mechanisms to the organization of complex signaling networks. Substrate prediction based o

• Our last area of exploration was the piperidine core as

  2021-12-04

  

  Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th

• gap27 br Conclusion br Acknowledgment This study

  2021-12-03

  

  Conclusion Acknowledgment This study was supported by grants from the Excellence Initiative of the German federal and state governments, the Else Kröner-Fresenius Foundation and the German Society for Cardiology (DGK) to F.K. and grants from the Deutsche Forschungsgemeinschaft (SFB TRR 219 M-0

• Herein we describe the development of second generation GSM

  2021-12-03

  

  Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME

• In analyzed alleles in this

  2021-12-03

  

  In 3/11 analyzed ionophore in this study, the c.472C>T missense variant was detected. This variant was previously reported in Malaysian, French, Indian and Pakistani patients (Bhai et al., 2018; Ijaz et al., 2017; Lebigot et al., 2015; Moey et al., 2018; Ngu et al., 2014) who were homozygous and co

• As for all DOACs measurement of

  2021-12-03

  

  As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe

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