• The only approved H R antagonist inverse

  2022-04-09

  

  The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or

• br Conflict of interest br Acknowledgements This

  2022-04-09

  

  Conflict of interest Acknowledgements This work was funded by the University of Turin (ex60% 2014), World Wide Style Project (WWS; University of Turin/Fondazione CRT) and University of Florence (ex60% 2014). ACR and AP designed the study; AP, EB and IO conducted the literature search and analy

• Molecular modeling studies also revealed insignificant diffe

  2022-04-08

  

  Molecular modeling studies also revealed insignificant differences in ligand-receptor interaction energies between R and S enantiomers of LPCs or their 2-OMe-analogues, suggesting that enantiomers of a particular structure should exert similar GPR119-mediated biological effect. Indeed, when studied

• br Experimental procedure br Acknowledgments This research w

  2022-04-08

  

  Experimental procedure Acknowledgments This research was supported by funds provided by NIH/NIAAA grant P01 AA020683 and the Waggoner Center for Alcohol and Addiction Research. Introduction Acute mesenteric ischemia (AMI) is still associated with a high mortality rate, and currently, an ea

• marbofloxacin Hippo signaling is an emerging tumor suppresso

  2022-04-08

  

  Hippo signaling is an emerging tumor suppressor pathway that plays key roles in normal physiology and tumorigenesis through the regulation of cellular proliferation and survival [4]. In humans, YAP is over-expressed as a result of genomic amplification of the 11q22 locus in a wide spectrum of human

• Further explorations at the ortho and meta positions of the

  2022-04-08

  

  Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp

• br Results and discussion A

  2022-04-08

  

  Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo

• BIX 02189 Introduction Glucose is the most important energy

  2022-04-08

  

  Introduction Glucose is the most important energy carrier of the brain. Glucose transporter type 1 (Glut1) is located at the blood–brain barrier and assures the energy-independent, facilitative transport of glucose into the brain [1]. Twelve transmembrane segments of the protein and an intracellula

• br WM astrocytes Grey matter astrocytes express a variety of

  2022-04-08

  

  WM astrocytes Grey matter astrocytes express a variety of GluR types that have both physiological and pathophysiological significance [87]. Non-NMDA GluR are also expressed in WM astrocytes [40], although the functionality of these receptors has not been tested. The fibrous astrocytes that popula

• Bacterial GluRS comes in two flavors discriminatory GluRS D

  2022-04-08

  

  Bacterial GluRS comes in two flavors, discriminatory GluRS (D-GluRS) and non-discriminatory GluRS (ND-GluRS). While D-GluRS exclusively catalyses the transfer of Glu to tRNAGlu, the ND-GluRS can also glutamylate tRNAGln forming Glu-tRNAGln. The misacylated product is then transformed to Gln-tRNAGln

• The effect of the selected compounds on NF kB transrepressio

  2022-04-08

  

  The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound

• br Acknowledgements br Introduction High intensity noise exp

  2022-04-08

  

  Acknowledgements Introduction High-intensity noise exposure has long been known to induce damage in the peripheral and central auditory system, often resulting in auditory pathologies such as hearing loss, tinnitus and hyperacusis (Syka, 2002; Roberts et al., 2010). Within the inner ear, struc

• br Results and Discussion br STAR Methods br

  2022-04-08

  

  Results and Discussion STAR★Methods Author Contributions Conflicts of Interest J.P.F. is a consultant for AstraZeneca, BMS, Johnson and Johnson, Novo Nordisk, and Sanofi, a member of the advisory panel for AstraZeneca and Sanofi, a member of the speaker’s bureau for Sanofi and Novo Nordi

• Here we examined whether complete ablation of GIP

  2022-04-08

  

  Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be

• The gene structures of cGalR and cGalR L were determined

  2022-04-07

  

  The gene structures of cGalR2 and cGalR2-L were determined by in silico comparison with the chicken genomic DNA sequences retrieved from the Ensembl database. Both cGalR2 and cGalR2-L genes are composed of two coding exons, separated by single introns of 0.9kb (cGalR2) or 3kb (cGalR2-L) locating wit

16439 records 489/1096 page Previous Next First page 上5页 486487488489490 下5页 Last page