• L002 receptor The more important effect of

  2022-08-09

  

  The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced L002 receptor release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenag

• Among the compounds prepared at this stage

  2022-08-09

  

  Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with moderat

• The aim of this study is to explore new

  2022-08-09

  

  The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof

• br Results and discussion br

  2022-08-09

  

  Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p

• The most classic case of acquired and relapsing

  2022-08-09

  

  The most classic case of acquired and relapsing epilepsy is temporal lobe epilepsy (TLE), which originates from the hippocampal formation, a structure situated in the mesial temporal lobe (Majores et al., 2007). Our experiment used the prominent pilocarpine-induced TLE model. Systemic administratio

• Three main transport systems are involved in solute

  2022-08-09

  

  Three main transport systems are involved in solute loss and red cell dehydration (summarised in Fig. 1: Lew and Bookchin, 2005): the deoxygenation-induced cation conductance (sometimes termed Psickle), the Ca-activated K+ channel (or Gardos channel) and the KCl cotransporter (KCC). Psickle is activ

• G quadruplex DNA structures may exist in

  2022-08-08

  

  G-quadruplex DNA structures may exist in either positive or negative strand of a promoter to regulate gene expression. The positive strand of the HOXC10 promoter is overall C-rich in the 1000 bp upstream of the TSS (36.6% of C versus 24.1% of G) and contains many C-runs; thus, G-quadruplex structure

• br Results and discussion CATALYST software allows automatic

  2022-08-08

  

  Results and discussion CATALYST software allows automatic pharmacophore construction by using a collection of molecules with activities ranging over a number of orders of magnitude. In addition, CATALYST pharmacophores (hypotheses) explain the variability of bioactivity with respect to the geomet

• Production of reactive oxygen species ROS at

  2022-08-08

  

  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

• AVE 0991 br Conclusion H R H R

  2022-08-08

  

  Conclusion H1R, H2R, and H3R mRNAs were expressed in rat OE. Moreover, these three histamine receptors were present in the cytoplasm of ORNs in OE. This is the first report of the expression and localization of histamine receptors in mammalian OE. These findings indicate that histamine may play a

• In an RNAi screen to interrogate the function of

  2022-08-08

  

  In an RNAi screen to interrogate the function of transmembrane proteins in ISCs/EBs, we identified the SJ protein tetraspanin 2A (Tsp2A) as a tumor suppressor. Further characterization reveals that Tsp2A expression initiates in ISCs and Tsp2A protein assembles at the SJs in the progenitor Moxifloxac

• Human epidermal growth factor receptor HER neu also known as

  2022-08-05

  

  Human epidermal growth factor receptor 2 (HER2/neu, also known as CerbB-2, or ERBB-2) is a proto-oncogene located on chromosome 17q21, which encodes a transmembrane protein with tyrosine kinase activity, and belongs to the HER receptor family (EGFR, named also HER1, HER3, and HER4) [6]. HER2 is invo

• GPR has been implicated in neuropathic and inflammatory

  2022-08-05

  

  GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow

• Continuing studies of endocannabinoid ligands at

  2022-08-05

  

  Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort

• br Potential endogenous agonists of GPR The first

  2022-08-05

  

  Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic Ursodiol [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO cells,

15877 records 408/1059 page Previous Next First page 上5页 406407408409410 下5页 Last page