• To shed more light on the binding of

  2021-09-07

  

  To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ

• br Endogenous lipids as SLC transporter modulators

  2021-09-07

  

  Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure [

• Excessive extracellular glutamate can be removed from brain

  2021-09-07

  

  Excessive extracellular glutamate can be removed from Nimodipine interstitial fluids to the blood plasma for the maintenance of proper extracellular glutamate homeostasis in the mammalian central nervous system [[5], [6], [7]]. The glutamate concentration in the blood plasma increases in case of is

• The typical pharmacophore for GPR

  2021-09-07

  

  The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors

• The developed method was used to quantify

  2021-09-07

  

  The developed method was used to quantify RBC membrane transport of the anomers of three monofluorinated analogs of glucose in a modified medium designed to provide stable metabolic properties of the cells over the lifetime of the experiment. This allowed us to evaluate the specific interaction (spe

• So far the functional significance of GluR A

  2021-09-07

  

  So far, the functional significance of GluR-A and GluR-B in synaptic plasticity has been best studied in the context of long-term potentiation of synaptic transmission in vitro in the hippocampus and the regulation of synaptic strength in paradigms underlying activity-dependent learning in vivo Taka

• Regarding the causative diseases of ES patients with unknown

  2021-09-07

  

  Regarding the causative diseases of ES, patients with unknown cause and those with encephalitis had significantly higher CSF levels of HOBt against GluN2B-NT2 and GluN2B-CT than the disease controls, but patients with genetic disorder and those with cortical dysplasia showed no significant differen

• br Experimental br Results br Discussion The use of

  2021-09-07

  

  Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,

• br Materials and methods br Results br

  2021-09-07

  

  Materials and methods Results Discussion Present study demonstrated the ability of a GIP agonist, D-Ala2GIP, to protect against the QA-induced neurobehavioral phenotype of HD in rats, for the first time. D-Ala2GIP treatment significantly improved the behavioral deficits, biochemical and neu

• A single ICV injection of GALP stimulated

  2021-09-06

  

  A single ICV injection of GALP stimulated food intake in goldfish at 1h post-administration. This result is similar to that observed in rats, where ICV injection of GALP exerted an acute orexigenic effect [14], [15], [16]. Simultaneously, our findings counter the results found in mice, where central

• Cellular inhibition is caused by

  2021-09-06

  

  Cellular inhibition is caused by the hyperpolarization of the cell and is mediated by both synaptic and extrasynaptic GABAARs. Synaptic GABAARs are sensitive to high concentrations of GABA released at the synapse and mediate phasic inhibition. In contrast, extrasynaptic GABAARs mediate tonic inhibit

• Through the analysis of various

  2021-09-06

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic gpcr signaling motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discoveri

• Tylosin tartrate MMV s distinct mode of inhibition addresses

  2021-09-06

  

  MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.

• Itraconazole In conclusion we have shown that the brain

  2021-09-06

  

  In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to

• As evidenced by SARs and crystallographic data HO has at

  2021-09-06

  

  As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer

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