• br Materials and methods br Results and discussion br Conclu

  2022-07-25

  

  Materials and methods Results and discussion Conclusions Acknowledgements This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2013 unit and COMPETE 2020 (POCI-01-0145-FEDER-006684), and also by t

• The synthesis of compounds and were achieved according to st

  2022-07-25

  

  The synthesis of compounds and were achieved according to standard procedures. As shown in , The compound 4-methyl-1-(4-sulfobutyl)quinolonium () was prepared by alkylation reaction. Compounds and were synthesized by substitution reactions between 4-fluorobenzaldehyde and , , '-trimethylethanedi

• Fatty acids are also known to activate G protein coupled

  2022-07-22

  

  Fatty acids are also known to activate G-protein coupled receptors (GPCRs). LCFAs activate the GPCRs for free fatty Cyclophosphamide (FFA)1 and FFA4 (Briscoe et al., 2003; Hirasawa et al., 2005), whereas SCFAs activate FFA2 and FFA3 receptors, which are expressed in bovine neutrophils (Alarcon et a

• In regards to animals several studies have

  2022-07-22

  

  In regards to animals, several studies have reported the peroxisomal localization of FPS (Krisans et al., 1994, Olivier et al., 2000, Kovacs et al., 2007). Transfections of mammalian cells with the rat short FPS isoform followed by immunodetection localized the enzyme to the peroxisome (Olivier et a

• Introduction of a chloropyridine group onto the

  2022-07-22

  

  Introduction of a chloropyridine group onto the fluoro derivative (→) leads to a similarly potent compound that exhibits a lower /, and as was observed with (), was rapidly cleared. However, the high clearance of () did not prevent the increase in the concentrations of FAAs even as its plasma levels

• br Introduction Histamine was generally

  2022-07-22

  

  Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activi

• Cut proteins have five evolutionarily conserved

  2022-07-22

  

  Cut proteins have five evolutionarily conserved domains. These include a homeodomain, three Cut repeats, and a coiled coil structure. The cut repeats, called CR1, CR2, and CR3, are composed of 70 amino acids, and, along with the homeodomain, are each capable of binding DNA. Mammalian cut proteins fu

• br Conclusion In this report we describe

  2022-07-22

  

  Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar

• Much of the understanding of this system has

  2022-07-21

  

  Much of the understanding of this system has come from several studies focussed on CB1. A significant amount of research has demonstrated that activation of the CB1 receptor by cannabinoid ligands stimulates food intake [10], reduces gastrointestinal motility [11], and increases lipogenesis [12] and

• There is no doubt that GPR is a LPI receptor

  2022-07-21

  

  There is no doubt that GPR55 is a LPI receptor; however, we should re-consider whether or not GPR55 is in fact another cannabinoid receptor. The pharmacologies of the GPR55 and CB1 receptors are complicated; CB1 inverse agonist/antagonists SR141716A (rimonabant) and AM251 were shown to be potent ago

• Modulation of the cannabinoid system has been reported

  2022-07-21

  

  Modulation of the cannabinoid system has been reported to exert anti-parkinsonian properties through different mechanisms. On one hand, cannabinoids have neuroprotective properties in different rodent models of PD, both through a CB1/CB2 receptor-independent mechanism (Lastres-Becker et al., 2005) a

• Because of its excellent GPR potency

  2022-07-21

  

  Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, 2-D08 was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extensive panel of 1

• Based on our finding that TFA modulates GlyR function and

  2022-07-21

  

  Based on our finding that TFA modulates GlyR function and reports that TFA-bound Angiotensin I (human, mouse, rat) can differ markedly from those synthesized without TFA, we retested a previously published dodecapeptide (D12-116) that also enhanced GlyR function but this time as a chloride salt (Ti

• To maintain low Glu concentrations in the synaptic cleft bel

  2022-07-21

  

  To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino Lonidamine synthesis is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocyt

• PBI is an agonist of GPR and

  2022-07-21

  

  PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th

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