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In experiments using D to
2022-03-08
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse GM 6001 tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1, Fig. 2, Fig
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In conclusion we have designed and characterized a
2022-03-08
In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date, N
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The general aim of our in vitro experiments was to
2022-03-08
The general aim of our in vitro experiments was to analyze the patterns of ghrelin and GHSR-1a expression in the mammary glands of dairy goats during pregnancy and to examine the direct effect of ghrelin on cell proliferation in cultured MECs of pregnant dairy goats. For this purpose, we cultured go
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C598-0466 So far several methods have been used
2022-03-08
So far, several methods have been used to monitor the level of GJC and its regulation in astrocytes studied in acute C598-0466 slices (see Giaume et al., 2012). This mainly includes approaches based either on electrophysiological properties of gap junction channels or on “dye coupling” experiments
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The Notch cleavage efficiency of Aph aS containing
2022-03-08
The Notch-cleavage efficiency of Aph1aS containing complexes was lower than that of Aph1aL γ-secretases, especially in combination with PS2, suggesting that Aph1aS is a determinant of low Notch-cleavage specificity, considering that the different subcellular localization of PS1 and PS2 didn't affect
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The orientation of the immobilized enzyme may
2022-03-07
The orientation of the immobilized enzyme may affect its activity and stability and therefore the final biocatalyst performance. Since proteins present areas more prone to unfolding in their surface or near to it [36], the immobilization through these areas may improve the final biocatalyst stabilit
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Determination of enzyme activity differs from other analytic
2022-03-07
Determination of enzyme activity differs from other analytical procedures. In this m6A case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic reaction pro
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br Chemistry Analog has been previously reported
2022-03-07
Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo
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Several small molecules such as erastin and RSL
2022-03-07
Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer difluprednate [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-dependent
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br Results br Discussion CD T
2022-03-07
Results Discussion CD8 T Oligomycin Complex are important for immune control of many viral infections (Ehtisham et al., 1993, Kagi et al., 1994, Mullbacher et al., 1999, Walsh et al., 1994). CD8 T cells are essential for efficient clearance of MAV-1 from the lungs and for airway inflammation d
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Another important question for future studies will be whethe
2022-03-07
Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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To discriminate the peripheral and central involvement
2022-03-07
To discriminate the peripheral and central involvement of FAAH in paracetamol action, we proposed a pharmacological strategy challenging the analgesic action of paracetamol observed in an inflammatory context with either a peripherally-restricted FAAH inhibitor (URB937, Clapper et al., 2010, Moreno-
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We also evaluated the effect
2022-03-07
We also evaluated the effect of varying ionic strength. These experiments included previously characterized H3 (residues 1–21) and SNAIL (residues 1–9) peptides [8], [34] to allow a comparative analysis with different ligands (Fig. 1A). As shown in Fig. 2 and listed in Table 2, it is evident that a
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br Discussion Our results showed that the histamine
2022-03-07
Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation
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br Conclusion br Acknowledgement br Introduction Biogenic am
2022-03-07
Conclusion Acknowledgement Introduction Biogenic amine histamine is synthesized from L-histidine by histidine decarboxylase (HDC). Histamine is involved in a wide variety of pathological and physiological processes including allergic reactions, inflammation, immune responses, gastric secret
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