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br During cardiac ischaemia a decrease in
2021-11-26
During cardiac ischaemia, a decrease in GJ coupling is observed, which results in slower conduction of electrical impulses and a higher risk of arrhythmias.[13], [20] In Huntington’s disease an increase in the TAI-1 australia of 5 Cxs was observed in the astrocytes in the brain, suggesting an adap
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Based on the previous report that FXR regulated
2021-11-26
Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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In stark contrast to this study Zhang and
2021-11-26
In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC on average treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment with the genotox
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Growing evidence supporting the anti inflammatory
2021-11-26
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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br Factor Xa an enzyme in the coagulation
2021-11-26
Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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br Application of TIRFM to visualizing exocytosis TIRFM
2021-11-26
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin 88 3 (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant mice, or s
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In studies described earlier IRL
2021-11-26
In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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A second H R antagonist
2021-11-26
A second H3R antagonist with benzamide-based structure from Johnson & Johnson is JNJ-31001074, known as Bavisant and under chemical IUPAC name of (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone. It is a compound with molecular weight 329.44, HBA four, and MLogP 1.52 encompass
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Tylophora atrofolliculata is a centuries used folk medicine
2021-11-26
Tylophora atrofolliculata is a centuries-used folk medicine for the treatment of rheumatism in China (Jiangsu New Medical College, 1977). One group of its bioactive components is phenanthroindolizidine alkaloids, which have been demonstrated as lead compounds of anti-tumor agents in our previous stu
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In summary P P macrocyclization proved to be
2021-11-26
In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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GPR has been implicated in neuropathic and
2021-11-26
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
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Human GPR hGPR was originally isolated in as
2021-11-26
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Compound was synthesized starting from
2021-11-26
Compound was synthesized starting from α-cyclopropyl glycine (). After protection of the free amine via methyl carbamate and esterification to the methyl ester, the pyrrolidine core was furnished by condensation with methyl acrylate under basic conditions. Double deprotonation of the pyrrolidine fol
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These differences have led to the recognition that
2021-11-25
These differences have led to the recognition that the extent to which transport contributes to shaping postsynaptic signals likely reflects a balance between the density of transporters and the amount of l-glutamate in the synaptic cleft. Consequently, those synapses exhibiting the characteristics
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In our study we observed elevation of
2021-11-25
In our study, we observed elevation of the fluorescent intensity in the layers without synaptic contacts (OS, ONL, INL, and GCL). In the enzyme-linked fluorescence assay system, released glutamate is catalyzed by the enzyme on the surface of a quartz glass. Therefore, the diffusion of glutamate onto
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