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Cultured cells or mouse lung tissues were harvested and lyse
2020-10-08
Cultured cells or mouse lung tissues were harvested and lysed in Radio-Immunoprecipitation Assay (RIPA) buffer (0.05 mol/l Tris–HCl pH 7.4, 0.15 mol/l NaCl, 0.25% deoxycholic acid, 1% NP-40, 1 mmol/l ethylenediamine tetraacetic Saracatinib (EDTA), 1 mmol/l phenylmethylsulfonyl fuoride, 1 μg/ml apr
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Cysteine protease inhibitors representing several chemical s
2020-10-08
Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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In summary our findings show that LPS can activate CysLT
2020-10-08
In summary, our findings show that LPS can activate CysLT2R on microglial Ruxolitinib to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of LP
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We next examined the effects of substituents around
2020-10-08
We next examined the effects of substituents around the carboxylic pramipexole dihydrochloride moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to
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Substitutions on the benzene ring
2020-10-08
Substitutions on the benzene ring of the phenyl acetic corticotropin releasing factor moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine ()
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One specific brain region that
2020-10-08
One specific WAY-100635 maleate salt region that may be involved in the reduction of anxiety after anti-SVG-30 treatment is the lateral septum which contains a high density of CRF2 receptors [5], [44]. The lateral septum often exhibits increased immediate early gene expression in response to stress
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In this study we observed
2020-10-08
In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased wehi when the sensitization condition was established. Similarly, CRF2 receptor increase was
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Among the various neurotransmitter systems pointed
2020-10-08
Among the various neurotransmitter systems pointed out to play a role in the mediation of defensive and antinociceptive responses elicited by environmentally aversive stimuli, the neuropeptide corticotropin-releasing factor or hormone (CRF or CRH) has attracted the interest of many researchers inves
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Abha et al reported Natural coumarinolignoids isolated
2020-10-08
Abha et al. reported Natural coumarinolignoids isolated from the seeds of Cleome viscosa consist of a racemic mixture of cleomiscosins A 19, B 20 and C 21 and were screened for anti-inflammatory activity through mol. docking and QSAR studies by using reported in vivo activity of Swiss albino mice. B
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Accumulated evidence indicates that apelin
2020-10-08
Accumulated evidence indicates that apelin plays a protective role in ischemic stroke, contributing to post-stroke recovery (Yang et al., 2014; Chen et al., 2015; Xin et al., 2015; Yan et al., 2015). Apelin gene (APLN) encodes prepro-apelin with 77 amino acids, while the C-terminal 23 price scd rec
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The reference standards methyl difluoro dioxolo benzo imidaz
2020-10-08
The reference standards methyl 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)carbamoyl)benzoate () and -(2,2-difluoro-5-[1,3]dioxolo[4′,5′:4,5]benzo[1,2-]imidazol-6-yl)-3-methoxybenzamide (), and their corresponding desmethylated precursors 3-((2,2-difluoro-5-[1,3]dioxolo[4′,5′:
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We have previously reported the characterization of
2020-10-08
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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br Allosteric inhibitors In general candidate drugs that
2020-10-08
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Further proof is required as to
2020-10-08
Further proof is required as to whether ER membrane receptors play a role in the maintenance of bone mass. It is also possible that other non-genomic pathways may be involved. Nevertheless, whatever the precise mechanism of action of estrogens may be, the imbalance between bone formation and resorpt
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In Fig results of this experiment are shown
2020-10-06
In Fig. 1 results of this experiment are shown as the contour plots of endopeptidase activity. Optimal for the enzyme production by this strain concentrations of peptone and inorganic phosphate were found to be 24 and 0.3g/l, respectively. For specific activity, the optima close to those for glutamy
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