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By association a possible mechanism which may underlie the p
2021-11-11
By association, a possible mechanism which may underlie the progression of seizures is long-term potentiation (LTP). Indeed, LTP shares many common mechanisms with seizures activity both anatomically and physiologically, and has been implicated as a mechanism of acute epileptogenesis (Wasterlain et
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Hydantoin in region F bridging the phenoxybenzene and benzim
2021-11-11
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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Of xenobiotic quinones thymoquinone methyl
2021-11-10
Of xenobiotic quinones, thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; Fig. 1) is one of the most thoroughly studied for its pharmacological properties. It is the most active component of Nigella sativa, commonly called black cumin2, 3, the essential oil of the seeds of which are used for trea
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Recently an increasing number of studies have highlighted th
2021-11-10
Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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Compound was synthesized in a racemic
2021-11-10
Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position
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In this study we further expanded the antitumor bioactivity
2021-11-10
In this study, we further expanded the antitumor bioactivity, with the BALB/c S-180 tumor model, which is long-established due to its highly aggressive in all strains of laboratory mice and rats (Cui et al., 2003). We investigated the tumor-regressing ability of β-glucan by different modes of admini
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p 00 The negative impact that dimers
2021-11-10
The negative impact that dimers present in gp120 preparations have on overall gp120 affinity for CD4i ligands, mainly by affecting the on-rate, was addressed in this report. Indeed, when his(6)-tagged gp120 proteins, purified with nickel beads (before FPLC, containing gp120 dimers) were used to meas
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br Discussion Agonist and antagonist action
2021-11-10
Discussion Agonist and antagonist action at the GluN1/GluN3 Pam3CSK4 Biotin sale is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via GluN
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UNC2025 In conclusion we have designed
2021-11-10
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,
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br Results br Discussion Our
2021-11-10
Results Discussion Our cardiomyocyte-specific GR knockout mice did not show spontaneous cardiac hypertrophy unless pressure overload was given to the heart. This finding is somewhat different from previous work of a cardiomyocyte-specific GR methylergometrine mouse model using GR-floxed mice w
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somatostatin receptor Regulation of FGF signalling is critic
2021-11-10
Regulation of FGF signalling is critical to ensure a balanced response to receptor stimulation. This occurs largely through negative feedback mechanisms, including receptor internalisation via ubiquitination (Wang et al., 2002) and induction of negative regulators, for example SPRY, SPRED 1 and 2 an
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br Materials and methods br Results br
2021-11-10
Materials and methods Results Discussion Several studies highlighted an improvement of glycaemic control in diabetic patients receiving sunitinib, while the underlying mechanism remained still elusive [3], [4], [5], [6], [8]. The present study gives evidence that sunitinib directly and spec
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Introduction Ventilator induced lung injury VILI
2021-11-10
Introduction Ventilator-induced lung injury(VILI) is the most common complication in the mechanical ventilation in clinic. Repetitive opening and closing of Tianeptine sodium at high pressures during artificial ventilation would generate shear stress and then lead to the damage of cell junction an
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Several observations about structure activity
2021-11-10
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Pimasertib class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage
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Glycopyrrolate Oltipraz has been shown to inhibit
2021-11-09
Oltipraz has been shown to inhibit the growth of HCC Glycopyrrolate and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with oltipraz
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