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br Materials and methods br Results br
2021-11-12
Materials and methods Results Discussion Employment of GIPR signaling, specifically the direction of this manipulation, as a strategy to improve body weight remains a contentious subject of intense scientific investigation [22], [32], [33]. Despite the physiological benefits of GIP on 8-Azi
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At present many methods have been
2021-11-12
At present, many methods have been applied for multiple detection. For example, 9-AC [[9], [10], [11]] is frequently used to detect multiple targets because of its exquisite sensitivity and specificity, but it is difficult to design experiments to test short-length oligonucleotides. Electrochemical
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From a cell signaling perspective given the importance
2021-11-12
From a cell signaling perspective, given the importance of agonist-directed signaling and biased agonism, one goal of this research update was to review the known contributions of G protein-dependent versus β-arrestin-dependent signals toward promotion of beneficial functions that FFA4 facilitates.
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15-deoxy-Δ-12,14-Prostaglandin J2 The exact mechanism by whi
2021-11-12
The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs
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Neuropathic pain NP is a
2021-11-12
Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c
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Last we demonstrate that the role of EZH
2021-11-12
Last, we demonstrate that the role of EZH2 as a transcriptional activator, with AR being a key target, coexists with its conventional catalytic role in gene repression and plays important oncogenic functions in AR-driven PCa (Figure 7F). Enzymatic EZH2 inhibitors such as EPZ and GSK126, although eff
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HIV incidence is often determined by following cohorts of
2021-11-12
HIV incidence is often determined by following cohorts of HIV-uninfected individuals and quantifying the rate of new HIV infections. HIV incidence can also be estimated using a cross-sectional study design, using laboratory assays to identify individuals who are likely to have recent HIV infection.
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The H R antagonist cimetidine Tagamet became the
2021-11-12
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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The proposed contributory role of endogenous histamine via a
2021-11-12
The proposed contributory role of endogenous histamine via activation of H1 receptor in the locomotor sensitization induced by caffeine was further ratified by H1 receptor antagonism during the induction phase and subsequently its effect on expression to locomotor sensitization induced by caffeine.
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Introduction Histamine Imidazolyl ethylamine is an important
2021-11-12
Introduction Histamine [2-(4-Imidazolyl)-ethylamine] is an important mediator of many physiological and pathological processes including inflammation, gastric allopurinol zyloprim secretion, neuromodulation, regulation of immune function, cell proliferation and differentiation, among others. Histam
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To prevent toxicity of free hemoglobin as well as
2021-11-12
To prevent toxicity of free hemoglobin as well as its degradation metabolites heme and free iron, several scavenger proteins and degradation enzymes protect the body. Haptoglobin (Hp) is the most well described hemoglobin scavenging protein that binds free hemoglobin and transports it to macrophages
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In contrast to sGC stimulators sGC activators promote enzyma
2021-11-11
In contrast to sGC stimulators, sGC activators promote enzymatic activity of sGC containing oxidized heme iron (Fe3+) or missing the heme group. A-350619 is one of the oldest activators of sGC to be discovered. A-350619 increased sGC activation in a non-additive manner with respect to YC-1, leading
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Among the compounds prepared at
2021-11-11
Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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M 1145 receptor Although glycine receptors predominate in th
2021-11-11
Although glycine receptors predominate in the brain stem and spinal cord, they are also expressed in higher brain regions such as the nucleus accumbens, frontal cortex, and hippocampus (Jonsson et al., 2012, Jonsson et al., 2009, Molander and Söderpalm, 2005b). A variety of drugs of abuse, including
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po1 br Results and discussion A diverse
2021-11-11
Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo
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