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p-Chlorophenylalanine Histamine modulates an attentional sta
2022-04-13
Histamine modulates an attentional state, which might affect performances in the object recognition test. Indeed, systemic injection of H3 receptor inverse agonists enhances the attentional state (41). However, the memory recovery in our study is unlikely to be due to the enhanced attentional state.
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The repurposing of well characterized and well tolerated
2022-04-13
The repurposing of well-characterized and well-tolerated drugs in order to treat illnesses for which they were not originally intended has emerged as an attractive alternative to a long and costly process of drug development. Repositioning antihistaminergic ligands seems a promising idea given that
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An interference of fluorescence derived from biological samp
2022-04-13
An interference of fluorescence derived from biological samples is also an important BMS-707035 receptor to be addressed in the fluorescent analysis for biological samples. Advanced glycation endproducts (AGEs) are representative endogenous fluorescent substances that are widely distributed in vario
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The absence of direct oxidation of Fe by L
2022-04-13
The absence of direct oxidation of Fe2+ by L1 in experiments in solution would be consistent with the recognized low O2 affinity of sGC. It is known that, in AICAR phosphate with other hemoproteins, such as globins and heme-containing oxygenases with a Fe2+-proximal histidine linkage, sGC prevents
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Fig summarizes the underlying mechanism of SB on
2022-04-12
Fig. 7 summarizes the underlying mechanism of SB on inhibiting inflammation and maintaining epithelium barrier integrity in the TNBS-induced colitis model. Our findings not only explained the protective effect of SB on colon health, but also provided evidence that GPR109A likely constitutes a valid
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The activation of the ERK
2022-04-12
The activation of the ERK pathway may participate in the sensitization of primary afferents in pain transmission (Ji et al., 2009, Lai et al., 2011); the blockade of ERK activation in the DRG can decrease mechanical and heat hypersensitivity in inflammatory pain. IL-10 can inhibit phosphorylation of
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Reports of hyperlocomotion after administration of ALX coupl
2022-04-12
Reports of hyperlocomotion after administration of ALX-5407 [27] coupled with the lack of hyperlocomotion after administration of SSR504734, a non-sarcosine, long-residence time, competitive inhibitor [19], suggested that the GlyT1 inhibitor chemotype may impact OP. Furthermore, a compound with a co
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Tamoxifen is still the most frequently used
2022-04-12
Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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Tetrazole is one of the most commonly used bioisosteres
2022-04-12
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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As a part of our continuing efforts
2022-04-12
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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br Methods GLUT DS was diagnosed either
2022-04-12
Methods GLUT1DS was diagnosed either when analysis of the SLC2A1 gene showed a pathogenic mutation and/or when cerebrospinal fluid (CSF) analysis met the criteria for GLUT1DS: a CSF Endoxifen below the 10th percentile, a cerebrospinal fluid (CSF) to blood ratio below the 25th percentile and CSF l
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Here we studied GLUT targeted nanomedicines as
2022-04-12
Here, we studied GLUT1-targeted nanomedicines as a new strategy directed to overcome vascular barrier, enhancing delivery and efficacy in solid tumors. These nanomedicines were prepared by controlled installation of glucose on polymeric micelles incorporating the antitumor agent cisplatin, which is
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The plasma levels of glucose and amino acids at day
2022-04-12
The plasma levels of glucose and amino acids at day likely represent the function in utero since the blood was collected within 2h after birth. To elucidate the roles of intestinal transporters as determinants of plasma levels of glucose and amino acids, we analyzed the correlation between the expre
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The HH Gli pathway has
2022-04-12
The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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Preladenant receptor Fourthly the distribution sites after i
2022-04-12
Fourthly, the distribution sites after i.c.v. injection of FAM-ghrelin(1–7)-NH2 were explored in mice using the technologies of fluorescence labeling. The green fluorescence of FAM-ghrelin(1–7)-NH2 was strongly distributed in these structures of lateral ventricle, lateral septal nucleus, dorsal part
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