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A motivation for this study is the ability
2022-02-01
A motivation for this study is the ability of PGD2 to inhibit hair lengthening (). Here we demonstrate that PGD2 also inhibits hair regeneration after wounding. Thus, PGD2 and Gpr44 inhibition of the hair follicle occurs in multiple contexts and may be exploited in future therapies. Pharmaceutical c
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The aim of this study is to
2022-02-01
The aim of this study is to explore new Glo-I inhibitors using the structure-based pharmacophore approach. Eighteen Glo-I co-crystallized structures have been explored to investigate their pharmacophoric features. Ninety two pharmacophoric models were generated. QSAR analysis followed by Ligand Prof
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Lamina II SG spinal cord neurons play an important role
2022-02-01
Lamina II (SG) spinal cord neurons play an important role in regulating nociceptive input from the periphery [20,21]. Moreover, lamina II neurons are concentrated with glycinergic or GABAergic inhibitory interneurons. Therefore, it is possible that β-alanine might modulate nociceptive transmission i
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To further implicate the role of EAAT in morphine
2022-02-01
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 HG-9-91-01 was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice
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We have previously shown in the same time
2022-01-31
We have previously shown in the same time frame reported here (10 min) that AG was not degraded into DAG [29] and that the half-life of AG in human serum is ∼10 min [49]. However, we cannot rule out in this study that there is not breakdown to DAG that could contribute to the levels of 125I-ghrelin
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br Galanin in depression A major impediment in depression
2022-01-31
Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard
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Natural product based drug discovery can be enhanced with
2022-01-31
Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in PCI-32765 binding assays, we used molecular modeling to predict how well these compounds f
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Here we report a new human
2022-01-31
Here, we report a new human genetic disorder in a patient with hypoalgesia, altered fear and memory symptoms, and a non-anxious disposition. This disorder is attributable to co-inheritance of a microdeletion in a novel pseudogene and a known FAAH hypomorphic SNP. The microdeletion is flanked by repe
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br Conclusion B esterases and reproductive parameters can be
2022-01-30
Conclusion B-esterases and reproductive parameters can be used as effect biomarkers of the aquatic contamination with chlorpyrifos. In P. corneus exposed for 14 days to the insecticide, the carboxylesterases determined with p-NFB proved to be the most sensitive biomarker. However, exposure to env
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br Conclusion In this report we describe the synthesis
2022-01-30
Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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GPR is present primarily in the pancreas and the
2022-01-30
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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br Clinical development of anti NASH drug
2022-01-30
Clinical development of anti-NASH drug therapies The current understanding of NASH pathogenesis has led to broad efforts to target several features of the disease, alone or in combination, even in the absence of liver-guided therapies. Therefore, drug development in NASH is a rapidly changing fi
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Previously localization studies have been
2022-01-30
Previously, localization studies have been conducted using antibody-based detection of Pgp protein in tissues of Clade V nematodes. In transgenic C. elegans, Cel-Pgp-3 and Cel-Pgp-1 proteins localized to the apical membranes of the excretory and intestinal cells and the anterior pharynx (Broeks et a
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br Materials and methods br
2022-01-30
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the 6656 mg of neurons and glial ce
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For many plasma membrane receptors
2022-01-30
For many plasma membrane receptors including GPCRs, their density on the cell-surface is finely controlled by various transcriptional, post-transcriptional and post-translational mechanisms, and is often a determinant of overall receptor function in a cell. To date, the transcriptional regulation an
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