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To combat the detrimental effects of neuropathological condi
2022-05-17
To combat the detrimental effects of neuropathological conditions, additional therapeutic interventions that either dampen chronic neuroinflammation or attenuate reductions in hippocampal neurogenesis are critically needed. The cannabinoid system has already been shown to rescue impaired neurogenesi
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Many studies support that the increase
2022-05-16
Many studies support that the increase of P4 improves embryonic survival and reduces embryonic losses in ruminants [6,[18], [19], [20]]. However, experimental results are variable, contradictory and often inconclusive results. Certain studies showed that administration of GnRH or hCG after artificia
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Bergmann glia cells BGCs are the
2022-05-16
Bergmann glia 2'-O-Methyl-ATP receptor (BGCs) are the most abundant glia cells in the cerebellum, comprising more than 90% of the cerebellar glia. These cells span the entire cerebellar molecular layer and encapsulate neuronal somata, dendrites and axons. BGC are involved in neurotransmitter uptake
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Herein we report the discovery of
2022-05-16
Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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factor xa inhibitors Interruption of glucagon signaling path
2022-05-16
Interruption of glucagon signaling pathway targeting glucagon receptor (GCGR) by gene knockout, antisense oligonucleotides or specific antagonists induces α-cell hyperplasia and alleviates hyperglycemia and other metabolic symptoms in diabetic animals and patients [[7], [8], [9]]. Here we used a ful
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The advent of the genomic era
2022-05-16
The advent of the genomic era has allowed greater detailed investigation of enzymatic properties and has shown that specific enzyme activity is linked to the substrate utilization profiles of the isoenzymes [30], [31]. Not surprisingly, the functional four β-galactosidases from A. niger F0215 shared
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The G protein coupled receptor GPR also called FFAR responds
2022-05-16
The G protein-coupled receptor, GPR40 (also called FFAR1) responds to medium and long chain unsaturated fatty acids, resulting in increase of insulin secretion during elevated glucose levels. The glucose dependency of insulin secretion makes this receptor a very good target for developing therapies
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Current studies have identified five orphan G
2022-05-16
Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs
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Immunohistochemistry using anti FFAR antibodies revealed imm
2022-05-16
Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import
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In this study we intended to explore the efficacy
2022-05-16
In this study, we intended to explore the efficacy of artesunate on liver fibrosis and further clarify its potential molecular mechanism. Artemisinin, a sesquiterpene lactone obtained from a Chinese plant Artemisia annua [27]. Artesunate, as a stable derivative of artemisinin, is an effective drug f
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Sperm capacitation was negatively r p
2022-05-16
Sperm capacitation was negatively (r = −0.68; p ive but not significant (r = 0.22). No significant relationship was observed between the expression levels of either CB1 receptor or FAAH and any of the sperm quality parameters studied. The scatter plot distribution of spermatozoa expression of CB1 an
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In studies described earlier IRL was administered intravenou
2022-05-16
In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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PF 04418948 br Author contributions br Acknowledgements The
2022-05-16
Author contributions Acknowledgements The work was supported in part by Natural Science Foundation of China (31601995, 31501028) and an internal research grant of Jianghan University (14042). The authors thank HY of Jingchu University of technology for revising the manuscript. Introduction
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With LML methyl oxo dihydropyridazin yl piperidin yl cyclobu
2022-05-16
With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform
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Introduction As a compound class histone deacetylase
2022-05-16
Introduction As a compound class, histone deacetylase inhibitors (HDIs) have been remarkably successful in the treatment of T-cell lymphoma [1]. Vorinostat (suberanilohydroxamic Amrubicin mg or SAHA) was approved by the FDA in 2006 for the treatment of cutaneous T-cell lymphoma [2], [3]; romidepsin
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