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While the S site has been
2021-12-17
While the S2 site has been implicated in binding, it FDA-approved Drug Library is unclear whether the S2 site plays a role in the substrate transport process. Crystal structures have revealed that different drugs and detergents can bind to the S2 site of SERT [8] and LeuT [[13], [14], [15]]. Howeve
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ICH induced striatal lesion produced a reduction
2021-12-17
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino MC 1568 transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia (R
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To confirm the in vitro findings atorvastatin or
2021-12-17
To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g
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Entinostat It is important to underline
2021-12-17
It is important to underline that Entinostat although ghrelin increases the motivation to eat even in fed state, its effects on food intake and reward are blunted in obese animal models (Zigman et al., 2016). This emphasizes also the interconnection between homeostatic regulation of food intake and
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br Materials and methods br Results and discussion br
2021-12-17
Materials and methods Results and discussion Conclusion Altogether, our data provide an unexpected insight into Cx26 trafficking pathway and gap junction assembly in the cochlea. Since many of the disease-causing mutations in GJB2 impair the trafficking and delivery of Cx26 to the cell surf
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At the end of experiments rats were injected
2021-12-17
At the end of experiments rats were injected high dose of sodium pentobarbital (90mg/kg) and the rat’s head was cut and frozen in −20°C for 20min with the injecting tube in situ before section. The location of the tip of the injecting tube was verified and all the tips of the injecting tube were in
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Introduction Initially postulated to represent the main sour
2021-12-16
Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba
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br Results and discussion The synthesis of core
2021-12-16
Results and discussion The synthesis of core aldehyde building block 2 commenced with known aldehyde 5. The Horner–Wadsworth-Emmons olefination of the latter (using commercially available 6) gave cinnamate ester 7. Facile hydrogenation of the double bond in 7 was achieved over Raney nickel withou
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Before discovery of their histone demethylase function
2021-12-16
Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tail
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The compounds described in this paper were
2021-12-16
The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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The importance of FXR FGF signaling
2021-12-16
The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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There is sufficient evidence to
2021-12-16
There is sufficient evidence to indicate that kisspeptin plays a role in regulating sheep reproduction. However, the molecular mechanism by which kisspeptin regulates GnRH formyl peptide receptors and reproduction has remained unclear. Therefore, in this study on GnRH in sheep, the promoter region o
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Herein we report the discovery
2021-12-16
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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Ghrelin is a brain gut peptide hormone
2021-12-16
Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing
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br Conclusion In the present
2021-12-16
Conclusion In the present study, we found that the majority of commercially available antibodies and antibody-based tools against galanin and its receptors that we tested do not meet validation requirements. Therefore, critical validation of these tools by the user is essential before being used
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