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The MeO CFO phen yl group was then
2022-02-03
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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TH287 receptor Introduction Parkinson s Disease PD
2022-02-03
Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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regadenoson Given the estimated number of
2022-02-03
Given the estimated number of 150–300 NSVDC channels in a red cell [7] and a single channel conductance of 30 pS at physiological salt concentrations [6], the maximum conductance observed in intact red regadenoson indicate either a very low open state probability, in the order of 10−3 or a far lowe
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In conclusion starting from the weakly potent
2022-02-03
In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic CNQX sale led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally reported series a
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Next we studied the effects of the compounds PA
2022-02-03
Next, we studied the effects of the compounds PA-Glu, PA-hSuc, and PA-hPim on the IGly of rat hippocampal neurons. As in the experiments with IGABA, IGly was affected by steroids with a pregnane skeleton, but not those with an androstane skeleton. At the same time, androstane steroids were shown to
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The ETA receptor has a
2022-02-03
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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br Conflict of interest br Acknowledgements
2022-02-01
Conflict of interest Acknowledgements This work was funded by the University of Turin (ex60% 2014), World Wide Style Project (WWS; University of Turin/Fondazione CRT) and University of Florence (ex60% 2014). ACR and AP designed the study; AP, EB and IO conducted the literature search and analy
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Hypoxia HIF and Inflammation Cellular responses to hypoxia
2022-02-01
Hypoxia, HIF, and Inflammation Cellular responses to hypoxia are essential for life and are now recognized to be dysregulated in a wide range of disease processes. The key players in these pathways are a family of transcription factors, the hypoxia-inducible factors (HIFs; see Glossary), as well as
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br Other Functions of HCA Receptors HCA receptors in particu
2022-02-01
Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor e1 activating enzyme 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in
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Biochemical assays have provided evidence that
2022-02-01
Biochemical assays have provided evidence that prolonged exposure to GPR35 agonists can induce GPR35 internalization [2], [4], [11], [13]. Our finding that neuronal excitability decreased regardless of whether the slices were superfused for a few minutes or incubated for a few hours with GPR35 agoni
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Cichlasoma dimerus as most teleost fish species present neur
2022-02-01
Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most Tranilast synthesis species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA
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br GnRH receptor expression is altered within GnRH
2022-02-01
GnRH receptor expression is altered within GnRH neuronal cells Kisspeptin failed to stimulate GnRH expression in our line of GT1-7 cells. Instead, we have found that kisspeptin increased the expression of the GnRH receptor in these acetylcholine receptor (Sukhbaatar et al., 2013). Based on the r
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br Materials and methods br Results br Discussion In
2022-02-01
Materials and methods Results Discussion In the CNS, GLP-1R is associated with G-protein signal transduction pathways, which can activate adenylyl cyclase and protein kinase A by cyclic adenosine monophosphate, and mediates neuronal activities implicated in various pathophysiological change
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Young et al described the role of
2022-01-31
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Hypertriglyceridemia is associated with an overproduction an
2022-01-31
Hypertriglyceridemia is associated with an overproduction and secretion of triglyceride-rich lipoproteins (TRLs), due to increased liver lipid substrate availability (Adiels et al., 2005, Choi and Ginsberg, 2011), and/or reduced catabolism of TRLs and their remnants, due to reduced lipoprotein lipas
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