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A compound structurally similar to
2022-08-13
A OSMI-1 structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-e
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br Discussion The present study explored
2022-08-12
Discussion The present study explored that the effect of the MTP gene −493G/T polymorphism on the risk of hepatic steatosis in Turkish patients with chronic HCV genotype 1 infection. Some researchers revealed that the MTP gene −493G/T polymorphism was associated with hepatic steatosis in CHC infe
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The neotropical fish Prochilodus lineatus has
2022-08-12
The neotropical fish Prochilodus lineatus has been widely used in experimental designs for being sensitive to variations in water quality and tolerant to laboratory conditions (Camargo and Martinez, 2006, Cazenave et al., 2014, da Silva and Martinez, 2014, Vieira et al., 2016). Concern and reports a
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Furthermore we observed a striking difference
2022-08-12
Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic 94535 type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of sGC. In combinatio
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Activity of compound in rat brain tissue highlights the pote
2022-08-12
Activity of compound 10 in rat N6-Methyl-ATP tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as
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br Introduction Nicotinic acid has been used clinically for
2022-08-12
Introduction Nicotinic Liproxstatin-1 HCl has been used clinically for more than 50 years [1] since it has anti-atherogenic effects, including the ability to reduce triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C), and elevate high-density lipoprotein cholesterol (HDL-C) [2]. Ni
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br Amino acid usage in cancer
2022-08-12
Amino 78416 usage in cancer Perspective High glucose consumption is a common feature of several types of tumor cells. Therefore, so far, in vivo positron emission tomography (PET) imaging with the glucose analog 18F-fluorodeoxyglucose (18F-FDG) has been used to detect various tumors. However,
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KYNA has been shown to regulate iNKT cytokine release Fallar
2022-08-12
KYNA has been shown to regulate iNKT cytokine release (Fallarini et al., 2010) and at high concentrations to reduce LPS-induced TNFα release from cultured peripheral blood mononuclear tetrandrine (Wang et al., 2006). Our results show that elevating KYNA to “exercised” levels is sufficient to promot
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The differential tissue and ligand dependent signaling
2022-08-12
The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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In breeding season small mammals increase
2022-08-12
In breeding season, small mammals increase dispersal and social communication to maximize their opportunity to mate. In the present study, we found that gerbils in April showed more locomotion and exploratory behavior in the open field test. Moreover, subadult gerbils in April and July were more lik
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TXA has been shown to be a competitive antagonist
2022-08-12
TXA has been shown to be a competitive antagonist on the GABAA receptor and potentially also the glycine [7], [12], [15] receptor. Furtmuller et al. showed that TXA right-shifted the GABA CRC by one order of magnitude [7], while in our study TXA similarly right-shifted the GABA EC50 value from 0.33
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Hepatic drug metabolizing enzymes and transporters expressio
2022-08-12
Hepatic drug-metabolizing Celastrol and transporters expression were regulated by nuclear receptors [19], [20], [21]. The effects of HFD-induced fatty liver on drug metabolizing enzymes in mice were recently studied, and the results provided a systematic evaluation of the changes of nuclear recepto
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Ionotropic glutamate receptors GluRs are ligand gated ion ch
2022-08-12
Ionotropic glutamate receptors (GluRs) are ligand-gated ion channels that mediate information processing at the majority of excitatory synapses in the brain and participate in such physiological processes as learning and memory, development and maintenance of cellular connections, and pain perceptio
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Decreases in LS mean h WMG
2022-08-12
Decreases in LS mean 24-h WMG versus placebo were observed with both the 10mg q.d. a.m. (−18.8mg/dL) and 6mg q.d. p.m. (−25.0mg/dL) MK-3577 ‘partial blockade’ regimens, but was not assessed for the 25mg b.i.d regimen. Decreases in FPG versus placebo were observed for both the 10mg q.d. a.m. (−7.2mg/
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How do myofibroblast sources compare between bone marrow and
2022-08-12
How do myofibroblast sources compare between bone marrow and other organs? Perivascular bmn 673 with MSC properties significantly contribute to fibrosis in muscle, fat, skin, heart, kidney, lung, and liver (reviewed in Iwayama et al., 2015) and activate Gli1 in many of these organs (Kramann et al.,
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