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The vast majority of clinical studies have shown that
2022-03-08

The vast majority of clinical studies have shown that chronic administration of GLP-1R agonists frequently lowers SBP/DBP in diabetic humans, which is consistent with preclinical studies, though the reported reductions are not as potent as those observed in their animal counterparts. In contrast, ac
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Two excellent GSMs with clear pharmacological effect across
2022-03-08

Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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At this point it needs
2022-03-07

At this point it needs, however, to be mentioned that most in vivo studies regarding the herein discussed nuclear receptors were performed in rodents, especially in mice. Due to the significant differences in metabolism in mice and humans, not all results are translatable between these species and h
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Recently some researchers working in China
2022-03-07

Recently, some researchers working in China Pharmaceutical University developed novel FFA1 agonists some of which were found to be efficacious in the management of type 2 diabetes and with low toxicity. For instance, Zheng et al. [48] in their in vivo study using experimental animals, reported that
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All of the abovementioned effects
2022-03-07

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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To validate that our natural experiment operates
2022-03-07

To validate that our natural experiment operates primarily through a large negative shock to the risk-taking incentives provided by option compensation measured by vega, we do two sets of tests. First, we confirm a significant drop in vega after the adoption of FAS 123R for treated firms relative to
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The H autoreceptors distributed mainly in the CNS act
2022-03-07

The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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GSK has also been used as PET radiotracer in
2022-03-07

GSK-189254 has also been used as PET radiotracer (in the form of [11C]-GSK-189254, also used as [11C]-AZ12807110 by Jucaite et al. (Jucaite et al., 2013)) to assess H3R occupancy (Ashworth et al., 2010), and is currently used in an image-based phase I clinical trial study for investigating GSK-23951
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br GC C and cGMP of mice and
2022-03-07

GC-C and cGMP: of mice and men As is usually the case for many genes, most of the studies that relate to GC-C have to date been carried out in mouse models, or in cell lines derived from human colorectal cancer tissue. What appeared to be a lacuna was any report of a human disorder that resulted
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The opposite modulation observed for circulating LPI levels
2022-03-07

The opposite modulation observed for circulating LPI levels and WAT GPR55 Pridinol Methanesulfonate receptor by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is
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Evaluating the plausibility of this selective scenario is ch
2022-03-07

Evaluating the plausibility of this selective scenario is challenging because of the uncertainties concerning the biological role of calpain-10 and the significance of its variants with regard to gene function and disease susceptibility. However, from a strictly evolutionary standpoint, our findings
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br Investigations br Genetics GLUT is a membrane bound glyco
2022-03-04

Investigations Genetics GLUT1 is a membrane-bound glycoprotein that provides base-rate glucose transport across blood-tissue barriers. It is constituitively expressed in erythrocytes, CDK4 inhibitor synthesis microvessels and astroglia. The gene exclusively associated with GLUT1 is SLC2A1, lo
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br Introduction Calorie restriction CR
2022-03-04

Introduction Calorie restriction (CR), in the absence of malnutrition, has beneficial effects on Cinacalcet function, including reducing the incidence of age-related neurodegenerative disease (Gräff et al., 2013), eliciting anti-depressant behavior (Lutter et al., 2008) and improving memory func
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Growth hormone secretagogue receptor GHSR is a
2022-03-04

Growth hormone secretagogue receptor (GHSR) is a member of G-protein-coupled receptor family [3]. GHSR is predominantly expressed in human pituitary, rhypothalamus and hippocampus [4]. GHSR is also expressed in peripheral tissues including lungs, liver, kidney, and adrenal gland. In cardiovascular s
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br Ghrelin interactions with the
2022-03-04

Ghrelin interactions with the opioid system The endogenous opioid system is an important regulator of appetite and metabolism (Bodnar, 2017, Nogueiras et al., 2012). In fact, several pharmacological studies have demonstrated that agonists of the three opioid receptors (mu, kappa, and delta) incre
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