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The present data suggest that
2021-12-24

The present data suggest that the decrease of liver BAs was mainly due to the decrease of hepatic BAs synthesis because the BA synthetic enzymes Cyp7a1, Cyp7b1 and Cyp8b1 were markedly reduced. The increase may also be due to the increase of hepatic BAs efflux, because the liver BA efflux transporte
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According to the implication of the endocannabinoid system
2021-12-24

According to the implication of the endocannabinoid system in IBD, we decided in our laboratory to develop selective CB agonists and FAAH inhibitors to treat these diseases. Recently, we described 3-carboxamido-5-aryl-isoxazoles as selective CB agonists. This series of isoxazoles possesses a 2-subst
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br Experimental br Results and discussions br Conclusions br
2021-12-24

Experimental Results and discussions Conclusions Declaration of interests Acknowledgements Financial support from the National Natural Science Foundation of China (21605089 and 81773483), the Ningbo Municipal Natural Science Foundation (2017A610228 and 2018A610217), the Open Subject o
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br H R agonists In
2021-12-24

H2R agonists In search for potent and selective H2R agonists, comprehensive structure–activity relationship studies have been conducted and led to the first H2R agonists, e.g. 4(5)-methylhistamine (16) which is actually now used as selective H4R agonist (Fig. 4) (Durant et al., 1975, Lim et al.,
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br Conclusions In summary our
2021-12-24

Conclusions In summary, our results demonstrate that in short term effect, TBT induced concentration-dependent vasorelaxation of HUA rings. Regarding the long term effects, exposure to a concentration of 100 μM TBT the human umbilical SBE 13 HCl have a dual effect, and a decrease of the 5-HT2A e
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Importantly other aspects of platelet function aggregation
2021-12-24

Importantly, other aspects of platelet function (aggregation, spreading, in vitro and in vivo thrombosis) important for haemostasis and thrombosis were unaltered in Ral DKO platelets and mice. Beyond haemostasis and thrombosis however, platelets have been implicated in numerous pathophysiological pr
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In this study we explore different
2021-12-24

In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed
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Level of CD and other blood parameters in patients
2021-12-24

Level of CD4 and other blood parameters in patients before and after intervention are presented in Table 2. The mean of the CD4+ level before treatment in the intervention and placebo groups was 161.5 ± 291.1 and 159.9 ± 337.4, respectively (P = 0.232), which increased after treatment in both groups
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On the other hand we
2021-12-24

On the other hand, we have previously demonstrated that gelsemine displaced the H3-strychnine from membrane fractions of rat spinal cord homogenates. In addition, spinal gelsemine antinociception was blocked by intrathecal injection of the specific glycine receptor antagonist strychnine or gene sile
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br Dysregulation of glutamate transporter expression and fun
2021-12-24

Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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Consistent with recent independent studies we
2021-12-24

Consistent with recent independent studies, we confirm that the GCG-induced increase in oxygen consumption is only partially blunted in Fgf21−/− mice [32], implicating additional GCGR-dependent mechanisms contributing to the acute GCG-dependent enhancement of energy expenditure. Notably, glucagon ad
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The molecular nature of these putative
2021-12-24

The molecular nature of these putative Ca2+ LY 294002 is at present unknown. Apart from the NSVDC channel, which is permeable to Ca2+ [27], [15] functional Ca2+ channels have been identified in patch clamp experiments [28]. These channels, which were characterized as B-channels, seem to have very lo
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The top panel of Fig
2021-12-23

The top panel of Fig. 3 depicts the average number of planaria visible during each observation for all cohorts in the group testing following light exposure. Although there was considerably more variability than in the light-exposure conditions, a t-test showed no significant difference in count bet
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In addition recent research shows that HK contributes
2021-12-23

In addition, recent research shows that HK2 contributes to the inhibition of apoptosis through the suppression of the formation of mitochondrial permeability transition pores in association with voltage-dependent anion channel (VDAC) protein [11]. We also found that AKT2 mediates HK2 resistance to a
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Amyloid Beta-Peptide (1-40) br Pharmacology br Background to
2021-12-23

Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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