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In order to evaluate the
2020-04-02

In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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br Application of D receptor PET
2020-04-02

Application of D1-receptor PET in psychiatric disorders Discussion Compared to other markers of the DA system, only a limited number of studies have investigated D1-R in psychiatric disorders. In schizophrenia, which is the most studied condition with a total of 83 identified unique patients,
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br Conclusion br Conflict of interest br Acknowledgments
2020-04-01

Conclusion Conflict of interest Acknowledgments The authors extend their appreciation to the Deanship of Scientific Research at King Saud University for funding the work through the research group project No. RGP-120. Introduction Methods Results Conclusions Introduction Pat
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br CXCR The CXC receptor and CXCR
2020-04-01

CXCR1/2 The CXC receptor 1 and 2 (CXCR1 and CXCR2) have been well characterised in vertebrates. In mammals and birds, the two receptors are shared by the ELR+ CXC ligands, namely the CXCL8 family members that have proinflammatory roles in recruitment of neutrophils, monocytes and macrophages to s
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The potential off target activity
2020-04-01

The potential off-target activity of against other ATP-dependent enzymes, such as kinases, was also investigated. Encouragingly, there was no significant inhibition of ATP binding to 97 human kinases, when was evaluated at 10μM within a DiscoveRx scanEDGE® kinome screen (, ). All together, these d
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br Materials and methods br Results br Discussion
2020-04-01

Materials and methods Results Discussion Drug of abuse induces widespread VX-745 changes in the molecular and cellular functions in circuits between VTA and its neighbored regions such as NAC, and amygdala. It is belived that these changes result behavioral phenotype that characterize addi
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There exists a glucose residue in the
2020-04-01

There exists a glucose residue in the structure of 5. Acid hydrolysis (Supplementary data) followed by TLC comparison with the reference compound as well as GC–MS analysis (l-cysteine methyl ester hydrochloride derivative: tR=22.22min for glucose residue of 5 and 22.46min for the reference compound)
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Ligand independent constitutively active variants have also
2020-04-01

Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o
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br Materials and methods br
2020-04-01

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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Injurious effects of cigarette smoke CS on human health
2020-04-01

Injurious effects of cigarette smoke (CS) on human health are progressively being acknowledged both in animal and human studies. CS is a highly complex mixture that contains substantive amounts of toxic oxidants, nitric oxide, organic compounds, free radicals and microbial cell components including
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br Results br Discussion Cell responds to fluctuating
2020-04-01

Results Discussion Cell responds to fluctuating environmental factors by activating a set of compensatory mechanisms including changes in the lipid profile. Compensatory reactions occurring in membranes in response to phosphate deprivation include replacement of phospholipids by phosphorus-fre
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br Advantages of modified proteins
2020-04-01

Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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KU14R receptor Alzheimer s disease AD is a chronic
2020-04-01

Alzheimer’s disease (AD) is a chronic, progressive neurodegenerative disorder of the KU14R receptor which is considered a leading cause of dementia and affects 20–30 million people worldwide. Presently, a suitable treatment and prevention strategy against AD is hardly available. Various studies hav
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In human neuroblastoma SH SY Y cells and in lymphoma
2020-04-01

In human neuroblastoma SH-SY5Y meclofenamate and in lymphoma Jurkat cells, Yamanaka et al. [56] showed that exogenously added 24(S)-hydroxycholesterol could be efficiently esterified by ACAT1. These results suggest that both ACAT1 and ACAT2 can control the oxysterol levels by directly esterifying t
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Group B phytocystatins are also expressed in caryopses
2020-03-31

Group B phytocystatins are also expressed in caryopses. Although their expression patterns during germination are similar to those of the group A inhibitors, their expression patterns during seed development vary, indicating that they play different roles in the latter process. The highest levels of
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