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Of the acidic hydroxyazoles involved
2020-11-16

Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Several evidences showed that seizures increase brain extrac
2020-11-16

Several evidences showed that seizures increase brain extracellular glutamate, which binds to N-methyl-d-aspartate (NMDA) receptor, then up-regulated cyclooxygenase-2 (COX-2) expression in brain capillaries to increase BBB P-gp expression [11,13,29,30]. A recent study demonstrated a different signal
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Several single nucleotide polymorphisms SNPs in humans affec
2020-11-16

Several single nucleotide polymorphisms (SNPs) in humans affect CYP3A expression and activity (Lamba et al., 2002). The CYP3A4 SNP rs2740574 (also referred to as CYP3A4*1B, by The Human Cytochrome P450 (CYP) Allele Nomenclature Database, http://www.cypalleles.ki.se/) is a change in the promoter regi
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Chemokines act as ligands for the
2020-11-16

Chemokines act as ligands for the chemokine receptors, which possess 7-transmembran domain-type proteins functionally coupled to G proteins. Leukocytes express 19 chemokine receptors which control their influx and activation at the site of inflammation. Human neutrophils express both CXCR-1 and CXCR
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Regarding the mechanism of action of CRF several studies
2020-11-16

Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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This work aimed to investigate whether
2020-11-16

This work aimed to investigate whether the increase in liver lipid depots, observed in the fetuses from rats fed a saturated-fat-rich diet, persists later in life in the offspring (a) at 21days of age immediately after weaning and (b) at 140days of age, after healthy nourishing. Furthermore, we want
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br Experimental methods br Results and discussion br Conclus
2020-11-16

Experimental methods Results and discussion Conclusions Here we describe the first reported method for high-yield Lisinopril dihydrate receptor of active and soluble mature CPG2 (in the absence of the leader peptide) and its individual catalytic and dimerization domains in E. coli. Such a
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Park et al expanded their own model as hydrogen bonding
2020-11-16

Park et al. [34] expanded their own model as hydrogen- bonding lattice fluid EOS (NLF-HB) [35] for calculating the activity coefficients of aqueous amino Medroxyprogesterone solution. Further, Pazuki et al. [36] extended the perturbed hard chain theory which has been proposed by Beret and Prausnitz
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The strong adsorption of amines to the
2020-11-16

The strong adsorption of amines to the stationary phase of gas chromatography (GC) columns causes issues such as tailing, ghosting and low reproducibility [12], [13]. A common practice to overcome this problem is the chemical derivatisation of amines prior to GC analysis [14]. Comprehensive reviews
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Several cholinesterase inhibitors have also been radiolabell
2020-11-16

Several cholinesterase inhibitors have also been radiolabelled with 11C as potential cholinesterase imaging agents. These include 11C-donepezil, 11C-methyltacrine, and 11C-physostigmine, which also have had limited success in demonstrating the known histochemically defined cholinesterase distributio
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br Conflict of interest br Acknowledgements This study was
2020-11-16

Conflict of interest Acknowledgements This study was supported by the National Natural Science Foundation of China (No.31571839), the Chinese Ministry Program for New Century Excellent Talents in University (NCET-12-0865), and Special Fund for Agro-scientific Research in the Public Interest (N
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br Conclusion In conclusion our findings do not suggest
2020-11-14

Conclusion In conclusion, our findings do not suggest that HT is an important determinant of future AD risk and are in line with a recent Cochrane review stating that HT is not indicated for preventing dementia or cognitive decline in postmenopausal women [13]. Contributors Conflict of inte
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MoAbs targeting the tumourigenic pathways such as IGF R may
2020-11-14

MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own immu
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There is an opposite opinion
2020-11-14

There is an opposite opinion indicating that EphB plays a role as cancer suppressor. Batlle et al. showed that loss of EphB expression represented a critical step in CRC progression, and CRCs that lacked EphB2 expression have been correlated with more advanced tumour stage, poor differentiation, and
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Interest in the PGE EP pathway
2020-11-14

Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing Tubastatin A HCl synthesis inflammation [1
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