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The excellent potencies selectivities and improved
2022-10-26

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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The putative physiological meaning of epinephrine related
2022-10-26

The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of c
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This study was funded and supported
2022-10-26

This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet
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br Results br Discussion Dopamine regulates behavioral respo
2022-10-26

Results Discussion Dopamine regulates behavioral responses to nicotine in Drosophila (Bainton et al., 2000), but neurochemical measurements of dopamine after nicotine stimulation had not been made. Here, we demonstrate for the first time that the stimulation of nAChRs causes dopamine release i
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br Materials and methods br Results and
2022-10-26

Materials and methods Results and discussions Conclusion Fermented camel milk with NS4 exhibited remarkable ACE-inhibitory activity, which revealed its potential application for the preparation of fermented camel milk beverage or fermented camel milk derived peptides in different foods or i
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Anti LT therapy by LO
2022-10-26

Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [
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The resolution cocrystal structure of ACL in complex with
2022-10-26

The 2.10Å resolution cocrystal structure of ACL in complex with citrate indicates that the carboxyl (COH) groups of citrate forms a network of H-bonds with hydrophilic residues surrounding the ACL citrate binding domain (CBD) (A). The - carboxyl group forms a salt bridge with the guanidine moiety of
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br Discussion Herein we demonstrate that mice deficient
2022-10-26

Discussion Herein, we demonstrate that mice deficient in L-12/15 LO are more sensitive to 3-NP-induced toxicity although a substantial individual variability in striatal lesion size in response to 3-NP in both genotypes was observed. This variability is not atypical; several studies demonstrate s
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We wanted to investigate the influence
2022-10-26

We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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Introduction Lipoxygenases LOXs are key
2022-10-26

Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic BTL105 (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other cells (Claesson, 2009)
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br Acknowledgements This work was
2022-10-26

Acknowledgements This work was supported by the Victorian Government Operational Infrastructure Support Program. KAB is supported by the Mavis Robertson Fellowship from the National Breast Cancer Foundation (NBCF; ECF-16-004), by an NBCF Novel Concept Award (NC-14-011), and by NHMRC project grant
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Among steroid saponins ginsenosides are the
2022-10-26

Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid
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br Results and discussion The soil fungus PSU RSPG
2022-10-26

Results and discussion The soil fungus PSU-RSPG37 (BCC56870) was isolated from soil samples collected from Rajjaprabha Dam, Suratthani Province, Thailand. The fungus was deposited at BIOTEC Culture Collection, National Center for Genetic Engineering and Biotechnology (BIOTEC), Thailand Science Pa
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Some of previous immunohistochemical studies
2022-10-26

Some of previous immunohistochemical studies have compared the levels of AR expression in low-grade versus high-grade and/or non-muscle-invasive versus muscle-invasive tumors. There was a significant or marginal decrease (Boorjian et al., 2004, Miyamoto et al., 2012b, Rau et al., 2011, Shyr et al.,
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Similarly results obtained in our lab using experimental dia
2022-10-26

Similarly, results obtained in our lab using experimental diabetic encephalopathy induced by streptozotocin (STZ) in C57BL-6 mice showed that the hippocampus of the diabetic animals exhibited reactive gliosis, neuronal loss, NF-kB signaling activation as well as high levels of IL-1β and vascular end
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