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To be a qualified non specific CYP
2021-04-27

To be a qualified non-specific CYP inhibitor used as an in vitro or in vivo screening tool to distinguish CYP involvement in the overall metabolism, a complete inhibition of the entire metabolism catalyzed by CYPs in a simple experiment is desired. Based on our results, 100 μM atipamezole can comple
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We neither observed changes in
2021-04-27

We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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br Methods br Results br Discussion The lowest intra CeA
2021-04-27

Methods Results Discussion The lowest intra-CeA dose of R278995/CRA0450 that prevented the elevations in sphingosine 1-phosphate receptor modulator reward thresholds associated with nicotine withdrawal was 0.05μg/side (0.1μg total bilateral dose). The total bilateral dose in the present stu
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br Method br Results br Discussion In this cross
2021-04-27

Method Results Discussion In this cross-sectional study, we investigated the relationship between the COMT ValMet polymorphism and age on regional cortical thickness in healthy adults across the lifespan. The mesocortical pathway was of primary interest because of its projections from the v
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The Fontan circulation When first
2021-04-27

The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital Clodronate Disodium sale disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creat
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Soon after the discovery of ET and the cloning of
2021-04-27

Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).
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br Conclusion This study demonstrates
2021-04-27

Conclusion This study demonstrates the presence of functionally viable ET receptors in the surgically extracted tissue from patients with CTEPH. The ET receptor was associated with smooth muscle cells, mainly the contractile phenotype of SMC that surrounds the recanalised 58 4 and can be seen wit
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Prenylation may turn a flavonoid
2021-04-27

Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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br Results and discussions In general experimental analysis
2021-04-27

Results and discussions In general, experimental analysis is time consuming and expensive. Thus, In the present study, Taguchi design of experiments (DOE) was adopted to reduce the number of trials. To analyze the data, a High Level Analysis (HLA) is performed by averaging measured data for each
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br STAR Methods br Acknowledgments We are grateful to
2021-04-27

STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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During the past few years several studies
2021-04-27

During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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The in vitro enantioselective metabolism of pesticides
2021-04-27

The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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The loss of secondary mutation T M
2021-04-27

The loss of secondary mutation T790M mutation after AR and SCLC transformation was also reported for Rociletinib. Piotrowska et al. using the MGH NGS platform recently reported in 13 biopsies among 12 EGFR T790M+ patients progressing after treatment with Rociletinib the loss of EGFR T790M mutation i
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We also found downregulation of TRIM in the
2021-04-27

We also found downregulation of TRIM32 in the hearts of dilated and hypertrophic cardiomyopathy patients in addition to TAC and phenylephrine treated mice [51]. TRIM32 and Dysbindin are known to interact in skeletal muscle, and we could confirm this interaction in cardiomyocytes as well. In cardiomy
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br Methodology To simulate chip flow trajectory the force an
2021-04-26

Methodology To simulate chip flow trajectory, the force and torque acting on the chips in high pressure coolant are computed based on the control volume method [6]. During the setup, a typical gun drill chip and gun drill bit are imported into ANSYS CFX 14.0 and prescribed as stationary solids. T
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