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Next we were able to demonstrate that compound retained the
2020-07-30
Next, we were able to demonstrate that compound 18 retained the favorable pharmacokinetic properties already established for the azaindole acetic Tianeptine sodium scaffold. In vitro Caco-2 permeability was moderate (Papp A–B/B–A 0.9/2.2×10−6cms−1), with good solubility of 5.2mg/ml at pH 6.8 determi
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Previously we reported the structure activity relationships
2020-07-30
Previously, we reported the structure–activity-relationships (SAR) of a series of pyrazinone-based CRF receptor antagonists, , , leading to highly potent and efficacious compounds such as , and ultimately to the discovery of (BMS-764459, ). Detailed SAR studies of the lower phenyl/pyridyl substitu
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Although the relationship between central and peripheral
2020-07-30
Although the relationship between central and peripheral regulation of CRF signaling is yet to be elucidated, an accumulation of findings indicates independent regulation between central and peripheral CRF signaling. For example, i.c.v. administration of CRF to hypophysectomized rats induced locomot
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br Materials and methods br Results br Discussion We
2020-07-30
Materials and methods Results Discussion We and others have previously reported behavioral patterns exhibited by WKY rats which are consistent with the heightened levels of anxiety, including an exaggerated secretion of stress hormones [22], reduced time exploring the OF arena and increased
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br The LSCP model and its
2020-07-30
The LSCP model and its properties In this section, we first introduce the LSCP model in Section 2.1. Some examples of the model are presented in Section 2.2 and basic properties of the model are presented in Section 2.3. Finally, Section 2.4 introduces finite dimensional approximations necessary
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At the same time we see decreased connectivity from
2020-07-30
At the same time, we see decreased connectivity from the pgACC to both the AUD and PHC in Met-carrier tinnitus individuals, which would be in keeping with the second proposal, i.e. that the pgACC is deficient in its tinnitus-suppressive effect. This is further supported by the fact that Met carriers
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Cy7.5 maleimide(non-sulfonated) We hypothesized that phospho
2020-07-30
We hypothesized that phosphorylation might also be involved in the oligomerization processes. In fact, phosphatase treatment of human serum samples and lysates from human omental adipose tissue caused an increase of HMW adiponectin. In line with these in vitro findings, we confirmed that CK1δ-mediat
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In the early stage of the HACl
2020-07-30
In the early stage of the HACl studies, LMCs in the lamina of the housefly were used to identify and characterize the Lapatinib (Hardie, 1987, Hardie, 1988, Nässel et al., 1988). In the present study, we isolated and characterized two types of Musca HCL channels for the first time, as these previous
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br Materials and methods br Results br Discussion
2020-07-29
Materials and methods Results Discussion Conclusions Acknowledgments Introduction Residues and metabolites of pharmaceuticals that reach aquatic systems can exert adverse effects on non-target organisms (Kasprzyk-Hordern et al., 2008, Brausch and Rand, 2011, Verlicchi et al., 2012,
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The discovery of a selective DGAT inhibitor has been the
2020-07-29
The discovery of a selective DGAT-1 inhibitor has been the subject of a number of recent reviews and publications., , , , , , , , First generation DGAT-1 inhibitors from Japan Tobacco, Pfizer, Bayer, and Abbott are shown in and have a terminal carboxylic chembridge receptor moiety which mimics the
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The DDR gene located on chromosome region
2020-07-29
The DDR1 gene, located on chromosome region 6p21.33, encodes a transmembrane tyrosine kinase receptor involved in melanocyte anchoring through binding to collagen IV (Silva de Castro et al., 2010). So far, only three studies have been conducted on the association between DDR1 polymorphism and the ri
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While coverage of the immunoregulatory functions and disease
2020-07-29
While coverage of the immunoregulatory functions and disease context of IL-12 family cytokines keeps growing, the field is characterized by debilitating gaps in our understanding of structure-function relationships. To date, the only structural and mechanistic data regarding the interaction of an IL
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Finally it has been emphasized that the PAG
2020-07-29
Finally, it has been emphasized that the PAG receives CRF-containing neuron projections from other anxiety-related p m x structures such as amygdala, hypothalamus and BNST (Gray and Magnuson, 1992). Furthermore, studies in vitro have shown an excitatory effect on PAG neurons following CRF administr
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A more detailed description of higher
2020-07-29
A more detailed description of higher-order thinking is offered by King, Goodson, and Rohani (1998): “Higher order thinking skills include critical, logical, reflective, metacognitive, and creative thinking. They are activated when individuals encounter unfamiliar problems, uncertainties, questions
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br Discussion and conclusion The current study
2020-07-29
Discussion and conclusion The current study made predictions, based on previous research outcomes, regarding the use of college entrance exam scores as indicators of academic success. As predicted for H1, H2, students\' ACT/SAT exam scores showed significant positive correspondence with both adva
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