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There are numerous theories of schizophrenia etiopathology a
2021-06-21
There are numerous theories of schizophrenia etiopathology and genetics is often taken into consideration [25]. The dopamine D2 receptor is important since it is blocked by typical antipsychotic drugs with high affinity which is correlated with the ability to control psychotic symptoms in schizophre
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JC-1 synthesis The compounds were ranked based on the Glide
2021-06-21
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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In this context we initiated a program to
2021-06-21
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in clemastine fumarate mg replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriaz
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Compound was advanced to a chronic efficacy study
2021-06-21
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, DMPO 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily for ea
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Eleutherococcus senticosus Rupt Maxim Maxim is
2021-06-21
Eleutherococcus senticosus (Rupt. & Maxim.) Maxim is a shrub belonging to the Araliaceae, which is commonly distributed in China, Korea, Japan and Russia. It has been traditionally used as folk medicine for the treatment of rheumatism, diabetes, and hepatitis (Nan et al., 2004). Recent phytochemical
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Recent pharmaceutical research in the field of respiratory
2021-06-21
Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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In conclusion our data demonstrated that montelukast and pra
2021-06-21
In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va
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The in vitro enantioselective metabolism of pesticides
2021-06-21
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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Acknowledgements This work was supported in part
2021-06-21
Acknowledgements This work was supported in part by a Scholarship Fund for Young Researchers by the Promotion and Mutual Aid Corporation for Private (2017 to S.K.), research grant from Japan Rett Syndrome Support Organization (2018 to S.K.), and MEXT-Supported Program for the Strategic Research Fou
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beta amyloid Taken together our results demonstrate that
2021-06-21
Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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In the preclinical evaluation of CRF receptor antagonists ef
2021-06-21
In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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Although many neurotransmitters e g catecholamines
2021-06-21
Although many neurotransmitters (e.g., catecholamines, serotonin, and excitatory/inhibitory amino acids) have been implicated in the modulation of anxiety-like responses (Carobrez et al., 2001, Molchanov and Guimaraes, 2002, Vianna et al., 2001), the so-called atypical neurotransmitters, endocannabi
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Role of ROS signaling in
2021-06-21
Role of ROS signaling in regulating cell death pathways has been well established. Involvement of CLIC1 in ROS production has been studied earlier. It was observed that macrophages from clic1 mice showed ~30% decrease in cellular ROS generation which effects macrophage function (Jiang et al., 2012).
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In the next experiments using a Cell Stress Array
2021-06-21
In the next experiments, using a Cell Stress Array kit we assessed the effect of mixture of progestogens on the expression of 26 proteins. One group of proteins including PON3, Phospho-p38a, SIRT2, SOD2, HIF-1 alpha, HIF-2alpha and p27 were upregulated upon progestogen treatment. HIF-1 functions as
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Estradiol the predominant circulating estrogen in humans it
2021-06-21
Estradiol, the predominant circulating estrogen in humans, it is mainly secreted by the granulosa cells of the ovarian follicles, and the corpora lutea, by the mechanisms indicated above. On the other hand, estretrol is synthesized exclusively during pregnancy by the fetal liver and reaches maternal
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