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1347 receptor In the previous study we demonstrated the impo
2025-02-05

In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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Although our data failed to reproduce the robust enhancement
2025-02-05

Although our data failed to reproduce the robust enhancement of LTP in the rat dentate with nicotine that was previously reported, our results with NS6740 suggest a more fundamental role for α7 receptor signaling in modulation of synaptic tone in the LTP pathway. The discovery of the cholinergic ant
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LY2940680 Very recently Niessen et al have described the res
2025-02-05

Very recently, Niessen et al. have described the resensitizing effect of MB327 on nAChR performing solid-supported membrane (SSM)-based electrophysiological experiments (Niessen et al., 2016) using plasma membrane preparations obtained from Torpedo californica. These findings validated and underline
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br In patients with spina bifida
2025-02-05

In patients with spina bifida and spinal cord injury, fecal incontinence is a serious issue that can impair activities of daily living and patient self-esteem. To address this Malone et al. first described the Antegrade Continence Enema (ACE) procedure in 1990 [1], which achieves continence by all
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Exemestane mg br LOX in colorectal cancer Colorectal cancer
2025-02-05

5-LOX in colorectal cancer Colorectal cancer (CRC) like other malignancies exhibits an overexpression of 5-LOX. Ohd et al. (Ohd et al., 2003) revealed in a study that malignant colon tissues overexpress 5-LOX activity and retain elevated levels of inflammatory mediators, leukotrienes. Additionall
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2'-O-Methyl-UTP solution br The human CYP A gene
2025-02-05

The human CYP17A1 gene is located on chromosome 10q24.3 (1) and spans 6.6 kb, which contain eight exons (2) and 1.6 kb of coding region. From this gene, the same 2.1-kb mRNA species is transcribed in both the adrenals and gonads (3), which yields a 57-kDa microsomal cytochrome P450c17 enzyme (CYP1
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Here we show that the co activation of RTKs and
2025-02-05

Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC N1-Methyladenosine triphosphate and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JA
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Unfortunately results of serum plasma AC
2025-02-03

Unfortunately, results of serum/plasma AC assessment after food antioxidant intake are rather controversial: although some papers reported an increase of AC after food antioxidant intake (Khan et al., 2015, Torabian et al., 2009), unexpectedly, in a lot of long-term intervention studies (days, week
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SB1518 To this the evidence of opposite effects
2025-02-01

To this, the evidence of opposite effects of noradrenaline and adrenaline on the striatal firing initiation (Fig. 6, Fig. 7) should not be ignored, because the striatum is related to controlling action timing by regulating the firing increase rate (Tanaka and Kunimatsu, 2011). Although the ligand su
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Search sphere This sphere includes the
2025-02-01

Search sphere 1: This sphere includes the bet bromodomain binding site between the α–γ subunits. The center point of the search area was located at x=35.26, y=77.67, z=137.74 and the initial search radius was set to 27Å which assures that the corresponding area outside the channel pore of the two su
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In addition to the above mentioned synaptic mechanisms the s
2025-02-01

In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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Having established the structural requirements for potency i
2025-02-01

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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br Aurora A Aurora B and Aurora C small molecule
2025-02-01

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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Human hepatocyte transplantation resulted in some animals
2025-01-31

Human hepatocyte transplantation resulted in some animals with relatively sparse repopulation while others had >90% of their liver containing human hepatocytes. The presence of circulating human albumin varied based on the amount of repopulation as the degree of humanization is reported to correlate
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Thiazole heterocycles constitute an interesting
2025-01-31

Thiazole heterocycles constitute an interesting class of molecules, which exhibit a broad spectrum of biological activity, including antifungal properties [[16], [17], [18], [19]]. Encouraged by our previous study that describes the activity of hydrazine-thiazole derivatives against C. gattii and C.
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