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As a continuation of our search
2023-05-25

As a continuation of our search for a selective AChE radioligand bearing a meta-F substituted N-benzyl moiety, we designed and synthesized a novel meta-F-CP-118,954 analog along with a meta-18F-labeled form via diaryliodonium salt-based precursor (Fig. 1). For comparative purposes, we incorporate th
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Although our data failed to
2023-05-25

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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Because the V ATPase inhibitors
2023-05-25

Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra
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br Method of literature search br Disclosures br Acknowledgm
2023-05-24

Method of literature search Disclosures Acknowledgment The authors thank and acknowledge Mrs. Jaini Parekh, BFA, for illustrating the diagram in Figure 1. An overview of angiogenesis Angiogenesis is a biological process through which there is the formation of new blood vessels from pre-
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Dual acting RAAS blockade and
2023-05-24

Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode
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Moreover mice exposed to high
2023-05-24

Moreover, mice exposed to high-cholesterol diet have mildly activated astrocytes, increased expression of ApoE and aquaporin-4 in the hippocampus, and altered levels of proteins associated with Aβ metabolism (Chen et al., 2016), which is related to a higher demand for cholesterol transport and the n
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Inflammatory factors released by activated cells during AD a
2023-05-24

Inflammatory factors released by activated cells during AD are very important for the disease progression. Not only several inflammatory cytokines, such as IL-1β, IL-18, and IL-33, but also anti-inflammatory ones, as IL-10 and IL-13, are upregulated in the brain of AD patients (Morimoto et al., 2011
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On the other hand it
2023-05-24

On the other hand, it is important to note that FR is different from the regulation of daily/circadian rhythms [44]. Based on models of physical systems [45], [46], it has been hypothesized that fractal physiological fluctuations reflect a network of elaborate regulatory processes interacting across
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An alternative to the agonist or
2023-05-24

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Aconitase clusters are prone to
2023-05-22

Aconitase clusters are prone to oxidations and are among the first to undergo a change in transition state during stages of electrophilic stress rendering them inactive [31]. Aconitase activity in LETO and OLETF did not differ at T0 suggesting that the early onset of insulin resistance may not be at
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Activation of AhR is also known to upregulate the expression
2023-05-17

Activation of AhR is also known to upregulate the expression of AhRR (AhR repressor), an inhibitor protein of AhR [29]. However, the exact mechanism by which AhRR represses AhR signaling is not well understood. The initial study by Mimura and colleagues suggested that AhRR is capable of directly com
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AdipoRon is an orally active synthetic
2023-05-17

AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r
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Rottlerin br Conclusion Our study of late life
2023-05-17

Conclusion Our study of late-life depression provides evidence of genotype-specific associations between depression and ACE methylation, as well as inverse correlations between ACE methylation and Rottlerin secretion. These findings highlight the potential need to consider methylation levels in c
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The cellular mechanism underlying the CGS mediated inhibitio
2023-05-17

The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Renal Cell Carcinoma RCC is a lethal cancer with
2023-05-17

Renal Cell Carcinoma (RCC) is a lethal cancer with bad prognosis due to development of chemoresistance and recurrence of an aggressive tumor with increased tumor-angiogenesis and metastasis [7]. We have found Axl and Gas6 to be differentially presented in RCC subtypes, and Axl to correlate to tumor
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