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Young et al described the role of adenine monophosphate
2023-11-09

Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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The excellent potencies selectivities and
2023-11-09

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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We also demonstrate that PACAP treatment dose
2023-11-09

We also demonstrate that PACAP treatment dose-dependently disrupts performance in the 5CSRTT, suggestive of attentional deficits, another core feature of mood and anxiety disorders. Treatment with PACAP (.5–1.0 µg) decreased the percentage of correct responses, increased the percentage of trials in
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Encouraged by this observation a systematic SAR study on
2023-11-09

Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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dynorphin Brain damage diseases such as cerebral ischemia
2023-11-09

Brain damage diseases, such as cerebral ischemia, brain trauma and infection are characterized by the increase in oxygen free radicals. Therefore, deeper understanding of the character and mechanism of free radical damage in the brain is important to ultimately relieve diseases and promote recovery
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Endoplasmic reticulum ER stress resulting from accumulation
2023-11-09

Endoplasmic reticulum (ER) stress resulting from accumulation of misfolded proteins in ER lumen stimulates a chain of adaptive responses termed as the unfolded protein response (UPR). Glucose related protein (GRP78/BiP), key ER chaperone essential for the activation of the ER-transmembrane signaling
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br Experimental protocols br Results and discussion
2023-11-09

Experimental protocols Results and discussion Conclusion 15-LOX-1 is an important mammalian lipoxygenase which plays an important role in the biosynthesis of leukotrienes, lipoxins and other signalling molecules. These signalling molecules play a regulatory role in several respiratory disea
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In the nineties we knew that baclofen
2023-11-09

In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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br Future view and implications The selection and spread of
2023-11-08

Future view and implications The selection and spread of multi(drug)-resistant microorganisms over the last decades has become a major and global public health concern [35]. Two growing threats originating from the fungal kingdom, i.e. Aspergillus fumigatus and Candida auris[36], [37], re-emphasi
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Introduction Alzheimer s disease AD is a complex
2023-11-08

Introduction Alzheimer's disease (AD) is a complex neurological disorder characterized by a progressive dementia resulting from synapse failure (Selkoe, 2002, Tanzi, 2005). The amyloid hypothesis maintains that the pivotal event in AD is the production of amyloid-β (Aβ) peptides following the prote
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The findings from our previous study indicate that mitochond
2023-11-08

The findings from our previous study indicate that mitochondrial biogenesis of astrocytes is increased under experimental septic condition [25]. Recent studies have shown that IL-6 can activate AMPK by increasing the concentration of AMP [26], while AMPK regulates mitochondrial biogenesis and autoph
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br Perspectives br Acknowledgments This investigation was su
2023-11-08

Perspectives Acknowledgments This investigation was supported by a Research Grant 2010/01385-5 from FAPESP (Sao Paulo Research Foundation, Brazil). P.F.S. was recipient of a CNPq (National Council for Scientific and Technological Development, Brazil) productivity grant. R.F.A. was recipient of
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br AKT signaling is essential during early dorsal patterning
2023-11-08

AKT signaling is essential during early dorsal patterning, neural crest induction and maturation AKT signaling modulates EMT and migration of the neural crest cells The defining feature of NC cells is their delamination from the dorsal neural epithelium. At the end of neurulation, mature premi
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Among the enzymes involved in adenosine metabolism adenosine
2023-11-08

Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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The geometry of two three
2023-11-08

The geometry of two, three, four and five LP533401 hcl neutral radical ACh molecule complexes with various electronic configurations, i.e. with various multiplicities equal to 1, 2 and 4 (for ACh trimer) were determined using DFT with the unrestricted B97d/SVP potential/basis set in Gaussian09 progr
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