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br Conclusions Several lines of evidence have
2024-04-15
Conclusions Several lines of evidence have been established, which support the adenosine kinase hypothesis of epileptogenesis, which is based on a sequence of events leading from acute 2-Cl-IB-MECA injury to initial downregulation of ADK, rise in extracellular adenosine, changes in astrocytic ade
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Tacrine an aminoacridine derivative Fig A
2024-04-15
Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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br LO and the secretase complex
2024-04-15
5LO and the γ-secretase complex Supporting this concept, during a recent trial testing the γ-secretase inhibitor semagacestat (LY 450139), AD patients actually experienced a functional decline compared to patients who took a placebo in addition to several other significant adverse effects (Doody
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Given these findings above we hypothesized
2024-04-15
Given these findings above, we hypothesized that hypernociception produced by intra-amygdala 8-OH-DPAT is result of hyperpolarization in this area. This neuronal inhibition of the amygdaloid complex might result in an inactivation of crucial neurotransmitter systems of the descending inhibitory pain
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Crystal structures were obtained of sulfonamide and amide
2024-04-15
Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Secondly leptin has been shown
2024-04-15
Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer GDC-0994 by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in the promoter
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To better illustrate the involved neuronal postganglionic pa
2024-04-15
To better illustrate the involved neuronal postganglionic pathways, central apelin-13 injection was performed in rats received peripheral preadministration of NOS inhibitor L-NAME, sympatholytic agent guanethidine and/or muscarinic receptor agonist bethanechol. Compared with the rats received vehicl
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AP was originally described as
2024-04-15
AP-1 was originally described as a heterodimer of the bZIP proteins c-Jun and c-Fos. The experiments described here showed that stimulation of TRPV1 channels induced the expression of both of these classical constituents of AP-1. The essential role of both proteins was analyzed in a series of experi
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br G protein activation through croaker ZIP An essential
2024-04-15
G protein activation through croaker ZIP9 An essential criterion for designating a steroid binding protein as a membrane steroid receptor is to demonstrate that it can transduce steroid signals in order to elicit a cellular response. Treatment with 100nMT caused G protein activation in croaker ZI
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br Acknowledgments br Introduction Alzheimer
2024-04-15
Acknowledgments Introduction Alzheimer's disease (AD) is a severe neurodegenerative disorder primarily affecting the elderly population. Senile plaques in the brain, one of the pathological hallmarks of AD, are formed by the accumulation of aggregated β-amyloid (Aβ) with an extensive β-sheet s
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br STAR Methods br AMPK A
2024-04-15
STAR★Methods AMPK: A Therapeutic Target in the β Cell? Loss of pancreatic β cell function is a hallmark of the transition to a diagnosis of T2DM (see Glossary) 1, 2, 3, 4. AMPK activation has gained attention for the treatment of hyperglycemia in prediabetes as an insulin-sensitizing agent bec
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TOK-001 The preferential expression of ALOX B in
2024-04-13
The preferential expression of ALOX15B in human macrophages may explain why human genetic studies investigating the association of ALOX15 with cardiovascular disease did not show consistent results. Two rare functional polymorphisms have been characterized in the ALOX15 gene, which leads to increase
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Ala a branched chain amino acid has been reported to
2024-04-13
Ala, a branched chain amino acid, has been reported to play a functional role in intracellular pH regulation, and it typically accumulates in response to various stresses (Limami et al., 2008, Rocha et al., 2010). Our data demonstrated that increasing Cd concentrations at lower Cd doses resulted in
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NLX a k a F
2024-04-13
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in pritelivir receptor to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additional
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sc4 library mg Our results showed that oral
2024-04-13
Our results showed that oral administration of cordycepin, in the concentrations of 5 and 10mg/kg for 3weeks, exerted no influence on body weight and hippocampus weight in mice. Although some reports have pointed out that cordycepin had toxic effects because it may be potential for inducing cell dea
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