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br Conclusions The present data suggest that homeostatic bal
2025-01-20

Conclusions The present data suggest that homeostatic balance of the cortical/hippocampal adenosinergic tone is necessary for normal working memory function and any deviation appears to impair performance – either as a consequence of A2AR under-activation when adenosine levels are reduced or due
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Altogether the situations described above clearly impede the
2025-01-18

Altogether, the situations described above clearly impede the critical steps of drug discovery and development and the scientific process in general [14]. In conclusion, it is the opinion of these authors that many exciting lines of drug discovery (which includes those devoted to nAChR ligands) have
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dna synthesis inhibitors antibiotics Zhang et al screened th
2025-01-18

Zhang et al. screened three thousand compounds library and found two active 3,5,6-substituted indolin-2-one molecules. Further, they designed various derivatives of this scaffold and among them compound 23 from the series was found active with 1.8 μM on Aurora-B kinase luminescent assay [53]. Jeffe
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Besides one should also consider that all antioxidant compou
2025-01-18

Besides, one should also consider that all antioxidant compounds (free soluble or insoluble bounds) exist all together in colon, where radicals and antioxidant compounds react continuously with each other. At this point, after the consumption of antioxidants bound to dietary fiber, they reach the co
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Kidney contributes importantly to the long
2025-01-18

Kidney contributes importantly to the long-term blood pressure control via regulating sodium homeostasis. Renal proximal tubule (RPT) is one of the most critical segments for sodium reabsorption within kidney and therefore involved in blood pressure adjustment. This process is regulated by numerous
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br AMPK as a druggable target AMPK signaling has attracted
2025-01-18

AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in
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br Introduction AMPA receptors AMPARs mediate the majority o
2025-01-18

Introduction AMPA receptors (AMPARs) mediate the majority of fast excitatory postsynaptic currents (EPSCs) in the H2A (107-122) peptide (Jonas, 2000). The brevity of EPSCs and rapid deactivation of AMPARs depend upon a short lifetime of synaptically released glutamate, estimated to be about 1 ms
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br Materials and methods br
2025-01-17

Materials and methods Results Discussion Conclusions These studies provide important mechanistic insights to explain the long-established physiological observation that obese adipose tissue has higher rates of basal lipolysis. Increased lipolysis contributes to increased hepatic Alarelin
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Here we have used transcriptome
2025-01-17

Here, we have used transcriptome analysis of primary neonatal rat cardiomyocytes treated with either the ETR agonist endothelin-1 or the α1-AR agonist phenylephrine to assess differences in their respective signalling networks, and further probed these differences using a panel of fluorescent resona
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Since natural and recombinant glycoprotein hormones exhibit
2025-01-17

Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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As an alternative to chronic receptor blockade we have been
2025-01-17

As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify cetirizine hcl adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facilit
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br New AMPK activators Fenofibrate is a
2025-01-17

New AMPK activators Fenofibrate is a drug of the fibrate class used for the treatment of dyslipidemia [53] but is also an agent that could alleviate DN-induced alterations through AMPK activation (Fig. 2). Streptozotocin-induced diabetic rats treated with fenofibrate improved in not only renal fu
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Our initial approach to identify hits was two
2025-01-17

Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI DMAT library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was incorp
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br Difference between ACh and ER tests There
2025-01-17

Difference between ACh and ER tests There are few reports concerning the provoked spasm between ER and ACh in the same patients [51], [52], [53]. Different mediators may have the potential of different coronary responses. In our experience, spasm provoked by intracoronary injection of ER is focal
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Regarding androgens it is known that they
2025-01-17

Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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