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br Perspectives and challenges Previously the main
2025-02-19
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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br A Rs which were cloned and
2025-02-19
A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including Cytidine 5-triphosphate involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R ag
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br Difference between ACh and ER tests There are few
2025-02-18
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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br Antioxidative stress and anti inflammation Oxidative stre
2025-02-18
Antioxidative stress and anti-inflammation Oxidative stress is a major cause of reduced endothelial NO bioavailability in hypertension, and inflammatory response is thought to play an important role in these processes (Blake and Ridker, 2001, Landmesser et al., 2006). Reactive oxygen species (ROS
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NLX a k a F or befiradol exhibits nanomolar affinity
2025-02-18
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in KU-57788 DNA repair inhibitor 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).
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To date more than different mutations in the
2025-02-18
To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su
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CYP A is one of the key metabolizing enzymes
2025-02-18
CYP3A4 is one of the key metabolizing heat shock protein inhibitors of the cytochrome P450 (CYP) superfamily of heme-containing monooxygenases. As the CYP family of enzymes plays important roles not only in the xenobiotic metabolism and detoxification of a large number of drugs, but also in the bio
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At present the role of autophagy
2025-02-18
At present, the role of autophagy in neurons remains controversial. Autophagy has homeostatic and waste-recycling functions and plays a protective role in neurodegeneration diseases. Moreover, it has been thought as a programmed cell death participating in the occurrence and development of various d
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In this report the natural compound deguelin potently
2025-02-18
In this report, the natural compound deguelin potently and dose-dependently suppressed Aurora B kinase activity in vitro, indicating that this compound is an effective Aurora B inhibitor. The docking study indicated that deguelin was docked into the ATP-binding pocket of Aurora B and formed hydropho
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Two critical determinants of receptor
2025-02-18
Two critical determinants of receptor trafficking are found within the GABAB1 cytoplasmic tail: the di-leucine internalization signal (EKSRLL) (Margeta-Mitrovic et al., 2000, Restituito et al., 2005) and the ER retention signal (RSRR) (Calver et al., 2001, Margeta-Mitrovic et al., 2000, Pagano et al
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br Consequences of central apelin APJ modulation Regarding
2025-02-18
Consequences of central apelin/APJ modulation Regarding extra-hypothalamic actions, recent data demonstrate that the central apelin/APJ system could be a potential new target for the regulation of memory (Han et al., 2014). Then, intracerebroventricular (icv) apelin administration in mice impairs
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As the experimental procedure used could reflect agonist sti
2025-02-18
As the experimental procedure used could reflect agonist-stimulation of both anterograde and retrograde APJ trafficking, as has been described for the δ-opioid peptide receptor (Zhang et al., 2006b, Zhang et al., 2006a), receptor internalization was more directly monitored by loading cell surface HA
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We have shown that an extensive region in SERBP amino
2025-02-18
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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We report here the case of
2025-02-18
We report here the case of a patient with probable genetic prion disease with a Creutzfeldt-Jakob disease-like phenotype associated with a rare PRNP E196K mutation who initially exhibited atypical clinical manifestations principally characterized by behavioral abnormalities. Case report An 80-ye
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Of the infants in the study there were twin deliveries
2025-02-18
Of the 580 infants in the study, there were 106 twin deliveries and 10 triplet deliveries. There was no difference in prenatal antibiotic exposure between multiple and singleton births. Nevertheless, analysis of maternal antibiotic use was based on the 309 individual mothers who were provided WZ314
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