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The ETA receptor has a
2022-04-24
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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The molecular mechanisms underlying VSMC ETB receptor upregu
2022-04-24
The molecular mechanisms underlying VSMC ETB receptor upregulation have been studied after 24–48h organ culture in both coronary and cerebral arteries. The increased expression of contractile ETB receptor at these time points has been shown to depend on transcriptional mechanisms and PKC and the ext
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We examined the expression of notch in the brains
2022-04-24
We examined the expression of notch-1 in the brains of mice following morphine or oxycodone tolerance. The results showed that notch-1 levels did not change following morphine or oxycodone tolerance, with or without the treatment of IRL-1620. This indicates the possibility that morphine or oxycodone
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Accumulating evidence suggests that the
2022-04-24
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, PP242 derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knockout mice
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The present study was therefore conducted with three
2022-04-24
The present study was therefore conducted with three aims; (1) we tested the effect of IRL-1620, a selective ETB receptor agonist, on the analgesic tolerance to morphine and oxycodone in mice; (2) we determined the expression of ETA receptors and ETB receptors in the dacomitinib synthesis of morphi
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br Conclusion In this research we have successfully
2022-04-24
Conclusion In this research we have successfully formulated a PEGylated liposomal formulation encapsulating IRL-1620. The liposomal nanocarriers loaded with IRL-1620 were characterized for their particle size, PDI, zeta potential, and loading efficiency. We established that the treatment with IRL
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In studies described earlier IRL was administered intravenou
2022-04-24
In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat
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br Formation of secretory vesicles and trafficking
2022-04-24
Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for 623 off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Amphiphysi
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br Acknowledgements br Insulin is a vital
2022-04-24
Acknowledgements Insulin is a vital peptide hormone with the exclusive capacity to regulate the blood glucose that entirely is secreting from pancreatic β cells (Kasai et al., 2014). The human insulin comprises 51 amino 623 residues, with a molecular mass of 5.808 kDa. INS, responsible for exp
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Increasing trans epithelial transport efficiency is another
2022-04-24
Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S
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Recent studies are beginning to explore this complex interpl
2022-04-24
Recent studies are beginning to explore this complex interplay of pathways. For example, intracellular trafficking of poly(lactic-co-glycolic acid)(PLGA) based nanoparticles was studied in detail using 30 different Rab proteins as markers for intracellular transport vesicles (involved in exocytosis,
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br Cellular transportation of nanoparticles
2022-04-24
Cellular transportation of nanoparticles and nanocomplexes Endocytosis and exocytosis are critically important phenomena in cellular metabolism, which involve the complex vesicular system. They deal with major cellular transportation activities including membrane homeostasis by transporting prote
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In addition to Rabs several proteins have been shown
2022-04-24
In addition to Rabs, several proteins have been shown to interact with Rabphilin3a, for instance the GluN2A subunit of the NMDA receptor, PSD-95 ([56,57] and references therein), Rabaptin-5, α-actinin [16] and SNAP-25 [21,23,41,61]. Only the latter has been reported to participate in the AR. Explori
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br Characterization of quantal exocytosis by amperometry A
2022-04-24
Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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Introduction Vesicular exocytosis an intracellular membrane
2022-04-24
Introduction Vesicular exocytosis, an intracellular membrane trafficking pathway, is a ubiquitous process for intercellular communication. It occurs when an intracellular vesicle fuses with the cell membrane and subsequently releases an infinitely minute number of chemical or biochemical messengers
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