High efflux ratio
Web5 de dez. de 2024 · P-glycoprotein (P-gp) is a major blood-brain barrier (BBB) efflux transporter. In vitro approaches, including bi-directional efflux ratio (ER), are used to measure P-gp-mediated transport, but findings can be inconsistent across models. We propose a novel, more physiologically relevant, in vitro model: uni-directional apical … WebIn vitro approaches, including bidirectional efflux ratio (ER), are used to measure P-gp-mediated transport, but findings can be inconsistent across models. We propose a novel, more physiologically relevant, in vitro model: unidirectional apical efflux ratio (AP-ER)-a ratio of permeability rates at the apical side of the BBB with and without P-gp inhibitor.
High efflux ratio
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Web29 de mai. de 2024 · What does a high efflux ratio mean? If the efflux ratio is greater than two then this indicates drug efflux is occurring. Talinolol, a known P-gp substrate, is … Web1 de mar. de 2010 · A high efflux ratio in vitro has been shown to correlate well with studies that have demonstrated a role for P-gp in drug penetration to the central nervous system in mice 26,27.
Web30 de out. de 2024 · Selonsertib exhibited high apparent permeability in the absorptive direction and high efflux ratio in Caco-2 cell monolayers, but moderate to low permeability and extremely high efflux ratio in MDR-MDCK cells. These results suggest that selonsertib may show limited distribution to the brain compared to intestinal absorption. Web18 de jul. de 2014 · Higher efflux ratio and lower BBB penetration of FLZ were showed under pathology model (Ad and Bd). To examine the contribution of P-gp and BCRP to …
WebGiven the obtained efflux ratio for quinic acid is above the cut-off value of two and the comparison with digoxin ... the overall intestinal absorption will be moderately low due to the involved active efflux mechanism. High concentrations of quinic acid in human plasma and urine following coffee consumption have been described. 34 However, ... Web16 de abr. de 2012 · High permeability and reduced efflux ratio generally correlate with low polar surface area (PSA) and high lipophilicity (cLogP). 30, 31 The P5 lactam provided an opportunity to further reduce PSA ...
Web31 de dez. de 2010 · Digoxin is certainly a sensitive probe substrate of P-gp in in vitro studies, as evidenced by a high efflux ratio across Caco-2, MDR1-MDCK and MDR1-LLCPK1 cells, as well as effective inhibition of ...
WebCaco-2 cells were used to compare P-gp mediated efflux and passive permeability using bidirectional transport of 11 antihistamines. An efflux ratio >2 indicated active efflux, … chip le grand bookWeb20 de ago. de 2024 · Based on in vitro/in vivo correlation studies, Papp values obtained from Caco-2 barrier studies are used to define and predict the intestinal permeability of the tested compounds. In vitro Papp values. Range of predicted in vivo absorption. Papp ≤ 10-6 cm/s. Low (0-20%) 10-6cm/s < Papp ≤ 10 x 10-6 cm/s. Medium (20-70%) chip lembergWebHigh Permeability Standard Moderate Permeability Standard Name of the Analyte/Internal Standard Analytical Method Description ... Efflux Ratio (B-to-A)/(A-to-B) Table 11. chip le grand twitterWebA bi-directional Caco-2 permeability assay is performed where the transport of the compound is measured in the apical to basolateral direction as well as the basolateral to … grants for bed and breakfastWeb20 de jan. de 2005 · Inhibition of P-gp by cyclosporin A (CsA) significantly reduced secretory flux of compounds known to be P-pg substrates, but only enhanced the absorptive flux of … grants for becoming a teacherWeb1 de nov. de 2013 · Discussion. This suggests that a compound with an efflux ratio of < 5 is at lower risk of having significant biliary clearance and that Caco-2 efflux ratio obtained from a high throughput screening assay may be used as an early indicator of biliary excretion.Although, we propose to reduce the occurrence of false positive prediction for … grants for beef processing facilitiesWeb27 de nov. de 2024 · The high efflux ratios were reduced in the presence of PSC833 and verapamil (P-gp specific inhibitors) as well as fumitremorgin C and Ko134 (BCRP specific inhibitors), and the efflux ratio ... chip lenihan obituary