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Drug penetration across the BBB is influenced by several mechanisms, such as passive diffusion, active influx, and active efflux.
Although there was variability in this limited dataset, BBB kinetics were consistent with passive diffusion or active influx.
For non-primary active influx transporters, the kinetics can be measured via uptake assay using intact cells.
Active influx and efflux are processes that can transport molecules against a concentration gradient, hence requiring ATP-provided energy.
In primate and human PET studies designed to evaluate the transport of a novel M1 allosteric agonist (GSK1034702) across the BBB, we have demonstrated good brain uptake and BBB passage consistent with passive diffusion or active influx.
The tight junctions between endothelial cells of the BBB force drugs to penetrate through rather than between these cells, either by passive diffusion, active influx or active efflux [1, 2].
Similar(45)
The bicarbonate sensitive pathway is the most important mechanism for active lithium influx into the cell [ 90].
A possible scenario is that the PSY-induced raft disruption can also change the overall membrane Ca2+ permeability and/or determine an active Ca2+ influx mediated by channels anchored to lipid rafts.
In general, possible explanations for other underpredicted outliers in our models could be that they undergo active transport (by influx or efflux transporters) or exhibit specific binding to some tissues, or they are stored in subcellular compartments in specific tissues.
This resting state is converted to a fluid, active state by influx of Na+.
Combinations of active and passive processes (influx and efflux, respectively, for some anions;(1050) efflux and influx, respectively, for Type II cations, 1058) both described in section ) were observed in the tubular epithelium of the nephron.
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