Effect of P-glycoprotein on the availability of oxime reactivators in the brain

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F20%3A00556186" target="_blank" >RIV/60162694:G44__/20:00556186 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/20:10418532
Result on the web
<a href="https://www.sciencedirect.com/science/article/abs/pii/S0300483X20301803?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/abs/pii/S0300483X20301803?via%3Dihub</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.tox.2020.152541" target="_blank" >10.1016/j.tox.2020.152541</a>

Result language
angličtina
Original language name
Effect of P-glycoprotein on the availability of oxime reactivators in the brain
Original language description
The ability to overcome cellular barriers in the body is crucial for efficient delivery of drugs to the target where intervention is needed. For drugs acting in the brain it is essential to overcome the blood-brain barrier (BBB). Such drugs include antidotes for the treatment of organophosphate poisoning, a current warfare and terroristic threat. Being lipophilic compounds, organophosphates readily penetrate the brain and block the enzyme acetylcholinesterase (AChE). They cause severe symptoms which may have fatal consequences. A major drawback of currently available oxime reactivators is their inability to reactivate AChE in the central nervous system (CNS) as they are unable to cross the blood-brain barrier. An important obstacle preventing many drugs from reaching their therapeutic target in the brain is the efflux transporter P-glycoprotein (P-gp), whose function is to prevent the penetration of potentially harmful substances. The aim of this study was to evaluate the effect of P-gp on the permeation of oximes into the brain. The study of this interaction was carried out on the CACO-2 cell line, stably expressing P-gp. As it turned out, P-gp has no essential influence on the central availability of clinically used oxime reactivators within this study.
Czech name
—
Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
30108 - Toxicology

Project
<a href="/en/project/NV17-32801A" target="_blank" >NV17-32801A: Centrally acting antidotes for the treatment of organophosphorus poisoning</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

Publication year
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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