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| Titel: |
In vitro screening of blood-brain barrier penetration of clinically used acetylcholinesterase reactivators |
| Auteur: |
Jana Zdarova Karasova Petr Stodulka Kamil Kuca |
| Verschenen in: |
Journal of applied biomedicine |
| Paginering: | Jaargang 8 (2009) nr. 1 pagina's 35-40 |
| Jaar: |
2009 |
| Inhoud: |
In this in vitro study, using the HPLC method, we determined the ability of acetylcholinesterase (AChE)reactivators, used clinically, to penetrate the blood-brain barrier (BBB). We evaluated pralidoxime, HI-6,obidoxime, trimedoxime and methoxime – reactivators varying in the position of the oxime group on thepyridinium ring and linker connecting the pyridinium rings. Our results indicated that pralidoxime, amonoquaternary AChE reactivator, was the oxime with the most penetration. Molecular weight seems to bethe most important factor for passive transport through the BBB. From the structural perspective, theconnecting linker also plays a key role in the ability of the reactivators to penetrate the CNS. In this case, thesimple and short linker is favorable for permeation of these compounds. The location of the oxime group onthe pyridine ring may also influence passive transport into the brain; the best position of the oxime groupseems to be position four. |
| Uitgever: |
University of South Bohemia (provided by DOAJ) |
| Bronbestand: |
Elektronische Wetenschappelijke Tijdschriften |
Details van artikel 10 van 14 gevonden artikelen
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