| Passive diffusion of acetylcholinesterase oxime reactivators through the blood-brain barrier: influence of molecular structure. | |
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MedLine Citation:
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PMID: 20546883 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In this in vitro study, high-performance liquid chromatography (HPLC) was used to determinate the penetration of 30 acetylcholinesterase (AChE) reactivators through the blood-brain barrier (BBB). According to our method, monoquaternary AChE reactivators were found to be able to penetrate the BBB. In addition to molecular structure, molecular weight appears to be an important factor for passive transport of oximes through the BBB. For bisquaternary reactivators, the connecting linker plays a key role in the ability to penetrate into the central nervous system (CNS): simple, short linkers tend to facilitate permeation. The location of groups on the pyridine ring also influences passive transport into the brain; the optimum position of the oxime group was found to be position four (para) and substitution of the oxime group on the pyridine ring by carbamoyl or amidoxime group markedly decreased penetration of AChE reactivators into the CNS. |
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Authors:
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Jana Zdarova Karasova; Miroslav Pohanka; Kamil Musilek; Filip Zemek; Kamil Kuca |
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Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't Date: 2010-05-26 |
Journal Detail:
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Title: Toxicology in vitro : an international journal published in association with BIBRA Volume: 24 ISSN: 1879-3177 ISO Abbreviation: Toxicol In Vitro Publication Date: 2010 Sep |
Date Detail:
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Created Date: 2010-08-31 Completed Date: 2010-12-14 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8712158 Medline TA: Toxicol In Vitro Country: England |
Other Details:
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Languages: eng Pagination: 1838-44 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Toxicology, Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic. karasova@pmfhk.cz |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Biological Markers Biological Transport Blood-Brain Barrier / metabolism* Cholinesterase Reactivators / chemistry, pharmacokinetics* Chromatography, High Pressure Liquid Diffusion Membranes, Artificial* Molecular Structure Oximes / chemistry, pharmacokinetics* Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Biological Markers; 0/Cholinesterase Reactivators; 0/Membranes, Artificial; 0/Oximes |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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