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In vitro reactivation of trichlorfon-inhibited butyrylcholinesterase using HI-6, obidoxime, pralidoxime and K048.
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- Author(s): Pohanka M;Pohanka M; Jun D; Kuca K
- Source:
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2009 Jun; Vol. 24 (3), pp. 680-3.
- Publication Type:
Journal Article; Research Support, Non-U.S. Gov't
- Language:
English
- Additional Information
- Source:
Publisher: Taylor & Francis Country of Publication: England NLM ID: 101150203 Publication Model: Print Cited Medium: Internet ISSN: 1475-6374 (Electronic) Linking ISSN: 14756366 NLM ISO Abbreviation: J Enzyme Inhib Med Chem Subsets: MEDLINE
- Publication Information:
Original Publication: Basingstoke, UK : Taylor & Francis, c2002-
- Subject Terms:
- Abstract:
Trichlorfon is a specific inhibitor of cholinesterases. It was typically used as an insecticide; however, trichlorfon was described as useful for symptomatic treatment of Alzheimer's disease some years ago. The presented study is aimed at reactivation of trichlorfon-inhibited butyrylcholinesterase since this enzyme play an important role in Alzheimer's disease as deputy for acetylcholinesterase and furthermore it could be applied as a scavenger in case of overdosing. We used in vitro reactivation test for considering only reactivation efficacy of butyrylcholinesterase that is inhibited by trichlorfon and not reactivation of butyrylcholinesterase inhibited by trichlorfon metabolic products. Four reactivators were used: HI-6, pralidoxime, obidoxime, and K048. Although all of the reactivators seem to be effective at 1 mM concentration, a lower concentration was not able ensure sufficient reactivation. There was also an observed lowering of reactivation efficacy when butyrylcholinesterase was exposed to trichlorfon for a longer time interval.
- Accession Number:
0 (1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane)
0 (Cholinesterase Inhibitors)
0 (Cholinesterase Reactivators)
0 (Oximes)
0 (Pralidoxime Compounds)
0 (Pyridinium Compounds)
3HXR312Z9M (Obidoxime Chloride)
DBF2DG4G2K (Trichlorfon)
EC 3.1.1.7 (Acetylcholinesterase)
EC 3.1.1.8 (Butyrylcholinesterase)
HUV88P6SJS (asoxime chloride)
P7MU9UTP52 (pralidoxime)
- Publication Date:
Date Created: 20081001 Date Completed: 20101012 Latest Revision: 20171116
- Publication Date:
20240829
- Accession Number:
10.1080/14756360802328315
- Accession Number:
18825528
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