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2011 | 58 | 2 | 193-198
Article title

A conjugate of pyridine-4-aldoxime and atropine as a potential antidote against organophosphorus compounds poisoning

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EN
Abstracts
EN
A conjugate of pyridine-4-aldoxime and atropine (ATR-4-OX) was synthesized and its antidotal efficiency was tested in vitro on tabun- or paraoxon-inhibited acetylcholinesterase (AChE) of human erythrocytes as well as in vivo using soman-, tabun- or paraoxon-poisoned mice. Its genotoxic profile was assessed on human lymphocytes in vitro and was found acceptable for further research. ATR-4-OX showed very weak antidotal activity, inadequate for soman or tabun poisoning. Conversely, it was effective against paraoxon poisoning both in vitro and in vivo. All animals treated with 5 % or 25 % LD50 doses of the new oxime survived after administration of 10.0 or 16.0 LD50 doses of paraoxon, respectively. Based on the persistence of toxicity symptoms in mice, the atropine moiety had questionable effects in attenuating such symptoms. It appears that ATR-4-OX has a therapeutic effect related to the reactivation of phosphylated AChE, but not to receptor antagonization.
Publisher

Year
Volume
58
Issue
2
Pages
193-198
Physical description
Dates
published
2011
received
2010-09-23
revised
2011-05-12
accepted
2011-06-09
(unknown)
2011-06-13
Contributors
author
  • University of Zagreb, School of Medicine, Zagreb, Croatia
author
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
  • Institute for Medical Research and Occupational Health, Zagreb, Croatia
author
  • Galapagos Research Centre d.o.o., Zagreb, Croatia
author
  • Galapagos Research Centre d.o.o., Zagreb, Croatia
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Document Type
Publication order reference
Identifiers
YADDA identifier
bwmeta1.element.bwnjournal-article-abpv58p193kz
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