Int. J. Mol. Sci. 2009, 10(7), 3065-3075; doi:10.3390/ijms10073065
Article

Effect of Seven Newly Synthesized and Currently Available Oxime Cholinesterase Reactivators on Cyclosarin-Intoxicated Rats

1 Department of Toxicology, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic 2 Center of Advanced Studies, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic 3 Department of Chemistry, Faculty of Sciences, J.E. Purkinje University, Horeni 13, 400 96, Usti nad Labem, Czech Republic
* Author to whom correspondence should be addressed.
Received: 27 May 2009; in revised form: 24 June 2009 / Accepted: 6 July 2009 / Published: 7 July 2009
(This article belongs to the Section Molecular Toxicology)
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Abstract: Seven new oxime-based acetylcholinesterase reactivators were compared with three currently available ones (obidoxime, trimedoxime, HI-6) for their ability to lessen cholinesterase inhibition in blood and brain of cyclosarin-treated rats. Oximes were given at doses of 5% their LD50 along with 21 mg/kg atropine five min before the LD50 of cyclosarin (120 ug/kg) was administered. Blood and brain samples were collected 30 minutes later. The greatest difference between acetylcholinesterase inhibition in blood of cyclosarin-treated rats was found after administration of HI-6 (40%), compared to 22% for trimedoxime and 6% for obidoxime. Only two of the seven newly synthesized oximes had any effect (K203 at 7%, K156 at 5%). Effective oximes against cyclosarin-inhibited plasma butyrylcholinesterase were HI-6 (42%), trimedoxime (11%), and K156 (4%). The oximes were less effective in brain than in blood, with reactivation values for HI-6 30% against acetylcholinesterase and 10% against butyrylcholinesterase. Values for newly synthesized oximes were less than 10% for K206, K269 and K203.
Keywords: acetylcholinesterase; butyrylcholinesterase; reactivators; oximes; cyclosarin

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MDPI and ACS Style

Karasova, J.Z.; Kassa, J.; Musilek, K.; Pohanka, M.; Novotny, L.; Kuca, K. Effect of Seven Newly Synthesized and Currently Available Oxime Cholinesterase Reactivators on Cyclosarin-Intoxicated Rats. Int. J. Mol. Sci. 2009, 10, 3065-3075.

AMA Style

Karasova JZ, Kassa J, Musilek K, Pohanka M, Novotny L, Kuca K. Effect of Seven Newly Synthesized and Currently Available Oxime Cholinesterase Reactivators on Cyclosarin-Intoxicated Rats. International Journal of Molecular Sciences. 2009; 10(7):3065-3075.

Chicago/Turabian Style

Karasova, Jana Zdarova; Kassa, Jiri; Musilek, Kamil; Pohanka, Miroslav; Novotny, Ladislav; Kuca, Kamil. 2009. "Effect of Seven Newly Synthesized and Currently Available Oxime Cholinesterase Reactivators on Cyclosarin-Intoxicated Rats." Int. J. Mol. Sci. 10, no. 7: 3065-3075.

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