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Effect of Seven Newly Synthesized and Currently Available Oxime Cholinesterase Reactivators on Cyclosarin-Intoxicated Rats
Department of Toxicology, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic
Center of Advanced Studies, Faculty of Military Health Sciences, Hradec Kralove, Czech Republic
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
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.
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.
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.