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.
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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.