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Testing a new reactivator for phosphorylated human acetylcholinesterase (CROSBI ID 547101)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | međunarodna recenzija

Kovarik, Zrinka ; Katalinić, Maja ; Lovrić, Jasna Testing a new reactivator for phosphorylated human acetylcholinesterase // 12th Medical Chemical Defence Conference 2009: Current status of bioanalytical detection of chemical warfare agents and antidotes, Munchen, Njemačka. München: Bundeswehr Institute of Pharmacology and Toxicology, 2009. str. 73-73

Podaci o odgovornosti

Kovarik, Zrinka ; Katalinić, Maja ; Lovrić, Jasna

engleski

Testing a new reactivator for phosphorylated human acetylcholinesterase

For the treatment of organophosphorus compound poisoning, currently used therapy consists of a combination of an acetylcholine-receptor agonist, e.g. atropine, and an acetylcholinesterase reactivator, oxime. Atropine decreases effects of excess acetylcholine by blocking peripheral muscarinic receptor sites resulting in secretion reduction and reversing constriction of smooth muscles. On the other hand, oximes as reactivators break the organophosphate-AChE bond and restore the activity of inhibited AChE. For this reason, we synthesized a new compound, ATP-4-OX, as a combination of atropin and pyridinium oxime, and tested its potency to reactivate tabun- and paraoxon-inhibited human erythrocyte AChE. Reactivation of paraoxon-inhibited AChE was very efficient. 100 % of AChE activity was restored after only 20 min even when lower concentration of this compound was applied. The overall reactivation rate constant, kr, was about 2000 min-1M-1. Opposite to paraoxon, ATP-4-OX was not efficient in reactivation of tabun-inhibited AChE (kr = 67 min-1M-1). The reactivation was slow and the maximum of 90 % was obtained in 7 h. Despite limiting reactivation potency for tabun, the ATP- 4-OX seems to be promising in counteracting pesticides.

reactivators ; oximes ; tabun ; inhibition ; acetylcholinesterase ; paraoxon

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Podaci o prilogu

73-73.

2009.

objavljeno

Podaci o matičnoj publikaciji

12th Medical Chemical Defence Conference 2009: Current status of bioanalytical detection of chemical warfare agents and antidotes, Munchen, Njemačka

München: Bundeswehr Institute of Pharmacology and Toxicology

Podaci o skupu

12th Medical Chemical Defence Conference 2009: Current status of bioanalytical detection of chemical warfare agents and antidotes, Munich, Germany

poster

23.04.2009-24.04.2009

München, Njemačka

Povezanost rada

Kemija