Naslov
Testing a new reactivator for phosphorylated human acetylcholinesterase

Autori
Kovarik, Zrinka ; Katalinić, Maja ; Lovrić, Jasna

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
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, 73-73

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

Mjesto i datum
München, Njemačka, 23.04.2009. - 24.04.2009

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
reactivators ; oximes ; tabun ; inhibition ; acetylcholinesterase ; paraoxon

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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