Evaluation of the reactivating efficacy of selected reactivators of paraoxon-inhibited acetylcholinesterase in vitro
Authors:
O. Holas 1; K. Musílek 1,2; V. Opletalová 1; K. Kuča 2,3
Authors place of work:
Univerzita Karlova v Praze, Farmaceutická fakulta v Hradci Králové, Katedra farmaceutické chemie a kontroly léčiv
1; Univerzita obrany Brno, Fakulta vojenského zdravotnictví Hradec Králové, Katedra toxikologie
2; Univerzita obrany Brno, Fakulta vojenského zdravotnictví Hradec Králové, Centrum pokročilých studií
3
Published in the journal:
Čes. slov. Farm., 2010; 59, 18-22
Category:
Original Articles
Summary
Organophosphorus pesticides (OPs) are ranked among the group of highly toxic irreversible inhibitors of acetylcholinesterase (AChE). The causal drugs in OPs intoxications are oxime reactivators of AChE. The reactivating efficacy of five newly prepared bispyridinium reactivators of acetylcholinesterase was tested on a model of a paraoxon-inhibited enzyme. The reactivating efficacy was tested by means of the standard in vitro test, the laboratory rat brain homogenate being used as the source of acetylcholinesterase. The result were compared with five commercially available AChE reactivators.
Key words:
acetylcholinesterase – organophosphorus pesticide – reactivator – in vitro – SAR
Zdroje
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Štítky
Pharmacy Clinical pharmacologyČlánok vyšiel v časopise
Czech and Slovak Pharmacy
2010 Číslo 1
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