Interaction of Organophosphorus Poisoning Antidotes with Muscarinic and Nitotinic Receptors

1 Summary in English Currently, organophosphorus (OP) poisoning is a threat particularly in war conflicts in connection with terrorism or a poisoning caused by OP pesticides in agriculture. The poisoning is caused by inhibition of the enzyme acetylcholinesterase (AChE), which, under physiological conditions, cleaves acetylcholine (ACh) and regulates the transmission of nerve signals. The inhibition of AChE leads to excessive stimulation of cholinergic receptors and clinically it manifests as so-called cholinergic syndrome. According to the structures affected, symptoms are divided into nicotinic, muscarinic and central. Organophosphates are lethal compounds, when death is caused by suffocation. Current treatment is mainly based on the application of anticholinergics (atropine) and /or on the application of AChE oxime reactivators (HI-6, obidoxime, pralidoxime etc.) Atropine inhibits excessive neural transmission by blocking muscarinic receptors. However, it is only symptomatic cure not causal. Whereas oximes, which represent a causal therapy, are able to unbind an OP compound from the AChE and restore its splitting function. Using reactivators has two major drawbacks; there is no universal reactivator against all types of OP compounds (soman, sarin, paraoxon etc.) and reactivation is possible only within a..