Organophosphates inactivate acetylcholinesterase (AChE) by reacting covalently with the active center serine, thus inhibiting its action of hydrolyzing acetylcholine at central and peripheral synapses. Acetylcholine accumulation results in an over-stimulation of cholinergic receptors, which can disrupt numerous biological functions. Asoxime is an asymmetric bis-pyridinium aldoxime that functions as an AChE reactivator through nucleophilic attack of oximate anions on organophosphate-AChE conjugates. It demonstrates therapeutic activity in experimental models of organophosphate poisoning, by reactivating phosphorylated AChE that was inhibited as a result of exposure to various cytotoxic nerve agents.
