In Search of an Effective in vivo Reactivator for Organophosphorus Nerve Agent-Inhibited Acetylcholinesterase in the Central Nervous System.

摘要

Organophosphorus nerve agents irreversibly inhibit the enzyme acetylcholinesterase (AChE), leading to excessive cholinergic neurotransmission and causing toxic lethal consequences. Current nerve agent therapies in the U.S. include 2-pralidoxime to reactivate inhibited AChE. Due to its quaternary structure, this oxime does not readily cross the blood brain barrier (BBB) to reactivate brain AChE and to mitigate CNS toxicity.