Time-Course Changes of Acetylcholinesterase Activity in Blood and Some Tissues in Rats After Intoxication by Russian VX
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The toxic effect of organophosphates is attributed to irreversible inhibition of acetylcholinesterase (AChE; EC 22.214.171.124), the enzyme that hydrolyses the neurotransmitter acetylcholine. Inhibition potency in vivo of one of the most toxic nerve agents—Russian VX (RVX; N,N-diethyl-2-[methyl-(2-methylpropoxy)phosphoryl]sulfanylethanamine) (1 × LD50 dose administered intramuscularly, i.m.) was studied in rats. AChE in blood was inhibited by 50%, 3 min after i.m. RVX. Butylcholinesterase (BChE; EC 126.96.36.199) in plasma was inhibited less rapidly and only by 10–20%, 20 min after RVX. AChE and BChE activities in diaphragm were reduced only 35% and 15% at 30 min. While AChE and BChE activities were reduced only about 20% and 15%, respectively, the decline in activity was rapid, occurring within 3 min. These findings indicate that RVX most potently inhibits ChE outside the central nervous system.