| Literature DB >> 19728005 |
Jana Zdarova Karasova1, Jiri Bajgar, Daniel Jun, Ruzena Pavlikova, Kamil Kuca.
Abstract
The toxic effect of organophosphates is attributed to irreversible inhibition of acetylcholinesterase (AChE; EC 3.1.1.7), 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 x LD(50) 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 3.1.1.8) 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.Entities:
Mesh：
Substances：
Year: 2009 PMID： 19728005 DOI： 10.1007/s12640-009-9102-5
Source DB: PubMed Journal: Neurotox Res ISSN： 1029-8428 Impact factor: 3.911