PMID: 11311445Apr 20, 2001Paper

Effects of chronic metrifonate treatment on cholinergic enzymes and the blood-brain barrier

Neurochemistry International
Z Rakonczay, H Papp

Abstract

After an acute (4 h) treatment with an irreversible cholinesterase inhibitor organophosphate, metrifonate (100 mg/kg i.p.), the activities of both acetyl- and butyrylcholinesterase were inhibited (66.0-70.7% of the control level) in the rat brain cortex and hippocampus. There were no significant changes in the acetyl- and butyrylcholinesterase activities in the olfactory bulb, or in the choline acetyltransferase activity in all three brain areas. After chronic (2 or 5 week) metrifonate treatment (100 mg/kg daily i.p.), the activities of both cholinesterases were substantially inhibited in the rat brain cortex and hippocampus (15.8-31.8% of the control levels), but there was no inhibition of the choline acetyltransferase activity. Moreover, chronic metrifonate treatment did not have any effect on the distribution of the acetylcholinesterase molecular forms. In vitro, metrifonate proved to be a more potent inhibitor of butyryl- than of acetylcholinesterase in both the cortex and the hippocampus. In the hippocampus, the butyrylcholinesterase activity was twice as sensitive to metrifonate inhibition as that in the cortex (IC50 values 0.22 and 0.46 microM, respectively). The effects of chronic (5 week) metrifonate treatment on the b...Continue Reading

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Citations

Aug 19, 2007·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Betul Karademir CatalgolBuket Alpertunga
Dec 12, 2002·Journal of Toxicology. Clinical Toxicology·J Kassa
Sep 29, 2011·Toxicology Mechanisms and Methods·Miroslav PohankaJiri Pikula

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