TITLE

The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder

AUTHOR(S)
Soukup, Ondrej; Holas, Ondrej; Binder, Jir�; Killy, Kumar; Tobin, Gunnar; Jun, Daniel; Fusek, Josef; Kuca, Kamil
PUB. DATE
June 2010
SOURCE
Journal of Applied Biomedicine;Jun2010, Vol. 8 Issue 2, p1
SOURCE TYPE
Academic Journal
DOC. TYPE
Article
ABSTRACT
Trimedoxime is a bisquaternary oxime that is widely used in the treatment of organophosphorous poisoning caused by tabun and paraoxon. We tested its affinity to acetylcholinesterase (AChE), its mechanism of interaction and effect on the cholinergic system of the rat bladder. The half maximal inhibitory concentration (IC50) of trimedoxime to recombinant AChE was found to be 82.0 mM � 30.1 mM. This represents a weak inhibition. Its interaction with AChE seems to be very similar to obidoxime - one aromatic nucleus interacts with the peripheral anionic site and the other with the residues TYR337 and TYR341 inside the cavity. Also the oxime moiety is moving towards the catalytic triade ready for the reactivation of the inhibited AChE. In the organ bath experiment no significant effect of trimedoxime was observed on the contraction of the detrusor caused by the muscarinic agonist metacholine.
ACCESSION #
51974838

 

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