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

Journal article
Authors Ondrej Soukup
Ondrej Holas
Jiri Binder
Uday Kumar Killi
Gunnar Tobin
Daniel Jun
Josef Fusek
Kamil Kuca
Published in Journal of Applied Biomedicine
Volume 8
Issue 2
Pages 87-92
ISSN 1214-021X
Publication year 2010
Published at Institute of Neuroscience and Physiology, Department of Pharmacology
Pages 87-92
Language en
Links dx.doi.org/10.2478/v10136-009-0008-...
Keywords acetylcholinesterase, trimedoxime, antidote, muscarinic receptors, reactivation
Subject categories Pharmacology

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.

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