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

Ondrej Soukup, Ondrej Holas, Jiri Binder, Kumar Killy, Gunnar Tobin, Daniel Jun, Josef Fusek, Kamil Kuca

. 2010 ; 8 (2) : 87-92.

Jazyk angličtina Země Česko

Perzistentní odkaz   https://www.medvik.cz/link/bmc10014968

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.

Citace poskytuje Crossref.org

Bibliografie atd.

Lit.: 23

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