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

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About: The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	We tested the affinity of tridoxime 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, e.g 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, 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. We tested the affinity of tridoxime 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, e.g 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, 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. (en)
Title	The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder (en)
skos:prefLabel	The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder The effect of trimedoxime on acetylcholinesterase and on the cholinergic system of the rat bladder (en)
skos:notation	RIV/60162694:G44__/10:00002293!RIV11-MO0-G44_____
http://linked.open...avai/riv/aktivita	I Z
http://linked.open...avai/riv/aktivity	I, Z(MO0FVZ0000604)
http://linked.open...iv/cisloPeriodika	8
http://linked.open...vai/riv/dodaniDat	2011
http://linked.open...aciTvurceVysledku	Soukup, Ondřej Jun, Daniel Fusek, Josef Kuča, Kamil
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ministerstvo obrany / Univerzita obrany - Fakulta vojenského zdravotnictví Hradec Králové
http://linked.open...dnocenehoVysledku	256227
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/10:00002293
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acetylcholinesterase; trimedoxime; antidote; muscarinic receptors; reactivation (en)
http://linked.open.../riv/klicoveSlovo	muscarinic receptors acetylcholinesterase reactivation trimedoxime antidote
http://linked.open...odStatuVydavatele	CZ - Česká republika
http://linked.open...ontrolniKodProRIV	[346142596D52]
http://linked.open...i/riv/nazevZdroje	Journal of Applied Biomedicine - print
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...UplatneniVysledku	2010
http://linked.open...v/svazekPeriodika	2010
http://linked.open...iv/tvurceVysledku	Kuča, Kamil Fusek, Josef Jun, Daniel Soukup, Ondřej Tobin, Gunnar Holas, Ondřej Binder, Jiří Killi, Kumar Uday
http://linked.open...ain/vavai/riv/wos	000277970800005
http://linked.open...n/vavai/riv/zamer	Informační zabezpečení krizového managementu pro oblast zdravotnictví
issn	1214-021X
number of pages	6 (xsd:int)
http://localhost/t...ganizacniJednotka	G44

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