Novel acetylcholinesterase reactivator K112 and its cholinergic properties

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F10%3A00002294" target="_blank" >RIV/60162694:G44__/10:00002294 - isvavai.cz</a>
Alternative codes found
RIV/60076658:12110/10:00012141 RIV/00023752:_____/10:00001074 RIV/68407700:21340/10:00163841
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
Novel acetylcholinesterase reactivator K112 and its cholinergic properties
Original language description
The oxime reactivator K112 is a member of the new group of xylene linker-containing AChE reactivators. Its cholinergic properties could be of importance at OP poisoning and are not related to the AChE reactivation that has been studied. It has been foundthat, despite of reactivating potency, this compound has additional effects. These cholinergic effects include a weak inhibition of AChE (IC(50)=43.8 +/- 4.88 ?M), inhibition of binding to the porcine muscarinic M2 receptor (IC(50)=4.36 ?M) and finally,the inhibition of HACU (68.4 +/- 9.9%), a key regulatory step in the synthesis of ACh. The inhibition of the binding of (3H)-HC-3 (64.7 +/- 4.7%) and the influence on the membrane fluidity have also been observed. Blocking properties of K112 on the muscarinic receptors have been revealed in the in vitro experiment (rat urinary bladder) and in the in vivo experiment (rat heart BPM) as well. All these cholinergic properties could significantly contribute to the antidotal effect of K112 at
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
IN - Informatics
OECD FORD branch
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Publication year
2010
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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