Novel acetylcholinesterase reactivator K112 and its cholinergic properties

Kód výsledku v 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>

Nalezeny alternativní kódy

RIV/60076658:12110/10:00012141 RIV/00023752:_____/10:00001074 RIV/68407700:21340/10:00163841

Výsledek na webu

—

DOI - Digital Object Identifier

—

Jazyk výsledku

angličtina

Název v původním jazyce

Novel acetylcholinesterase reactivator K112 and its cholinergic properties

Popis výsledku v původním jazyce

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

Název v anglickém jazyce

Novel acetylcholinesterase reactivator K112 and its cholinergic properties

Popis výsledku anglicky

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

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

IN - Informatika

OECD FORD obor

—

Projekt

—

Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2010

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Biomedicine and Pharmacotherapy

ISSN

0753-3322

e-ISSN

—

Svazek periodika

64

Číslo periodika v rámci svazku

8

Stát vydavatele periodika

FR - Francouzská republika

Počet stran výsledku

5

Strana od-do

—

Kód UT WoS článku

000283571100006

EID výsledku v databázi Scopus

—