Methylacridinium and its cholinergic properties

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F09%3A00002181" target="_blank" >RIV/60162694:G44__/09:00002181 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11160/09:00210089 RIV/44555601:13440/09:00004894

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Methylacridinium and its cholinergic properties

Popis výsledku v původním jazyce

10-Methylacridinium iodide (methylacridinium; MA) is an inhibitor of cholinesterases. Inhibitors of acetylcholinesterase (AChE) are used in the treatment of myasthenia gravis, Alzheimer's disease, and in the prophylaxis of poisoning with organophosphates. We have found that MA inhibits AChE by binding with relatively high potency to the peripheral anionic site (IC50 = 1.68 +/- 0.14 mu M; human recombinant AChE) and equally to its inhibition of butyrylcholinesterase (BuChE; IC50 = 3.54 +/- 0.27 mu M; BuChE from human serum). MA also inhibits the binding of [H-3]N-methylscopolamine to the muscarinic M2 receptor subtype, possibly in an allosteric manner (IC50 = 1.90 mu M). Functional effects on both the enzyme and the receptor could be observed in contractile studies on the isolated rat bladder. The ability of MA to cross the blood-brain barrier (log P = -0.32; polar surface area 3.88) provides prerequisites for a potential use of the drug in the treatment of neural disorders.

Název v anglickém jazyce

Methylacridinium and its cholinergic properties

Popis výsledku anglicky

10-Methylacridinium iodide (methylacridinium; MA) is an inhibitor of cholinesterases. Inhibitors of acetylcholinesterase (AChE) are used in the treatment of myasthenia gravis, Alzheimer's disease, and in the prophylaxis of poisoning with organophosphates. We have found that MA inhibits AChE by binding with relatively high potency to the peripheral anionic site (IC50 = 1.68 +/- 0.14 mu M; human recombinant AChE) and equally to its inhibition of butyrylcholinesterase (BuChE; IC50 = 3.54 +/- 0.27 mu M; BuChE from human serum). MA also inhibits the binding of [H-3]N-methylscopolamine to the muscarinic M2 receptor subtype, possibly in an allosteric manner (IC50 = 1.90 mu M). Functional effects on both the enzyme and the receptor could be observed in contractile studies on the isolated rat bladder. The ability of MA to cross the blood-brain barrier (log P = -0.32; polar surface area 3.88) provides prerequisites for a potential use of the drug in the treatment of neural disorders.

Druh

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

CEP obor

FP - Ostatní lékařské obory

OECD FORD obor

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Projekt

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Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2009

Kód důvěrnosti údajů

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

Název periodika

Neurotoxicity Research

ISSN

1029-8428

e-ISSN

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Svazek periodika

16

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

6

Strana od-do

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Kód UT WoS článku

000271028000004

EID výsledku v databázi Scopus

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