Methylacridinium and its cholinergic properties

Result code in 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>
Alternative codes found
RIV/00216208:11160/09:00210089 RIV/44555601:13440/09:00004894
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
Methylacridinium and its cholinergic properties
Original language description
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.
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
FP - Other medical fields
OECD FORD branch
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Publication year
2009
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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