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Methylacridinium and its cholinergic properties.

Journal article
Authors Ondrej Soukup
Jan Proska
Jiri Binder
Jana Zdarova Karasova
Gunnar Tobin
Daniel Jun
Jan Marek
Kamil Musílek
Josef Fusek
Kamil Kuca
Published in Neurotoxicity research
Volume 16
Issue 4
Pages 372-7
ISSN 1029-8428
Publication year 2009
Published at Institute of Neuroscience and Physiology, Department of Pharmacology
Pages 372-7
Language en
Subject categories Pharmaceutical pharmacology


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. Using spectrophotometric Ellman's method at 436 nm and commercial enzymes we found that MA inhibits AChE by binding with relatively high potency to the peripheral anionic site (IC(50) = 1.68 +/- 0.14 muM; human recombinant AChE) and equally to its inhibition of butyrylcholinesterase (BuChE; IC(50) = 3.54 +/- 0.27 muM; BuChE from human serum). MA also inhibits the binding of [(3)H]N-methylscopolamine to the muscarinic M2 receptor subtype, possibly in an allosteric manner (IC(50) = 1.90 muM). 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.

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