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The effect of HI-6 on cholinesterases and on the cholinergic system of the rat bladder.

Journal article
Authors Ondrej Soukup
Miroslav Pohanka
Gunnar Tobin
Daniel Jun
Josef Fusek
Kamil Musilek
Jan Marek
Jiri Kassa
Kamil Kuca
Published in Neuro endocrinology letters
Volume 29
Issue 5
Pages 759-62
ISSN 0172-780X
Publication year 2008
Published at Institute of Neuroscience and Physiology, Department of Pharmacology
Pages 759-62
Language en
Links www.ncbi.nlm.nih.gov/entrez/query.f...
Subject categories Pharmacology

Abstract

OBJECTIVES: The current standard treatment of organophosphate poisoning consists of an administration of anticholinergic drugs and cholinesterase reactivators (oximes). Oximes can react - except their reactivating effect on cholinesterases - directly with cholinoreceptors. HI-6 is an oxime that may have an inhibitory effect on the muscarinic receptors, too. METHODS: In our work, we have investigated an influence of HI-6 on the acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and on the muscarinic receptors in vitro. The study was conducted using biosensor technique and on the rat bladder using in vitro test (tissue bath; methacholine as muscarinic agonist). IC50 for BChE from human serum was determined to be 1.01x10-6 M and for human erythrocytes AChE 3.31x10-6 M, respectively. CONCLUSION: We assume that the demonstrated contractile response can be attributed to the inhibition of the AChE at the lower concentration and to a predominant inhibition of muscarinic receptor at higher concentration of compound tested.

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