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| 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 |
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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