Issue 3, 2012
From the journal:

MedChemComm

1,1′-(Propane-1,3-diyl)bis(4-tert-butylpyridinium) di(methanesulfonate) protects guinea pigs from soman poisoning when used as part of a combined therapy

Christopher M. Timperley,*a   Mike Bird,a   Christopher Green,b   Matthew E. Price,b   John E. Chad,c   Simon R. Turner†bc  and  John E. H. Tattersallb  

* Corresponding authors

a Detection Department, Dstl Porton Down, Salisbury, Wiltshire, UK
E-mail: cmtimperley@dstl.gov.uk
Fax: +44 1980 617523
Tel: +44 1980 613566

b Biomedical Sciences Department, Dstl Porton Down, Salisbury, Wiltshire, UK

c School of Biological Sciences, University of Southampton, UK

Abstract

Syntheses of 1,1-(propane-1,3-diyl)bis(4-tert-butylpyridinium) diiodide (MB327) and its di(methanesulfonate) salt (MB399) are described. Protection experiments in guinea-pigs showed that MB399, a noncompetitive nicotinic antagonist that produces fast open channel block at the ion channel of the nicotinic acetylcholine receptor, is able to improve survival of animals poisoned with the organophosphorus nerve agent soman when used therapeutically in combination with hyoscine and physostigmine. Successful anti-nicotinic therapy, a novel approach to the treatment of nerve agent poisoning, may offer a revolutionary improvement in nerve agent countermeasures compared to the current optimisation of existing pharmacological approaches.

Graphical abstract: 1,1′-(Propane-1,3-diyl)bis(4-tert-butylpyridinium) di(methanesulfonate) protects guinea pigs from soman poisoning when used as part of a combined therapy

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Article information

DOI
https://doi.org/10.1039/C2MD00258B
Article type
Concise Article
Submitted
12 Oct 2011
Accepted
28 Nov 2011
First published
19 Dec 2011

Med. Chem. Commun., 2012,3, 352-356

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1,1′-(Propane-1,3-diyl)bis(4-tert-butylpyridinium) di(methanesulfonate) protects guinea pigs from soman poisoning when used as part of a combined therapy

C. M. Timperley, M. Bird, C. Green, M. E. Price, J. E. Chad, S. R. Turner and J. E. H. Tattersall, Med. Chem. Commun., 2012, 3, 352 DOI: 10.1039/C2MD00258B

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