Abstract:
:Standard treatment of poisoning by organophosphorus (OP) nerve agents with atropine and oximes lacks efficacy with some nerve agents. Promising in vitro and in vivo results were obtained with the bispyridinium compound SAD-128 which was partly attributed to its interaction with nicotinic acetylcholine receptors. Previous studies indicate that bispyridinium compounds interact with muscarinic acetylcholine receptors as well. The muscarinic M(5) receptor is not well investigated compared to other subtypes, but could be important in the search for new drugs for treating nerve agent poisoning. A set of bispyridinium compounds structurally related to SAD-128 were tested in competition binding experiments with recombinant human M(5) muscarinic acetylcholine receptors. Five of the six investigated bispyridinium compounds interacted with the orthosteric binding site, with affinities in the low micromolar range. These data indicate that interaction of bispyridinium compounds with muscarinic receptors may contribute to their therapeutic efficacy.
journal_name
Drug Test Analjournal_title
Drug testing and analysisauthors
Niessen KV,Tattersall JE,Timperley CM,Bird M,Green C,Thiermann H,Worek Fdoi
10.1002/dta.410subject
Has Abstractpub_date
2012-03-01 00:00:00pages
292-7issue
3-4eissn
1942-7603issn
1942-7611journal_volume
4pub_type
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