Abstract:
:Newly developed acetylcholinesterase reactivators K117 [1,5-bis(4-hydroxyiminomethylpyridinium)-3-oxapentane dichloride] and K127 [(1-(4-hydroxyiminomethylpyridinium)-5-(4-carbamoylpyridinium)-3-oxapentane dibromide)] were tested for their potency to reactivate tabun-inhibited human brain cholinesterases. Pralidoxime and trimedoxime were chosen as standard reference reactivators. Human tissue was used, as that was closer on the real treatment of human beings. As a result, oxime K127 was found as the best tested reactivator according to the constant k(r), characterizing the overall reactivation process. On the contrary, the maximal reactivation ability expressed as percentage of reactivation was the best for trimedoxime. This differences were caused as a result of using the enzyme from different species. Due to this, experiments on human tissue should be conducted after in vitro and in vivo tests on animals to eliminate such important failures of promising oximes.
journal_name
Basic Clin Pharmacol Toxicoljournal_title
Basic & clinical pharmacology & toxicologyauthors
Kuca K,Cabal J,Jung YS,Musilek K,Soukup O,Jun D,Pohanka M,Musilova L,Karasová J,Novotný L,Hrabinova Mdoi
10.1111/j.1742-7843.2009.00421.xsubject
Has Abstractpub_date
2009-09-01 00:00:00pages
207-10issue
3eissn
1742-7835issn
1742-7843pii
PTO421journal_volume
105pub_type
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