Literature DB >> 15008517

A comparison of the ability of a new bispyridinium oxime--1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane dibromide and currently used oximes to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods.

K Kuca1, J Kassa.   

Abstract

The efficacy of a new bispyridinium oxime 1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane dibromide, called K048, and currently used oximes (pralidoxime, obidoxime, the oxime HI-6) to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun, cyclosarin, VX) was tested by in vitro methods. The new oxime K048 was found to be a more efficacious reactivator of nerve agent-inhibited acetylcholinesterase than pralidoxime (in the case of VX, tabun and cyclosarin), obidoxime (cyclosarin and tabun) and HI-6 (tabun) but it did not reach the efficacy of currently used oximes for the reactivation of acetylcholinesterase inhibited by sarin. Thus, the oxime K048 seems to be a relatively efficacious broad spectrum acetylcholinesterase reactivator and, therefore, it could be useful for the treatment of a nerve agent-exposed population if information about detection of the type of nerve agent is not available.

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Year:  2003        PMID: 15008517     DOI: 10.1080/14756360310001605552

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  12 in total

1.  Reactivation of organophosphate-inhibited acetylcholinesterase by quaternary pyridinium aldoximes.

Authors:  Kamil Kuca; Jirí Patocka; Jirí Cabal; Daniel Jun
Journal:  Neurotox Res       Date:  2004       Impact factor: 3.911

2.  The present approaches to the development of prophylactic and therapeutic antidotes against nerve agents.

Authors:  Jiří Kassa; Jiří Bajgar; Kamil Kuča; Kamil Musílek; Jana Karasová
Journal:  Interdiscip Toxicol       Date:  2008-06

3.  Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes.

Authors:  Kamil Kuca; Daniel Jun
Journal:  J Med Toxicol       Date:  2006-12

4.  The influence of oxime and anticholinergic drug selection on the potency of antidotal treatment to counteract acute toxic effects of tabun in mice.

Authors:  Jirí Kassa
Journal:  Neurotox Res       Date:  2006-01       Impact factor: 3.911

5.  In vitro reactivation potency of acetylcholinesterase reactivators--K074 and K075--to reactivate tabun-inhibited human brain cholinesterases.

Authors:  Kamil Kuca; Jiri Cabal; Daniel Jun; Kamil Musilek
Journal:  Neurotox Res       Date:  2007-02       Impact factor: 3.911

6.  In vitro ability of currently available oximes to reactivate organophosphate pesticide-inhibited human acetylcholinesterase and butyrylcholinesterase.

Authors:  Daniel Jun; Lucie Musilova; Kamil Musilek; Kamil Kuca
Journal:  Int J Mol Sci       Date:  2011-03-23       Impact factor: 5.923

7.  Oximes: inhibitors of human recombinant acetylcholinesterase. A structure-activity relationship (SAR) study.

Authors:  Vendula Sepsova; Jana Zdarova Karasova; Jan Korabecny; Rafael Dolezal; Filip Zemek; Brian J Bennion; Kamil Kuca
Journal:  Int J Mol Sci       Date:  2013-08-16       Impact factor: 5.923

8.  A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase.

Authors:  Kamil Kuca; Kamil Musilek; Daniel Jun; Jana Zdarova-Karasova; Eugenie Nepovimova; Ondrej Soukup; Martina Hrabinova; John Mikler; Tanos C C Franca; Elaine F F Da Cunha; Alexandre A De Castro; Martin Valis; Teodorico C Ramalho
Journal:  BMC Pharmacol Toxicol       Date:  2018-02-21       Impact factor: 2.483

9.  Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study.

Authors:  David Malinak; Eugenie Nepovimova; Daniel Jun; Kamil Musilek; Kamil Kuca
Journal:  Molecules       Date:  2018-09-07       Impact factor: 4.411

Review 10.  Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016-2019).

Authors:  Alexandre A de Castro; Letícia C Assis; Flávia V Soares; Kamil Kuca; Daniel A Polisel; Elaine F F da Cunha; Teodorico C Ramalho
Journal:  Biomolecules       Date:  2020-03-12
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