Literature DB >> 15639788

Reactivation of organophosphate-inhibited acetylcholinesterase by quaternary pyridinium aldoximes.

Kamil Kuca1, Jirí Patocka, Jirí Cabal, Daniel Jun.   

Abstract

We investigated the relationship between the chemical structure of acetylcholinesterase (AChE; EC 3.1.1.7) reactivators and their potency in reactivating this enzyme, after prior inhibition by VX (O-ethyl-S-(2-diisopropylaminoethyl)-methylthiophosphonate), tabun, sarin, and cyclosarin. The oximes, pralidoxime (2-PAM), HI-6 [1-(2-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-2-oxa-propane dichloride], obidoxime and HS-6 [1-(2-hydroxyiminomethylpyridinium)-3-(3-carbamoylpyridinium)-2-oxa-propane dichloride] were used as representatives of the group of AChE reactivators. Rat brain AChE was used as the appropriate source of the enzyme. Our results confirm that there is no single broad-spectrum oxime suitable for the treatment of poisoning with all highly toxic organophosphorus agents.

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Year:  2004        PMID： 15639788     DOI： 10.1007/BF03033452

Source DB:  PubMed          Journal:  Neurotox Res        ISSN： 1029-8428            Impact factor:   3.911


  15 in total

1.  Reactivating effect of alpha,omega-bis-(4-pyridinealdoxime)-2-trans-butene dibromide on isopropyl-methylphosphonylated acetylcholinesterase.

Authors:  J Patocka; J Bielavský; F Ornst
Journal:  FEBS Lett       Date:  1970-10-05       Impact factor: 4.124

2.  Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase.

Authors:  Kamil Kuca; Jirí Bielavský; Jirí Cabal; Jirí Kassa
Journal:  Bioorg Med Chem Lett       Date:  2003-10-20       Impact factor: 2.823

3.  Reactivating potency of obidoxime, pralidoxime, HI 6 and HLö 7 in human erythrocyte acetylcholinesterase inhibited by highly toxic organophosphorus compounds.

Authors:  F Worek; R Widmann; O Knopff; L Szinicz
Journal:  Arch Toxicol       Date:  1998-03       Impact factor: 5.153

Review 4.  Review of oximes in the antidotal treatment of poisoning by organophosphorus nerve agents.

Authors:  J Kassa
Journal:  J Toxicol Clin Toxicol       Date:  2002

5.  A comparison of the efficacy of a new asymmetric bispyridinium oxime BI-6 with presently used oximes and H oximes against sarin by in vitro and in vivo methods.

Authors:  J Kassa; J Cabal
Journal:  Hum Exp Toxicol       Date:  1999-09       Impact factor: 2.903

6.  A comparison of the efficacy of acetylcholinesterase reactivators against cyclohexyl methylphosphonofluoridate (GF agent) by in vitro and in vivo methods.

Authors:  J Kassa; J Cabal
Journal:  Pharmacol Toxicol       Date:  1999-01

7.  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.

Authors:  K Kuca; J Kassa
Journal:  J Enzyme Inhib Med Chem       Date:  2003-12       Impact factor: 5.051

8.  Oximes-induced reactivation of rat brain acetylcholinesterase inhibited by VX agent.

Authors:  Kamil Kuca; Jirí Kassa
Journal:  Hum Exp Toxicol       Date:  2004-04       Impact factor: 2.903

Review 9.  Organophosphate poisoning.

Authors:  T C Marrs
Journal:  Pharmacol Ther       Date:  1993       Impact factor: 12.310

Review 10.  Review of oximes available for treatment of nerve agent poisoning.

Authors:  R M Dawson
Journal:  J Appl Toxicol       Date:  1994 Sep-Oct       Impact factor: 3.446
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  6 in total

Review 1.  Neurotoxins and neurotoxicity mechanisms. An overview.

Authors:  Juan Segura-Aguilar; Richard M Kostrzewa
Journal:  Neurotox Res       Date:  2006-12       Impact factor: 3.911

2.  The acute toxicity of acetylcholinesterase reactivators in mice in relation to their structure.

Authors:  Lucie Bartosova; Kamil Kuca; Gabriela Kunesova; Daniel Jun
Journal:  Neurotox Res       Date:  2006-06       Impact factor: 3.911

Review 3.  Neurotoxins and neurotoxic species implicated in neurodegeneration.

Authors:  Juan Segura Aguilar; Richard M Kostrzewa
Journal:  Neurotox Res       Date:  2004       Impact factor: 3.911

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

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

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.  Time-course changes of acetylcholinesterase activity in blood and some tissues in rats after intoxication by Russian VX.

Authors:  Jana Zdarova Karasova; Jiri Bajgar; Daniel Jun; Ruzena Pavlikova; Kamil Kuca
Journal:  Neurotox Res       Date:  2009-11       Impact factor: 3.911
  6 in total

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