Cent Eur J Public Health 2004, 12(Supplement):S59-S61

In Vitro Reactivation of Tabun-Inhibited Acetylcholinesterase Using New Oximes - K027, K005, K033 and K048

Kuča K., Cabal J.
Department of Toxicology, Purkyně Medical Military Academy, Hradec Králové, Czech Republic

Four new AChE oximes for reactivation of acetylcholinesterase inhibited with tabun - K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium) propane dibromide], K005 [1,3-bis(2-hydroxyiminomethylpyridinium) propane dibromide], K033 [1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide] and K048 [1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium) butane dibromide] were prepared. Their efficacies to reactivate tabun-inhibited acetylcholinesterase were studied and compared with the currently used acetylcholinesterase reactivators (pralidoxime, obidoxime and HI-6). Reactivator K048 seems to be promising reactivator of tabun-inhibited AChE. Its reactivation potency is significantly higher than the efficacy of HI-6 and pralidoxime, and comparable with the potency of the obidoxime at human relevant doses.

Klíčová slova: acetylcholinesterase, nerve agents, oximes, reactivation

Zveřejněno: 1. březen 2004  Zobrazit citaci

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Kuča K, Cabal J. In Vitro Reactivation of Tabun-Inhibited Acetylcholinesterase Using New Oximes - K027, K005, K033 and K048. Cent Eur J Public Health. 2004;12(Supplement):S59-61. PubMed PMID: 15141981.
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Reference

  1. Kassa J: Review of oximes in the antidotal treatment of poisoning by organophosphorus nerve agents. J Toxicol Clin Toxicol 2002; 40: 803816. Přejít k původnímu zdroji...
  2. Krejčová G, Kassa J: Neuroprotective efficacy of pharmacological pretreatment and antidotal treatment in tabun-poisoned rats. Toxicology 2003; 185: 129-139. Přejít k původnímu zdroji...
  3. Marrs TC: Organophosphate poisoning. Pharmacol Therap 1993; 58: 51-66. Přejít k původnímu zdroji...
  4. Kuča K, Kassa J: A comparison of the ability of a new byspyridinium oxime - 1-(hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium)butane dibromide and currently used oximes to reactivate nerve agent-inhibited rat brain acetylcholinesterase by in vitro methods. J Enz Inhib 2003 (In press). Přejít k původnímu zdroji...
  5. Kuča K, Bielavský J, Cabal J, Bielavská J: Synthesis of a potential reactivator of acetylcholinesterase 1-(4-hydroxyiminomethylpyridinium)3-(carbamoylpyridinium)-propane dibromide. Tetrahedron Lett 2003; 44: 3123-3125. Přejít k původnímu zdroji...
  6. Kuča K, Bielavský J, Cabal J, Kassa J: Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase. Bioorg Med Chem Lett 2003; 13: 3545-3548. Přejít k původnímu zdroji...
  7. Kuča K, Cabal J: In vitro comparison of the reactivation effectivity of the potential symmetric bisquaternary acetylcholinesterase reactivators differing in the length of the connecting chain Voj Zdrav Listy 2003 (in press).
  8. Koplovitz I, Stewart JR: A comparison of the efficacy of HI-6 and 2-PAM against soman, tabun, sarin and VX in the rabbit. Toxicol Lett 1994; 70: 169-179. Přejít k původnímu zdroji...
  9. Kassa J, Cabal J: 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. Human Exp Toxicol 1999; 18: 560-565. Přejít k původnímu zdroji... Přejít na PubMed...
  10. Kuča K, Patočka J, Cabal J: Reactivation of organophosphate inhibited acetylcholinesterase activity by α,ω-bis-(4-hydroxyiminomethylpyridinium)alkanes in vitro. J Appl Biomed 2003 (in press). Přejít k původnímu zdroji...