A comparison of reactivating efficacy of newly developed oximes (K074, K075) and currently available oximes (obidoxime, HI-6) in cyclosarin-and tabun-poisoned rats

Kassa, Jiřı́; Jun, Daniel; Kuča, Kamil

doi:10.1080/14756360601114361

Cited by 14 publications

(10 citation statements)

References 23 publications

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“…While trimedoxime and obidoxime are preferred for the treatment of acute poisoning with organophosphorus insecticides (OPI) because they are considered to be sufficiently effective reactivators of OPIinhibited AChE [28,29,30], the oxime HI-6 appears to be a promising antidote against highly toxic fluorophosphonates, especially soman and cyclosarin, because it is able to protect experimental animals from adverse effects and improve survival of poisoned animals [14,15]. Nevertheless, our results clearly demonstrate its low potency to reactivate tabun-inhibited AChE in rats and protect tabun-poisoned mice from its lethal toxic effects [31,32]. Trimedoxime as well as obidoxime seem to be more effective oximes for the treatment of acute tabun poisonings than the oxime HI-6 but their potency to eliminate tabun-induced lethal effects is limited, when they are administered at low, human-relevant doses [32].…”

Section: Discussioncontrasting

confidence: 71%

A comparison of the reactivating and therapeutic efficacy of newly developed bispyridinium oximes (K250, K251) with commonly used oximes against tabun in rats and mice

Kassa¹,

Karasová²,

Bajgar³

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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The potency of newly developed bispyridinium compounds (K250, K251) in reactivating tabun-inhibited acetylcholinesterase and reducing tabun-induced lethal toxic effects was compared with currently available oximes (obidoxime, trimedoxime, the oxime HI-6) using in vivo methods. Studies determined percentage of reactivation of tabun-inhibited blood and tissue AChE in poisoned rats and showed that the reactivating efficacy of both newly developed oximes is comparable with the oxime HI-6 but it is significantly lower than the reactivating effects of obidoxime and trimedoxime, especially in diaphragm and brain. Both newly developed oximes were also found to be able to slightly reduce lethal toxic effects in tabun-poisoned mice. Their therapeutic efficacy is higher than the potency of the oxime HI-6 but it is lower than the therapeutic effects of trimedoxime and obidoxime. Thus, the reactivating and therapeutic potency of both newly developed oximes (K250, K251) does not prevail over the effectiveness of currently available oximes and, therefore, they are not suitable for their replacement for the treatment of acute tabun poisoning.

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Section: Discussioncontrasting

confidence: 71%

A comparison of the reactivating and therapeutic efficacy of newly developed bispyridinium oximes (K250, K251) with commonly used oximes against tabun in rats and mice

Kassa¹,

Karasová²,

Bajgar³

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…This compound exceeded the effect of previous oximes K-27 (8) ad K-48 (9) including commercial trimedoxime (7) against GA, but exhibited very high toxicity [34]. This reason excludes K-74 (10) from further in vivo testing.…”

Section: Introductionmentioning

confidence: 93%

Synthesis, Antidotal Effects and HPLC Behavior of Some Novel Pyridinium Aldoximes

Laufer¹,

Kalász²,

Musílek

et al. 2010

COC

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Pyridinium aldoximes are used as antidotes in organophosphate poisoning. In the reactivation process they form a complex with the organophosphates, even if the serine active site of acetylcholinesterase enzymes has been inactivated by the organophosphorus compounds. Essential disadvantage of the previously used pyridinium aldoximes is the instability and the toxicity of these complexes. Novel pyridinium aldoximes show more effective detoxifying effects.A general scheme of the synthesis of several novel and very promising pyridinium aldoximes and their basic characteristics are shown in this paper.

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“…Intoxication of those nerve agents, which were not reactivated by obidoxime, could be then treated by using atropine only, anticonvulsives and other supportive treatment. Second possibility is to use military antidotes, especially oxime HI-6, which is considered to be broad-Reactivation potency of the acetylcholinesterase reactivator Obidoxime is limited spectrum reactivator [26][27][28][29] . However, it is at present time not approved for civilian purposes.…”

Section: Discussionmentioning

confidence: 99%

Reactivation Potency of the Acetylcholinesterase Reactivator Obidoxime Is Limited

Kuča¹,

Musílek²,

Pohanka³

et al. 2009

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

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A comparison of reactivating efficacy of newly developed oximes (K074, K075) and currently available oximes (obidoxime, HI-6) in cyclosarin-and tabun-poisoned rats

Cited by 14 publications

References 23 publications

A comparison of the reactivating and therapeutic efficacy of newly developed bispyridinium oximes (K250, K251) with commonly used oximes against tabun in rats and mice

A comparison of the reactivating and therapeutic efficacy of newly developed bispyridinium oximes (K250, K251) with commonly used oximes against tabun in rats and mice

Synthesis, Antidotal Effects and HPLC Behavior of Some Novel Pyridinium Aldoximes

Reactivation Potency of the Acetylcholinesterase Reactivator Obidoxime Is Limited

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