A Comparison of the Potency of Newly Developed Oximes (K005, K027, K033, K048) and Currently Used Oximes (Pralidoxime, Obidoxime, HI-6) to Reactivate Sarin-Inhibited Rat Brain Acetylcholinesterase By in Vitro Methods

1. The efficacy of the oxime HLö-7 and currently used oximes (pralidoxime, obidoxime, HI-6) to reactivate acetylcholinesterase inhibited by various nerve agents (sarin, tabun, cyclosarin, VX) was tested by in vitro methods. 2. Both H oximes (HLö-7, HI-6) were found to be more efficacious reactivators of sarin and VX-inhibited acetylcholinesterase than pralidoxime and obidoxime. On the other hand, their potency to reactivate tabun-inhibited acetylcholinesterase is very low and does not reach the reactivating efficacy of obidoxime. In the case of cyclosarin, the oxime HI-6 was only found to be able to sufficiently reactivate cyclosarin-inhibited acetylcholinesterase in vitro. 3. Thus, the oxime HLö-7 does not seem to be more efficacious reactivator of nerve agent-inhibited acetylcholinesterase than HI-6 according to in vitro evaluation of their reactivation potency and, therefore, it is not more suitable to be introduced for antidotal treatment of nerve agent-exposed people than HI-6.

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In Vitro Potency of H Oximes (HI-6, HLö-7), the Oxime BI-6, and Currently Used Oximes (Pralidoxime, Obidoxime, Trimedoxime) to Reactivate Nerve Agent-Inhibited Rat Brain Acetylcholinesterase

Journal of Toxicology and Environmental Health Part A ◽

10.1080/15287390500364283 ◽

2006 ◽

Vol 69 (15) ◽

pp. 1431-1440 ◽

Cited By ~ 7

Author(s):

Kamil Kuca ◽

Jiri Cabal ◽

Jiri Kassa ◽

Daniel Jun ◽

Martina Hrabinova

Keyword(s):

Rat Brain ◽

Nerve Agent ◽

Hi 6 ◽

Hlö 7 ◽

Brain Acetylcholinesterase

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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

Journal of Enzyme Inhibition and Medicinal Chemistry ◽

10.1080/14756360310001605552 ◽

2003 ◽

Vol 18 (6) ◽

pp. 529-535 ◽

Cited By ~ 93

Author(s):

K. Kuča ◽

J. Kassa

Keyword(s):

Rat Brain ◽

Nerve Agent ◽

In Vitro Methods ◽

Brain Acetylcholinesterase

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A comparison of tabun-inhibited rat brain acetylcholinesterase reactivation by three oximes (HI-6, obidoxime, and K048) in vivo detected by biochemical and histochemical techniques

Journal of Enzyme Inhibition and Medicinal Chemistry ◽

10.3109/14756360903433373 ◽

2010 ◽

Vol 25 (6) ◽

pp. 790-797 ◽

Cited By ~ 3

Author(s):

Jiri Bajgar ◽

Petr Hajek ◽

Jana Karasova Zdarova ◽

Jiri Kassa ◽

Antonin Paseka ◽

...

Keyword(s):

Rat Brain ◽

Hi 6 ◽

Acetylcholinesterase Reactivation ◽

Brain Acetylcholinesterase

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

Human & Experimental Toxicology ◽

10.1191/0960327104ht434oa ◽

2004 ◽

Vol 23 (4) ◽

pp. 167-171 ◽

Cited By ~ 26

Author(s):

Kamil Kuča ◽

Jiří Kassa

Keyword(s):

Rat Brain ◽

Brain Homogenate ◽

Hi 6 ◽

Brain Acetylcholinesterase

A comparison of one mono- and seven bisquaternary acetylcholinesterase (AChE) reactivators of acetylcholinesterase inhibited by VX agent was performed. As a source of the acetylcholinesterase, a rat brain homogenate was taken. There were significant differences in reactivation potency of all tested oximes. The oxime TO205 seems to be the most efficacious followed by TO046, HI-6, HS-6, K027, obidoxime, MMC and 2-PAM. In addition, the results of this study showed that the reactivation potency of the tested reactivators depends on many factors-such as the number of pyridinium rings, the number of oxime groups and their position, as well as the length and the shape of linkage bridge between two pyridinium rings.

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