scholarly journals A Comparison of the Potency of the Oxime HLö-7 and Currently Used Oximes (HI-6, Pralidoxime, Obidoxime) to Reactivate Nerve Agent-Inhibited Rat Brain Acetylcholinesterase by in vitro Methods

2005 ◽  
Vol 48 (2) ◽  
pp. 81-86 ◽  
Author(s):  
Kamil Kuča ◽  
Jiří Cabal ◽  
Jiří Kassa ◽  
Daniel Jun ◽  
Martina Hrabinová
Keyword(s):  
Rat Brain ◽  
Nerve Agents ◽  
Nerve Agent ◽  
The Other ◽  
In Vitro Evaluation ◽  
In Vitro Methods ◽  
Hi 6 ◽  
Hlö 7 ◽  
Brain Acetylcholinesterase

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.

Synthesis and in vitro evaluation of donepezil-based reactivators and analogues for nerve agent-inhibited human acetylcholinesterase

RSC Advances ◽  
2016 ◽  
Vol 6 (22) ◽  
pp. 17929-17940 ◽  
Author(s):  
Julien Renou ◽  
José Dias ◽  
Guillaume Mercey ◽  
Tristan Verdelet ◽  
Catherine Rousseau ◽  
...  
Keyword(s):  
Nerve Agent ◽  
In Vitro Evaluation ◽  
Hi 6

Donepezil-based reactivators 1–3 show a better ability (8 fold higher) than pralidoxime to reactivate VX-hAChE, and oxime 2 is 5 to 11 fold more efficient than pralidoxime and HI-6 respectively to reactivate of VX-hBChE.

scholarly journals Evaluation of Potency of Known Oximes (Pralidoxime, Trimedoxime, HI-6, Methoxime, Obidoxime) to in vitro Reactivate Acetylcholinesterase Inhibited by Pesticides (Chlorpyrifos and Methylchlorpyrifos and Nerve Agent (Russian VX)

2007 ◽  
Vol 50 (3) ◽  
pp. 203-206 ◽  
Author(s):  
Kamil Musílek ◽  
Kamil Kuča ◽  
Daniel Jun
Keyword(s):  
Organophosphorus Pesticides ◽  
Nerve Agents ◽  
Nerve Agent ◽  
Hi 6 ◽  
Acetylcholinesterase Reactivators

Nerve agents and pesticides belong to the group of organophosphates. They are able to inhibit irreversibly the enzyme acetylcholinesterase (AChE). Acetylcholinesterase reactivators were designed for the treatment of nerve agent intoxications. Their potency to reactivate pesticide-inhibited AChE was many times evaluated. In this study, five commonly used AChE reactivators (pralidoxime, methoxime, HI-6, obidoxime, trimedoxime) for the reactivation of AChE inhibited by two pesticides (chlorpyrifos and methylchlorpyrifos) were used. Russian VX (nerve agent) as a member of nerve agents’ family was taken for comparison. Obtained results show that oximes developed against nerve agent intoxication are less effective for intoxication with organophosphorus pesticides. Especially, methylchlorpyrifos-inhibited AChE was found to be poorly reactivated by the compounds used.

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

2004 ◽  
Vol 23 (4) ◽  
pp. 167-171 ◽  
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.

scholarly journals <em>In vitro</em> reactivation of chlorpyrifos-inhibited rat brain acetylcholinesterase from pyrazole-oxime derivatives

2020 ◽  
Author(s):  
Manjunath Katagi ◽  
Girish Bolakatti ◽  
Sujatha ML ◽  
Suchitra M ◽  
Shivlingrao Mamledesai
Keyword(s):  
Rat Brain ◽  
Oxime Derivatives ◽  
Brain Acetylcholinesterase
Sign in / Sign up

Export Citation Format

Share Document