Reactivation Potential of Novel More Lipophilic Pralidoxime Analogs
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F18%3A50014451" target="_blank" >RIV/62690094:18470/18:50014451 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/18:10376449 RIV/60162694:G44__/18:43889544 RIV/61988987:17110/18:A1901RUH
Result on the web
<a href="http://dx.doi.org/10.2174/1570180814666171013163019" target="_blank" >http://dx.doi.org/10.2174/1570180814666171013163019</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1570180814666171013163019" target="_blank" >10.2174/1570180814666171013163019</a>
Alternative languages
Result language
angličtina
Original language name
Reactivation Potential of Novel More Lipophilic Pralidoxime Analogs
Original language description
Background: Novel, more lipophilic analogs of pralidoxime - 2-PAM (K347, K087) and 4-PAM (K349, K120) have been tested in this study due to the recently discovered fact that monoquaternary AChE reactivators penetrate BBB in higher amount. In vitro tests were run against the several organophosphorus agents including tabun, sarin, cyclosarin, soman, VX-agent, Russian VX-agent, diisopropylfluorophosphate and chlorpyrifos. Methods: Standard potentiometric method was used for the evaluation of reactivation efficacy. Rat brain homogenate was used as the source of acetylcholinesterase. Results: The efficacy of novel reactivators was compared against standard AChE reactivators (2-PAM and 4-PAM). K349 and K120 (10-3 M) were 1.1 and 4.8-fold more effective in the reactivation of sarin-inhibited AChE compared with 4-PAM, respectively. Moreover, K120 in 105 M concentration, which is attainable in the plasma within antidotal treatment of intoxication, was 2.1-fold more effective than standard. Generally, the best results were observed for oxime K120. Conclusion: None of the newly prepared benzylated 2-PAM and 4-PAM analogs showed such a broad spectrum of action as standard pralidoxime.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30108 - Toxicology
Result continuities
Project
<a href="/en/project/GA15-16701S" target="_blank" >GA15-16701S: Concept of non-quaternary reactivators AChE as the antidotes of organophsophorus poisoning - a new hope or a blind way?</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2018
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Letters in drug design & discovery
ISSN
1570-1808
e-ISSN
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Volume of the periodical
15
Issue of the periodical within the volume
8
Country of publishing house
AE - UNITED ARAB EMIRATES
Number of pages
6
Pages from-to
822-827
UT code for WoS article
000436085100002
EID of the result in the Scopus database
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