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Göteborgs universitets publikationer

Pralidoxime – the gold standard of acetylcholinesterase reactivators – reac­tivation in vitro efficacy

Författare och institution:
Kamil Kuca (-); M Hrabinova (-); Ondrej Soukup (-); Gunnar Tobin (Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi); Jana Zdarova Karasova (-); Miroslav Pohanka (-)
Publicerad i:
Bratislava Medical Journal, 111 ( 9 ) s. 502-504
Artikel, refereegranskad vetenskaplig
Sammanfattning (abstract):
Objective: In this work, we aim to summarize the universality of this compound, its reactivation potential when different cholinesterase inhibitors are used. Background: Pralidoxime is considered as a gold standard of acetylcholinesterase reactivators - antidotes used in case of nerve agent poisonings. It has been commercially available for many years. However, several studies deem this oxime an old-fashion antidote. Methods: Pralidoxime was synthesized at our department. The reactivating efficacy was tested on 10 % (w/v) rat brain homogenate that had been incubated with appropriate inhibitor for 30 minutes to reach 96 % inhibition of AChE. Then, pralidoxime was added for 10 minutes. Measurements were performed at 25 °C, pH 8, and 10-3and 10-5M concentrations of AChE reactivators. The activities of brain AChE were measured by a potentio-static method. Results: No sufficient reactivation was achieved at the concentration of 10-5 M, which is a concentration that can be reached after administration of therapeutic doses. At a higher dose (10-3 M), pralidoxime reactivated AChE inhibited by paraoxon, chlorpyrifos, Russian VX, VX and sarin. Conclusion: From the obtained results, it is clear that pralidoxime seems to be a poor reactivator of AChE inhibited by organophosphorous AChE inhibitors and thus cannot be labeled as a universal reactivator.
Ämne (baseras på Högskoleverkets indelning av forskningsämnen):
Medicinska grundvetenskaper ->
Farmakologi och toxikologi ->
cholinesterase, reactivator, oxime, inhibitor, pralidoxime
Postens nummer:
Posten skapad:
2010-11-03 17:53
Posten ändrad:
2011-11-24 16:08

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