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Pralidoxime – the g...
Pralidoxime – the gold standard of acetylcholinesterase reactivators – reactivation in vitro efficacy
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Kuca, Kamil (författare)
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Hrabinova, M (författare)
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Soukup, Ondrej (författare)
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visa fler...
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- Tobin, Gunnar, 1954 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi,Institute of Neuroscience and Physiology, Department of Pharmacology
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Karasova, Jana Zdarova (författare)
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Pohanka, Miroslav (författare)
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visa färre...
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(creator_code:org_t)
- 2010
- 2010
- Engelska.
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Ingår i: Bratislava Medical Journal. - 0006-9248. ; 111:9, s. 502-504
- Relaterad länk:
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https://gup.ub.gu.se...
Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- cholinesterase
- reactivator
- oxime
- inhibitor
- pralidoxime
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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