Results 141 to 150 of about 1,056 (182)

Potency of new structurally different oximes to reactivate cyclosarin-inhibited human brain acetylcholinesterases [PDF]

Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
Antidotes currently used for organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Owing to the wide-spread of these toxic compounds worldwide, development of antidotes in the case of first aid is needed. To select the most promising
Kamil Kuca, Daniel Jun, Martina Hrabinova   +2 more
exaly   +3 more sources

Effect of Seven Newly Synthesized and Currently Available Oxime Cholinesterase Reactivators on Cyclosarin-Intoxicated Rats [PDF]

International Journal of Molecular Sciences, 2009
Seven new oxime-based acetylcholinesterase reactivators were compared with three currently available ones (obidoxime, trimedoxime, HI-6) for their ability to lessen cholinesterase inhibition in blood and brain of cyclosarin-treated rats. Oximes were given at doses of 5% their LD50 along with 21 mg/kg atropine five min before the LD50 of cyclosarin (120
Jana Zdarova Karasova, Jiri Kassa, Kamil Musilek   +2 more
exaly   +3 more sources

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In vitro detoxification of cyclosarin (GF) by modified cyclodextrins

Toxicology Letters, 2011
Developing potent detoxification strategies for prophylaxis and therapy against organophosphate (OP) intoxication still represents a challenging task. Clinical application of numerous investigated substances including enzymes and low molecular scavengers like metal ions or nucleophiles could not yet be realised due to profound disadvantages. Presenting
Müller, Susanne, Koller, Marianne, Le Provost, Romain, Lafont, Olivier, Estour, François, Wille, Timo, Thiermann, Horst, Worek, Franz, Reiter, Georg   +8 more
openaire   +4 more sources

In vitro toxicokinetic studies of cyclosarin: Molecular mechanisms of elimination

Toxicology Letters, 2014
The toxicokinetics of in vitro elimination of highly toxic cyclosarin (GF) in biological systems revealed striking stereoselective differences in the range of 0.01μM to 1mM GF. While weak concentration dependency was detected for elimination of the toxic (-)-enantiomer indicating catalytic processes, elimination of less toxic (+)-GF followed unusual ...
Georg, Reiter, Susanne, Müller, Marianne, Koller, Horst, Thiermann, Franz, Worek   +4 more
openaire   +2 more sources

Comparison of sarin and cyclosarin toxicity by subcutaneous, intravenous and inhalation exposure in Gottingen minipigs

Inhalation Toxicology, 2014
Sexually mature male and female Gottingen minipigs were exposed to various concentrations of GB and GF vapor via whole-body inhalation exposures or to liquid GB or GF via intravenous or subcutaneous injections. Vapor inhalation exposures were for 10, 60 or 180 min.
Douglas R Sommerville, Pe
exaly   +3 more sources

Effectiveness of a substituted β-cyclodextrin to prevent cyclosarin toxicity in vivo

Toxicology Letters, 2014
Standard treatment of poisoning by organophosphorus (OP) nerve agents with atropine and an oxime has a limited efficacy. An alternative approach is the development of stoichiometric or catalytic (bio-)scavengers which should be able to prevent systemic toxicity. Recently, a β-cyclodextrin derivative, 6-OxP-CD, bearing a pyridinium oximate in 6-position
Franz, Worek, Thomas, Seeger, Michael, Zengerle, Stefan, Kubik, Horst, Thiermann, Timo, Wille   +5 more
openaire   +2 more sources

Mechanistic studies of new oximes reactivators of human butyryl cholinesterase inhibited by cyclosarin and sarin

Journal of Biomolecular Structure and Dynamics, 2016
Butyryl cholinesterase (BChE) has been seen as a key enzyme in the search for new strategies in the treatment of poisoning by organophosphates (OPs), since human BChE (HssBChE), complexed with the appropriate oxime, can be a suitable scavenger and deactivator for OPs in the blood stream.
Lima, Willian E. Amaral de, Francisco, Ander, Cunha, Elaine Fontes Ferreira da, Radic, Zoran, Taylor, Palmer, França, Tanos C. C., Ramalho, Teodorico C.   +6 more
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Structural Factors Influencing Potency of Currently Used Acetylcholinesterase Reactivators for Treatment of Cyclosarin Intoxications

Current Pharmaceutical Design, 2007
Cyclosarin is one member of nerve agent family. Recent treatment of intoxications by organophosphorus compounds, such as nerve agents or pesticides, consists of rapid administration of anticholinergics and AChE reactivators. Owing to the threat of terroristic use of these compounds during last years, improvement of antidotal therapy still continues. As
Kamil, Kuca, Daniel, Jun, Jiri, Bajgar
openaire   +2 more sources

Potency of Five Structurally Different Acetylcholinesterase Reactivators to Reactivate Human Brain Cholinesterases Inhibited by Cyclosarin

Clinical Toxicology, 2007
Acetylcholinesterase (AChE; EC 3.1.1.7) reactivators are used as a part of the antidotal therapy of organophosphorus pesticide and nerve agent intoxications. Cyclosarin is one member of the nerve agent family. In this article, we compared the reactivation potency of five structurally different AChE reactivators (pralidoxime, trimedoxime, methoxime, HS ...
Kamil Kuca, Daniel Jun, Martina Hrabinova   +2 more
exaly   +3 more sources

Effect of reversible ligands on oxime-induced reactivation of sarin- and cyclosarin-inhibited human acetylcholinesterase

Toxicology Letters, 2015
Poisoning by organophosphorus compounds (OP) used as pesticides and nerve agents is due to irreversible inhibition of the enzyme acetylcholinesterase (AChE). Oximes have been widely recognized for their potency to reactivate the inhibited enzyme. The limited efficacy of currently available oximes against a broad spectrum of OP-compounds initiated novel
Corinna, Scheffel, Horst, Thiermann, Franz, Worek   +2 more
openaire   +2 more sources