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New group of xylene linker-containing acetylcholinesterase reactivators as antidotes against the nerve agent cyclosarin [PDF]

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2006
Nerve agents such as sarin, cyclosarin and tabun are organophosphorus substances able to inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents.
Kamil Kuca, Daniel Jun, Kamil Musilek
exaly   +3 more sources
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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   +4 more
openaire   +2 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   +5 more
openaire   +2 more sources

Identification of S419 on human serum albumin as a novel biomarker for sarin and cyclosarin exposure

Rapid Communications in Mass Spectrometry, 2020
Rationale Organophosphorus nerve agents are highly toxic because they inhibit acetylcholinesterase activity, thereby causing a series of symptomatic poisoning. Upon entering the body, nerve agents bind active amino acid residues to form phosphonylated adducts.
Feiyan Fu   +8 more
openaire   +2 more sources

Effects of low-level sarin and cyclosarin exposure on hippocampal microstructure in Gulf War Veterans

Neurotoxicology and Teratology, 2018
In early March 1991, shortly after the end of the Gulf War (GW), a munitions dump was destroyed at Khamisiyah, Iraq. Later, in 1996, the dump was found to have contained the organophosphorus (OP) nerve agents sarin and cyclosarin. We previously reported evidence of smaller hippocampal volumes in GW veterans with predicted exposure to the Khamisiyah ...
Linda L. Chao, Yu Zhang
openaire   +4 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.
Stanley W, Hulet   +5 more
exaly   +3 more sources

Signs of cyclosarin-induced neurotoxicity and its pharmacological treatment with quaternary pyridinium-oximes reactivators

Toxicology, 2005
Cyclosarin (GF-agent; O-cyclohexylmethylfluorophosphonate) belongs to highly toxic organophosphorus compounds. Potential for exposure to chemical warfare organophosphosphorus nerve agents, such as cyclosarin exists on the battlefield, or in the civilian sector as a threat by a terrorist group, as well as an accident as part of current demilitarization ...
Kamil Kuca, Lucie Bartosova
exaly   +3 more sources

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

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   +2 more
openaire   +2 more sources

Effects of Low-level Inhalation Exposure to Cyclosarin on Learned Behaviors in Sprague-Dawley Rats

Journal of Toxicology and Environmental Health, Part A, 2006
Behavioral and biochemical effects of low-level whole-body inhalation exposure to the chemical warfare nerve agent cyclosarin (GF) were evaluated. Sprague-Dawley rats were first trained on a variable-interval, 56-s (VI56) schedule of food reinforcement.
Raymond F, Genovese   +4 more
openaire   +2 more sources

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