نتایج جستجو برای: reactivators
تعداد نتایج: 133 فیلتر نتایج به سال:
In the present paper we show a comprehensive in vitro, ex vivo and in vivo study on hydrolytic detoxification of nerve agent and pesticide OPs (organophosphates) catalysed by purified hBChE (human butyrylcholinesterase) in combination with novel non-pyridinium oxime reactivators. We identified TAB2OH (2-trimethylammonio-6-hydroxybenzaldehyde oxime) as an efficient reactivator of OP-hBChE conjug...
Organophosphophorus compounds (OP) has been widely used as pesticides and as warfare nerve agents. They act by phosphorylating the hydroxyl group of the Ser 203 residue of the Acetylcholinesterase (AChE) active site, inhibiting its catalytic activity, causing the cholinergic Syndrome [1]. Currently, the OP poisoning treatment consists in the use of reactivators, for example oximes, a class of c...
Organophosphate compounds (OP) are potent inhibitors of acetylcholinesterases (AChEs) and can cause lethal poisoning in humans. Inhibition of AChEs by the OP soman involves phosphonylation of the catalytic serine, and subsequent dealkylation produces a form known as the "aged" enzyme. The nonaged form can be reactivated to a certain extent by nucleophiles, such as pralidoxime (2-PAM), whereas a...
Daphnia magna is a freshwater microcrustacean which is often used for acute and chronic toxicity testing in aquatic ecotoxicology. Recently, tests with daphnids have been used to prescreen the toxicity of newly synthesized acetylcholinesterase reactivators (oximes), which appear as weak inhibitors of acetylcholinesterase (AChE). In our study we investigated and compared the toxicity of five rev...
Acetylcholinesterase is involved in the termination of impulse transmission by rapid hydrolysis of the neurotransmitter acetylcholine in numerous cholinergic pathways in the central and peripheral nervous systems. The enzyme inactivation, induced by various inhibitors, leads to acetylcholine accumulation, hyperstimulation of nicotinic and muscarinic receptors, and disrupted neurotransmission. H...
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) hydrolyze the neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic neurotransmission. Although closely related, these enzymes display very different substrate specificities that only partially overlap. This disparity is largely due to differences in the number of aromatic residues lining the active site...
Organophosphate (OP) poisoning is one of the most common causes of poisoning in developing countries especially in Southeastern Asia. Poisoning with phosphorus-containing organic chemicals or OP compounds can be managed with antidotes like oximes which are potential reactivators of acetylcholinesterase (AChE). The efficacy of oxime therapy in OP poisoned patients mainly depends upon various fac...
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