نتایج جستجو برای: reactivators

تعداد نتایج: 133  

Journal: :The Biochemical journal 2013
Zoran Radić Trevor Dale Zrinka Kovarik Suzana Berend Edzna Garcia Limin Zhang Gabriel Amitai Carol Green Božica Radić Brendan M Duggan Dariush Ajami Julius Rebek Palmer Taylor

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...

2017
Mancini Costa da Cunha

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...

Journal: :Journal of medicinal chemistry 2009
Benoît Sanson Florian Nachon Jacques-Philippe Colletier Marie-Thérèse Froment Lilly Toker Harry M Greenblatt Joel L Sussman Yaacov Ashani Patrick Masson Israel Silman Martin Weik

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...

2006
Šárka Veselá Vlastimil Ondruška Kamil Kuča Jiří Patočka

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...

2013
Mirjana B Čolović Danijela Z Krstić Tamara D Lazarević-Pašti Aleksandra M Bondžić Vesna M Vasić

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...

Journal: :Molecules 2017
Terrone L Rosenberry Xavier Brazzolotto Ian R Macdonald Marielle Wandhammer Marie Trovaslet-Leroy Sultan Darvesh Florian Nachon

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...

Akriti Kaura Girish Thunga, Rama Mylapuri Sreedharan Nair Sudha Vidyasagar Sureshwar Pandey Vijayanarayana Kunhikatta

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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