Search results for "ACETYLCHOLINESTERASE"
showing 6 items of 86 documents
In vivo inhibition of AChE activity in the European eel Anguilla anguilla exposed to technical grade fenitrothion.
1998
European eel (Anguilla anguilla) were exposed to sublethal fenitrothion concentrations in a continuous flow-through system for 4 days. Plasma acetylcholinesterase (AChE) activity was evaluated after 2, 8, 12, 24, 32, 48, 56, 72 and 96 h pesticide exposure. AChE activity in the plasma of the eel decreased as concentration of fenitrothion increased. Pesticide induced significant inhibitory effects on the AChE activity of A. anguilla ranging from 51% inhibition at sublethal concentration of 0.02 ppm to 57% inhibition at sublethal concentration of 0.04 ppm. Eel were exposed to both fenitrothion concentrations for 96 h and then allowed a period of recovery in pesticide-free water. Following 1 we…
Use of drug treatments for Alzheimer's disease in France: a study on a national level based on the National Alzheimer's Data Bank (Banque Nationale A…
2012
Purpose To examine the way in which specific drug treatments for Alzheimer's disease are used and whether their use complies with clinical practice guidelines issued by the French National Authority for Health in patients with Alzheimer's disease. Methods We analysed a cross-section of the French National Alzheimer's databank (BNA). Participants were individuals who consulted centres contributing to the BNA in 2010 and diagnosed with Alzheimer's disease and with at least one Mini Mental State Examination (MMSE) score recorded during the course of the year. Results Of 191 919 consultations recorded in the database, 29.9% involved a diagnosis of Alzheimer's disease, and 26 809 patients had co…
Developmental changes and acetylcholinesterase activity in the metamorphosing brain ofTenebrio molitor: Correlation to ecdysteroid titers
1994
The brain of Tenebrio molitor exhibited marked fluctuations in acetylcholinesterase (AChE) activity throughout metamorphosis. This was true AChE activity, since it was inhibited by high substrate concentrations and by 10 μM of the specific AChE inhibitor BW284C51 [(1,5-bis'4-allyldimethylammoniumphenyl)-pentan-3-one dibromide] but not by iso-OMPA (tetraisopropylpyrophosphoramide), a cholinesterase (but not AChE) inhibitor. The histochemical AChE activity was localized in the neuropile and the nuclear envelope of neurons and glial cells. The enzyme extracted from brains with 1% Triton X-100 and 1 M NaCl sedimented as a single peak in a sucrose density gradient, with a sedimentation coefficie…
Der Effekt von Neostigmin an der motorischen Endplatte beim Intermediärsyndrom der Alkylphosphatvergiftung
1991
A patient with severe organophosphate intoxication received Neostigmine 1 mg IV during the intermediate syndrome. This dose resulted clinically and neurophysiologically in a marked deterioration of neuro-muscular transmission. This effect of neostigmine on the neuromuscular block during the intermediate syndrome (deterioration) differs from its effect on a similar pattern (improvement), which is seen in the delayed neuropathy following organophosphate exposure. The administration of therapeutic doses of cholinesterase inhibitors in patients with a reduced safety margin due to inhibition of endplate acetylcholinesterase may be dangerous.
Preclinical progress with CHF2819, a novel orally active acetylcholinesterase inhibitor
2002
(-)-(3aS,8aS,1S)-1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol-2′-ethylphenylcarbamate N-oxide hydrochloride (CHF2819) is a novel, orally active acetylcholinesterase inhibitor (AChEI) for Alzheimer's disease (AD). CHF2819 appears as a selective inhibitor of AChE, being 115 times more potent against this enzyme than butyrylcholinesterase (BuChE). Moreover, CHF2819 appears more selective for inhibiting central (brain) than peripheral (heart) AChE. In vivo studies show that CHF2819 significantly increases acetylcholine (ACh) levels in young adult rat hippocampus in a dose-dependent manner. Moreover, aged animals exhibit a marked increase in hippocampal concentrations of this…
CHF2819: Pharmacological profile of a novel acetylcholinesterase inhibitor
2002
CHF2819 is a novel orally active acetylcholinesterase inhibitor (AChEI) developed for the treatment of Alzheimer's disease (AD). CHF2819 is a selective inhibitor of AChE, it is 115 times more potent against this enzyme than against butyrylcholinesterase (BuChE). Moreover, CHF2819 is more selective for inhibition of central (brain) AChE than peripheral (heart) AChE. In vivo CHF2819, 0.5, 1.5, and 4.5 mg/kg p.o., significantly and in dose-dependent manner increased acetylcholine (ACh) levels in hippocampus of young adult rats. Moreover, aging animals, with lower basal ACh levels than young adult rats, also exhibit a marked increase in hippocampal levels of this neurotransmitter after administ…