Acetylcholinesterase peripheral

De Ferrari GV, Mallender WD, Inestrosa NC, Rosenberry TL (2001) Thioflavin T is a fluorescent probe of the acetylcholinesterase peripheral site that reveals conformational interactions between the peripheral and acylation sites. J Biol Chem 276(26) 23282... 

Bourne, Y., Taylor, P., Radic, Z., March-ot, P. Structural Insights into Ligand Interactions at the Acetylcholinesterase Peripheral Anionic Site. EMBO J. 2003, 22, 1-12. 

There is a second type of cholinesterase called butyrylcholinesterase, pseudocholinesterase, or cholinesterase. This enzyme is present in some nonneural cells in the central and peripheral nervous systems as well as in plasma and serum, the liver, and other organs. Its physiologic function is not known, but is hypothesized to be the hydrolysis of esters ingested from plants (Lefkowitz et al. 1996). Plasma cholinesterases are also inhibited by organophosphate compounds through irreversible binding this binding can act as a detoxification mechanism as it affords some protection to acetylcholinesterase in the nervous system (Parkinson 1996 Taylor 1996). 

Furthermore, any particular type of site belonging to any one of these categories may exist in a number of different cellular or tissue locations. For example, acetylcholinesterase is located in a number of different mammalian tissues (e.g., brain, peripheral nervous system, and red blood cells), and all of these may be inhibited by... 

Donepezil is a piperidine cholinesterase inhibitor, which reversibly and non-competitively inhibits centrally active acetylcholinesterase 34 This specificity is claimed to result in fewer peripheral side effects as compared to the other ChE inhibitors. 

Organophosphate Ester Hydraulic Fluids. The biomarkers of effects after exposure to organophosphate ester hydraulic fluids are well established in cases of delayed neuropathy (clinical signs of peripheral neuropathy). Further study would be helpful to determine whether certain effects (such as diarrhea after oral exposure) are due to direct action of the toxic agent on the target organ or to inhibition of acetylcholinesterase at the acetylcholine nerve receptor site on the organ. 

Eichler, J., Anselment, A., Sussman, J.L., Massoulie, J. and Silman, I. (1994) Differential effects of peripheral site ligands on Torpedo and chicken acetylcholinesterase. Molecular Pharmacology 45, 335-340. 

Compound 10 was evaluated for anti-bacterial activity and acetylchohnesterase (AChE) inhibitory activities. This compound was foimd to be inactive in antibacterial assay and exhibited AChE inhibitory activity with an ICj, value of 67 pM. Acetylcholine serves as a neurotransmitter in the central and peripheral nervous system. Acetylcholinesterase (AChE) stops the function of acetylcholine by its... 

Acetylcholinesterase (AChE) is the enzyme that hydrolyzes and thereby deactivates acetycholine (ACh) after it binds to the receptor. The enzyme is present in peripheral and central synaptic sites, in erythrocytes, and in the placenta. 

Diazinon, an anticholinesterase organophosphate, inhibits acetylcholinesterase in the central and peripheral nervous system. Inhibition of acetylcholinesterase results in accumulation of acetylcholine at muscarinic and nicotinic receptors leading to peripheral and central nervous system effects. These effects... 

Diazinon toxicity results predominantly from the inhibition of acetylcholinesterase in the central and peripheral nervous system. The enzyme is responsible for terminating the action of the neurotransmitter, acetylcholine, in the synapse of the pre- and post-synaptic nerve endings or in the neuromuscular junction. However, the action of acetylcholine does not persist long as it is hydrolyzed by the enzyme, acetylcholinesterase, and rapidly removed. As an anticholinesterase organophosphate, diazinon inhibits acetylcholinesterase by reacting with the active site to form a stable phosphorylated complex which is incapable of destroying acetylcholine at the synaptic gutter between the pre- and post-synaptic nerve... 

Grassi, J., Frobert, Y., Lamourette, P, andLagoutte, B. (1988) Screening ofmono-clonal antibodies using antigens labeled with acetylcholinesterase application to the peripheral proteins of photosystem 1. Anal Biochem 168, 436-450... 

Table 8 shows that at concentrations of 10-7 — 10 8M l-(chloromethyl)sila-trane does not affect phosphodiesterase of the rat brain and monoamine oxidase of the rat liver. At the same time, at 10 4M concentration the preparation weakly inhibits the acetylcholinesterase of the rat brain. Therefore, 1-(chloromethyl)sila-trane may be expected to produce a gentle stimulatory effect on the processes in the central and peripheral nervous system which are mediated by acetylcholine. l-(Chloromethyl)silatrane activates mildly the preparation of summarized ATP values of the rat liver. No reaction is observed with SH-groups of glutathione. 

Johnson, J. L., Cusack, B., Hughes, T. F., McCullough, E. H., Fauq,A., Romanovskis, P., Spatola, A. F. and Rosenberry, T. L. (2003). Inhibitors tethered near the acetylcholinesterase active site serve as molecular rulers of the peripheral and acylation sites. J. Biol. Chem. 278,38948-38955. 

Donepezil is primarily a reversible inhibitor of acetylcholinesterase with a long elimination half-life. It lacks the hepatotoxicity of tacrine but frequently causes nausea, vomiting and diarrhoea. These side effects, together with occasional bradycardia, sycope and changes in the sleep architecture, are directly associated with a central and peripheral enhancement of cholinergic function. At the present time, donepezil is the most widely prescribed anticholinesterase in the United States and Europe. 

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