Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The action of eserine of acetylcholinesterase (AchE) reversible inhibitor of frog muscle fibres membrane potential (MP) under various physico-chemical conditions in external solution was studied. The data obtained show that changes of external pH in any direction decrease the depolarisation of the membrane produced by eserine. The dose-effect curve is linear at pH 7, but it has saturation at pH 6 and pH 9. Dependence of the membrane depolarisation in the presence of eserine upon calcium ions concentration in external solution is S-shape. Protonophore 3C1CCP (carbonilcianamid-m-3C1-phenylhydrazon) depolarises the membrane further in the presence of eserine. Valinomycin under these conditions completely restores the MP. Evidence is obtained that eserine reduces potassium permeability of the muscle membrane. It is supposed that membrane-bound AchE is involved in the ionic permeability regulation of the muscle membrane at rest.
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PMID:[Eserine-induced change in membrane potential of frog muscle fibers]. 96 99

Dependence of the amplitude of miniature end-plate currents on frequency of spontaneous quantal release modulated by the elevation of K+ concentration was studied in the frog voltage clamped neuromuscular junctions. A sharp increase of mEPC frequency (not less than approximately 50 per sec) was followed by an obvious fall in both their amplitude and acceleration of decay only in the presence of 3 microM prostigmine (acetylcholinesterase inhibitor) and 5 microM proadiphene, these agents promoting a desensitization of cholinergic postsynaptic membrane. Probable depletion of transmitter store is not involved in the phenomenon observed which is mainly due to the repetitive activation of the postsynaptic zones and the increase of the desensitized cholinoreceptor number.
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PMID:[Desensitisation of postsynaptic membrane in the neuro-muscular junction due to an increase in spontaneous quantal release of a mediator]. 1243 84

Review of the own and literature data on substrate specificity with use of thiosubstrates for cholinesterases of various species. Dependence of cholinesteratic hydrolysis parameters on various elements of their structure is considered: the acyl part, alkyl "bridge" between ester atom and onion group, and ammonium grouping of molecule of 44 thioesters. A comparative enzymological analysis of the substrate specificity is performed with use of thiocholine esters of acetic, propionic, and butyric acids for 40 cholinesterase preparations of mammals, insects, molluscs, and plants.
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PMID:[Thiosubstrates of different cholinesterases]. 1841 8

Dependence on benzodiazepines (BZDs) or Z-drugs (zolpidem, zopicline and zaleplon) is a common clinical phenomenon. Traditional detoxification of BZDs dependence includes tapering used dose gradually and using equivalent doses of long-acting BZDs as substitutes. This kind of regimen tends to take a long time (up to 4weeks) and may require hospitalization. Acetylcholinesterase inhibitors have been shown to reverse BZDs induced sedation. We propose that oral form acetylcholinesterase inhibitors (donepezil, galantamine and rivastigmine) also posses the effect of inhibiting GABA receptors, and act as indirect antagonist, to be applied in the rapid detoxification treatment of BZDs and Z-drug dependence.
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PMID:Rapid detoxification of benzodiazepine or Z-drugs dependence using acetylcholinesterase inhibitors. 2477 20