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)

Female rats were addicted to methadone via small dosages in their drinking water. The addicted animals were impregnated, and continued to receive the drug during pregnancy and lactation. Offspring were examined at birth and at age 21 days. Compared to controls whose mothers did not receive the drug, pups of addicted mothers at birth had significantly lower weight, brain weight and brain protein; litter size, brain DNA and brain acetylcholinesterase activity were not significantly different between the two groups. At age 21, pups of addicted mothers had significantly lower brain protein and brain acetylcholinesterase than did controls; body weight and brain DNA were not significantly different.
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PMID:Effect of maternal methadone addiction on offspring in rats. 56 48

Albino rats were kept for a year under conditions of everyday motor loading or of a constant hypokinesia. An increase of the motor activity results in rise in the acetylcholinesterase activity determined in the synaptosomal and purified mitochondrial fractions while hypokinesia induces a pronounced decrease in this enzyme activity. The butyrylcholinesterase activity somewhat decreases in the synaptosomal fraction after hypokinesa but does not change under the motor loading regime. Motor loading causes an increase in the amount of synaptosomal water-soluble proteins possessing an intermediate electrophoretic mobility and seem to correspond to the brain-specific protein 14-3-2. In the synaptosomal fraction the amount of membrane proteins with a low electrophoretic mobility and with the cholinesterase activity rises. Hypokinesia, on the contrary, decreases the amount of these membrane proteins.
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PMID:[Effect of motor regimes on water-soluble and membrane proteins and cholinesterase activity in subcellular fractions of rat brain tissue]. 62 7

Two-phase systems consisting of water, dextran and poly(ethylene glycol) have been used for partition of membranes obtained from Torpedo marmorata electric organ. The partition behaviour of the membranes could be adjusted by using a polymer with covalently-bound charged groups. By using this method, the membranes were divided into several fractions which were analyzed for nicotinic acetylcholine receptor and acetylcholinesterase content. It was found that nicotinic receptor-enriched membranes were separated from those containing esterase in a single partition step. Receptor-enriched membranes obtained by gradient centrifugation could be further separated into two receptor fractions by the two-phase technique. The results also reveal at least two types of acetylcholinesterase-rich membranes.
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PMID:Synaptic membranes from Torpedo marmorata electric organ. 1. Separation and analysis of nicotinic acetylcholine receptor- and acetylcholinesterase-containing membrane vesicles using aqueous two-phase systems. 71

Content of organophosphorous inhibitors (with the structure RO/CH3/P/O/SC2H4SC2H5) of cholinesterase as well as their hydrophobic properties (distribution coefficient in hexan/water system) were studied in subcellular fractions of rat brain. Relative content of organophosphorous inhibitors was distinctly decreased in supermicrosomal fraction with increase of hydrophobic properties of the fraction. Nuclear and mitochondrial fractions contained the more hydrophobic substances in relatively higher amount. When homogenate of supermicrosomal fraction was incubated at 37 degrees, own brain cholinesterase was not depressed by organophosphorous inhibitors, containing in the fraction at low concentration. The phenomenon exhibits that content of free organophosphorous inhibitors is distinctly lower in the subcellular fractions studied than amount of the inhibitors, extracted with chloroform.
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PMID:[Intracellular distribution of phosphoorganic cholinesterase inhibitors in rat brain]. 73 75

The Dutch aquatic environment was monitored from September 1969 to December 1975 for organochlorine pesticides and their metabolites, cholinesterase inhibitors, and aromatic amines. The 1,492 samples analyzed included surface water, rainwater, groundwater, and drinking water. The highest concentrations of hexachlorobenzene (HCB) and alpha- and beta-benzene hexachloride (BHC) were found in the Rhine River and its tributaries. Concentrations of the compounds in the Dutch part of the Rhine River decreased downstream. Other organochlorine pesticides and their metabolites, heptachlor, heptachlor epoxide, aldrin, dieldrin, endrin alpha- and beta-endosulfan, and sigmaDDT were detected occasionally, but only in low concentrations. Cholinesterase inhibitors and aromatic amines were always present in the Rhine River and its tributaries.
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PMID:Organochlorines, cholinesterase inhibitors, and aromatic amines in Dutch water samples, September 1969--December 1975. 74 May 17

At the same temperature and with adequate circulation of blood or receptor solution beneath it the permeability of the stratum corneum of the rabbit ear to T2O or to 32P-TPP was the same in vivo as in vitro. When skin permeability was measured in vitro, the subcutaneous adipose tissue present in the full-thickness skin of the rat delayed the penetration of CR, a lipophilic substance with a low water solubility, and decreased the permeability constant by nearly 3x. The retardant solvent PEG 300 did not penetrate the stratum corneum; it formed a hydrogen-bonded complex with the cholinesterase inhibitor VX, thereby reducing the thermodynamic activity and penetration rate of this compound through the stratum corneum. The accelerant solvent DMSO removed protein components from the stratum corneum; electron microscope studies showed that the cells of stratum corneum so treated became separated from one another, and their contents became stainable in bulk with Pb++, indicating the creation of new diffusion pathways. When the temperature, clearance of penetrant from the lower surface of the stratum corneum and penetrant formulation were the same in vivo as in vitro, and the surface of the stratum corneum was saturated with the penetrant or its solution, the results of permeability measurements made in vivo were similar to those made in vitro.
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PMID:Factors affecting the permeability of skin. The relation between in vivo and in vitro observations. 75 61

Schrebera alata is a deciduous fuel tree from which the Samburu people in Northern Kenya obtain bark for medicinal purposes. A pharmacologically active principle that produces analgesic effects can be extracted from the bark with hot water. When administered to rats daily for a period of 6 weeks, the extract of bark (referred to as II kau kawa by the Samburu) caused reduced activities of succinic dehydrogenase, an enzyme that is involved in oxidative processes, and cholinesterase in heart and liver tissues. Histological sections from the liver revealed extensive cellular degeneration and small areas with necrotic lesions. Only that fraction of the bark extracts which contained components less soluble in alcohol produced such lesions within a 2 weeks period. The same fraction is associated with pharmacological activity. Since hepatic injuries occur frequently and the incidence of primary hepatic carcinoma is high in tropical areas, the role of natural toxins as aetiologic factors for cirrhotic conditions must be adequately clarified. It is apparent that bark from S.alata possesses some toxicity and its effects on the liver indicate it can contribute significantly to prevalent hepatocellular damages.
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PMID:Hepatic changes induced by Schrebera alata (Hochst): a preliminary report on the toxicology of II kau kawa. 82 19

As a continuation of our efforts to develop and study inhibitors which act presynaptically on neuromuscular function, sulfur analogues of hemicholinium-3 (HC-3, 1) and acetyl-seco-hemicholinium-3 (AcHC-3, 3) were prepared. In each case sulfur is substituted for the noncarbonyl oxygen in HC-3 (1) and AcHC-3 (3). As expected on the basis of conformational differences between acetylcholine and acetylthiocholine both of the thio analogues are produced in the seco form and do not cyclize spontaneously or when subjected to aqueous, acidic conditions up to 100 degrees C. Both compounds are stable in aqueous pH 7.4 solutions at 37 degrees C and in slightly acidic D2O solutions for more than 24 h. While thio-seco-hemicholinium 3 (11) is stable in the presence of acetylcholinesterase and butyrylcholinesterase in H2O at pH 7.4, acetylthio-seco-hemicholinium-3 (12) reacts within seconds to form the hemiacetal form of thiohemicholinium-3 (16). Mouse toxicity studies (LD50) indicate that while 12 is approximately as toxic as HC-3 (1) and AcHC-3 (3), 11 is 226 times less toxic. As in the studies with 1 and 3, mice were protected from 11 by choline and slightly by neostigmine. It is of interest, however, that almost equal and intermediate protection against 12 was afforded by choline and neostigmine. Structure-toxicity relationships of 1,3,11, 12, and 16 are discussed.
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PMID:Effect of sulfur substitution for the noncarbonyl oxygen in hemicholinium-3 and acetyl-seco-hemicholinium-3. Synthesis, biological activity, and structure-toxicity relationships. 83 27

In order to develop and study inhibitors of neuromuscular function which act presynaptically, three stable analogues of acetyl-seco-hemicholinum-3 (AcHC-3,2) were prepared. These analogues have 2-ethoxyethyltrimethylammonium, 4-oxopentyltrimethylammonium, and n-pentyltrimethylammonium moieties substituted for the 2-acetylethyltrimethylammonium (acetylcholine) moieties of AcHC-3 (2) to form the ether 2, ketone 4, and alkane 5 analoggues of AcHC-3 (2). Although AcHC-3 (2) has been shown to undergo deesterification rapidly in basic solutions and slowly at pH 7.4, it has been found to be stable in H2O or D2O under slightly acidic conditions. All of the analogues are stable for extended time under both slightly acidic conditions and at pH 7.4 in H2O or D3O. It has been found that 2 reacts with acetylcholinesterase and butyrylcholinesterase within seconds in H2O at pH7.4. However, deesterification of 2 with subsequent cyclization to the hemiacetal form of hemicholinium-3 (HC-3, 1) is prevented at pH 7.4, possibly by an irreversible binding of 2 to the enzyme. The analogues 3-5, however, do not react under identical conditions. Mouse toxicity studies (LD50) indicate that 2 is approximately as toxic as HC-3 (1), whereas 3, 4, and 5 are 14.2, 23.8, and 43.1 times less toxic, respectively. The toxic effects of 3-5, like 1 and 2, are antagonized by choline but not by neostigmine in mice. Structure-activity relationships of 2-5 are discussed.
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PMID:Synthesis and structure-toxicity relationships of three new stable analogues of acetyl-seco-hemicholinium-3. 95 Jun 41

Hydrophobity (coefficient in distribution in the hexane water system) and the content of cholinesterase organophosphorous inhibitors (OPI) of the structure Ro (CH3) P (O) SC2H4 SC2H5 were studied in the rat brain. When the O-alkyl radical is increased hydrophobity rises and the relative content of free OPI in the brain extracted by chloroform decreases. With an increase in R from the ethyl to butyl one the ability to the additional inhibition of the brain own cholinesterase lowers due to incubation of homogenate at 37 degrees C, that evidences for an essential drop in the studied series of the free OPI fraction relative to the free OPI extracted by chloroform.
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PMID:[Binding of phosphoorganic cholinesterase inhibitors in rat brain tissue]. 98 15


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