Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Experiments in vitro demonstrated that a thermostatic treatment of an aqueous chlorophos solution at 38 degrees is attended by its increased cholinesterase activity. The speed of the process is much higher in an alkaline medium. A joint incubation of chlorophos with the TMB-4 reactivator of pH of 7.5 and 38 degrees not only fails to result in decomposition of the poison, but on the contrary, tends to speed up the progressive accretion of the inhibitory properties of this organophosphorus compound. The author considers the data obtained as one of the proofs pointing to the formation during direct interaction of TMB-4 with chlorophos or the product of its transformation of a stable complex appearing to be a powerful anticholinesterase agent.
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PMID:[Heightened anticholinesterase activity of chlorophos in its interaction with the TMB-4 reactivator in vitro]. 0 34

The authors found that the contractile activity of isolated myofibers as-well as superprecipitation of myosin B were reduced after intoxication of white rats with 1/2 of dose of LD50 of neguvon. The reaktivator of cholinesterase TMB-4 (20 mg/kg) recovered the contractile capability of myofibres even on the third day after treatment, but superprecipitation of myosin B-after the twentieth day.
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PMID:[Changes in the transverse striated musculature during treatment with the pesticide, Neguvon, and TMB-4 reactivator]. 43 9

Studied was the activity of low concentrations --- 1-10-12, and 1.10-18 -- of the specific reactivators of the enzyme cholinesterase (ChE): 2-PAM, TMB-4 Toxogonin, HS-3, and HS-6, in a chromodacryorrhea test (ChDT) with rats, daily (in the course of 30 days -- 1 ml/100 g), twice (at an interval of 10 days -- 1 ml/100 g) and once (5 mg/kg) at subcutaneous application. Described is an activating affect (observed for the first time in vivo) on ChE preduced by low and very low concentrations of reactivators of the group of oximes. HS-3 produced best activating effects. The low concentrations of the specific oxime ractivators of ChE, followed up by ChDT, can be used as sensitive quantitative indicators of the activity of ChE. They can also serve to specify the mode of action power and term of effectiveness of these reactivators.
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PMID:[Effect of some reactivators on cholinesterase activity in the chromodacryorrhea test in rats]. 79 66

A single application of a mixture of cholinolytic and reactivator of cholinesterase (TMB-4 compos. SPOFA) administered intravenously in the dose of 10.0 mg of trimedoxim per kg of live weight to sheep for 60 minutes after an intramuscular intoxication with O-ethyl S-(2-dimethylaminoethyl) methyl phosphonothioate (EDMM) in the dose of 0.00835 mg per kg of live weight (i.m. LD50, 2h) produces an immediate clinical effect. The reactivation of the erythrocytary acetyl cholinesterase (AChE, E.C.3.1.1.7.) examined in 15 minutes after the administration of the antidotal mixture is almost 100 p.c., the reactivation of the plasmatic butyryl cholin esterase (ChE, E.C.3.1.1.8.) approx. from 70 to 80 p. c. Restitution ad integrum occurred not later than in 14 days after the intoxication.
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PMID:[Antidotal effect of TMB-4 compos. Spofa in sheep intoxicated with O-ethyl S-(2-dimethylaminoethyl) methyl phosphonothioate]. 82 81

Per os intoxication of sheep with O-ethyl S-(2-dimethylaminoethyl)methyl phosphonium thioate (EDMM) in the dose of 0.209 mg per kg of live weight, that means p.o. LD50 (2 h), can be therapeutically mastered by means of an antidotal mixture of the reactivator of cholinesterase (trimedoxim) and of the cholinolytic (atropine), which is commercially available in the SPOFA preparation TMB-4 compos. for human purposes, if the effective dose of the reactivator was 10.0 mg per kg of live weight and if it was applied intravenously, and if the dose of the cholinolytic consisted, per 1 kg of live weight, of 0.08 mm. The antidotal mixture was applied, when the degree of the muscarinic and nicotinic symptoms and the corresponding degree of the inhibition of erythrocytary and plasmatic cholinesterase were on such a level which, according to the classification criteria, we consider a severe grade of intoxication with a dubious diagnosis.
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PMID:[Therapy of organophosphate poisoning in animals]. 82 2

In anesthetized cats, whose peripheral muscarinic-cholinorecptors are blocked by m-cholinolytics (benzilyl choline) failing to penetrate into the brain, the cholinesterases reactivator diethyxime debars the centrally caused fall of the arterial pressure produced by armine, an inhibitor of cholinesterases readily gaining access into the brain. Diethyxime is also capable of abolishing the depression of the phrenic nerve action potentials produced by armine. Dipyroxime-a quaternary diethyxime analogue and also a quaternary cholinesterase reactivator fails to produce such an effect.
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PMID:[Central action of a new cholinesterase reactivator, diethyxime]. 92 73

The administration of 2-pyridine aldoxime methyl chloride (2-PAM Cl) is a standard part of the regimen for treatment of human overexposure to many organophosphorus pesticides and nerve agents. However, some literature references indicate that poisoning by carbaryl (1-naphthyl N-methyl carbamate), an insecticide in everyday use, is aggravated by the administration of 2-PAM Cl. This effect has been reported in the mouse, rat, dog and man. We have found that the inhibition of both eel acetylcholinesterase (eel AChE, EC 3.1.1.7) and human serum cholinesterase (human BuChE, EC 3.1.1.8) by carbaryl was enhanced by several oximes. Based on 95% confidence limits the rank order of potentiation with eel AChE was TMB-4 = Toxogonin > HS-6 = HI-6 > 2-PAM Cl. By the same criterion, the rank order of potentiation with human BuChE was TMB-4 > Toxogonin > HS-6 = 2-PAM Cl. Carbaryl-challenged mice also reflected a potentiation since TMB-4 exacerbated the toxicity more than 2-PAM Cl. Our hypothesis is that certain oximes act as allosteric effectors of cholinesterases in carbaryl poisoning, resulting in enhanced inhibition rates and potentiation of carbaryl toxicity.
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PMID:Studies of the amplification of carbaryl toxicity by various oximes. 141 99

The authors present a retrospective analysis of 50 patients with acute intoxication with various organophosphate cholinesterase inhibitors who were treated in the course of 8 years by comprehensive conservative and extracorporeal elimination treatment. The mean age of the patients was 38 years. During therapy conservative treatment was used (gastric lavage, repeated lavage of the large intestine, forced diuresis, TMB-4 fusion through activated carbon, amberlite XAD-2 and XAD-4, haemodialysis). A total of 63 haemoperfusions and 15 simultaneous haemoperfusions with haemodialysis were performed. Treatment was successful in 92%. The results of treatment depended on early attendance of the patient in the dialyzation centre, on the onset of intense comprehensive treatment and the concurrent presence of other diseases.
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PMID:[Use of hemoperfusion and cholinesterase in acute poisoning with organophosphate cholinesterase inhibitors--clinical analysis of 50 patients]. 175 4

The soluble and immobilized cholinesterases (acetyl cholinesterase of human blood erythrocytes (EC 3.1.1.7) and butyryl cholinesterase of equine blood serum, (EC 3.1.1.8] were inactivated by such irreversible inhibitors as diisopropyl fluorophosphate (DFP), O,O-dimethyl-O-(2,2)-dichlorovinyl) phosphate (DDVP), paraoxone, armine. The inactivated enzymes were reactivated under the effect of TMB-4 (1,1'-trimethylene-bis)-4-formyl-pyridine bromide (dioxime). The values of the reactivation rate constants proved to be equal both for the soluble and immobilized cholinesterases inactivated by the same irreversible inhibitor. The immobilized enzyme is simpler and more correct to study the reactivating action than the soluble one.
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PMID:[Reactivation of phosphorylated cholinesterase immobilized in a gelatin membrane]. 236 91

Pharmacokinetics of dipyroxime was studied following intravenous injection to noninbred albino male rats. Dipyroxime is a cholinesterase reactivating drug now widely used as an antidote in poisonings caused by organophosphorus pesticides. Dipyroxime pharmacokinetics analysis made it possible to propose a formula for approximation of the data on another animal species (dogs). The drug concentration in the dog blood plasma is in a good correlation with the predicted level.
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PMID:[Pharmacokinetics of dipyroxime in the body of rats and dogs]. 358 40


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