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1
Cloning of Acetylcholinesterase Gene in a Microbial Vector.
1987-01-01

Techniques to distinguish between the activities of human acetylcholinesterase and pseudocholinesterase have been developed. Human neuroblastoma cell lines have been shown to synthesize human acetylcholinesterase and the level of enzyme within these cells...

National Technical Information Service (NTIS)

2
THE PHYSIOLOGICAL EFFECTS OF ARGON, HELIUM AND ...
1967-10-31

... The activity of purified tyrosinase, acetylcholinesterase, alpha-chymotrypsin and other enzymes is inhibited with increasing effectiveness by AR > Kr ...

DTIC Science & Technology

3
The effect of polyamidoamine dendrimers on human erythrocyte membrane acetylcholinesterase activity.
2004-12-01

Polyamidoamine (PAMAM) dendrimers impact on activity of acetylcholinesterase was studied. It has been shown that dendrimers induce a biphasic effect: depending on their concentrations they increase or decrease enzyme activity. It may be due to two types of interactions: direct--between dendrimers and the ...

PubMed

4
Molecular Dynamics of Acetylcholinesterase
2002-06-01

Molecular dynamics simulations are leading to a deeper understanding of the activity of the enzyme acetylcholinesterase. Simulations have shown how breathing motions in the enzyme facilitate the displacement of substrate from the surface of the enzyme to the buried active ...

Energy Citations Database

5
EFFECTS OF WATER POLLUTANTS AND OTHER CHEMICALS ON FISH ACETYLCHOLINESTERASE (IN VITRO)

Acetylcholinesterase (AChE) preparations from the muscle of the fathead minnow (Pimephales promelas Rafinesque) were treated (in vitro) with 74 chemicals of various classes, many of which are environmental contaminants, to determine their effect upon enzyme activity. A highly inh...

EPA Science Inventory

6
Crystallization of Acetylcholinesterase (AChE) from Torpedo Electric Organ.
1991-01-01

The objective of this project is the crystallization of the enzyme acetylcholinesterase (AChE), with the long-term objective of determining its three-dimensional structure and, thereby, the detailed topography of its active site. Torpedo electric organ wa...

National Technical Information Service (NTIS)

7
Acetylcholinesterase and Acetylcholine Receptor.
1986-01-01

We are studying the properties of the active site, and the region peripheral to it, of acetylcholinesterase (AcChE), the enzyme which hydrolyzes and thus terminates the action of the important neurotransmitter acetylcholine (AcCh). We have studied the res...

National Technical Information Service (NTIS)

8
Acetylcholinesterase: from 3D structure to function.
2010-02-04

By rapid hydrolysis of the neurotransmitter, acetylcholine, acetylcholinesterase terminates neurotransmission at cholinergic synapses. Acetylcholinesterase is a very fast enzyme, functioning at a rate approaching that of a diffusion-controlled reaction. The powerful toxicity of organophosphate poisons is attributed primarily to their ...

PubMed

9
Acetylcholinesterase: From 3D Structure to Function
2010-02-04

By rapid hydrolysis of the neurotransmitter, acetylcholine, acetylcholinesterase terminates neurotransmission at cholinergic synapses. Acetylcholinesterase is a very fast enzyme, functioning at a rate approaching that of a diffusion-controlled reaction. The powerful toxicity of organophosphate poisons is attributed primarily to their ...

PubMed Central

10
Mechanism of action of organophosphorus and carbamate insecticides.
1990-07-01

Organophosphorus and carbamate insecticides are toxic to insects and mammals by virtue of their ability to inactivate the enzyme acetylcholinesterase. This review addresses the mechanism of inhibition of acetylcholinesterase by organophosphorus and carbamate esters, focusing on structural requirements necessary for anticholinesterase ...

PubMed Central

11
Induction of plasma acetylcholinesterase activity in mice challenged with organophosphorus poisons.
2011-07-02

The restoration of plasma acetylcholinesterase activity in mice following inhibition by organophosphorus pesticides and nerve agents has been attributed to synthesis of new enzyme. It is generally assumed that activity levels return to normal, are stable and do not exceed the normal level. We have observed over the ...

PubMed

12
X-ray Structures of Torpedo californica Acetylcholinesterase Complexed with (+)-Huperzine A and (-)-Huperzine B: Structural Evidence for an Active Site

data are presented on the interaction with Torpedo californica acetylcholinesterase (TcAChE acetylcholine (ACh). The enzyme acetylcholinesterase (AChE; EC 3.1.1.7) functions in cholinergic synapses for AD using AChE inhibitors as drugs (5-7). The inhibitors approved so far include synthetic compounds

E-print Network

13
Reactivation of aged organophosphorus inhibited acetylcholinesterase. Final report
1988-09-30

The purpose of the work done was to prepare derivatives of 2-PAM that are substituted in the 3-position by groups capable of bonding to, or liganding with, the oxygen on the phosphorus of aged, poisoned (by phosphonylation or phosphorylation) acetylcholinesterase. The derivatives suggested for preparation were designed to facilitate cleavage of the bond between phosphorus and ...

Energy Citations Database

14
Photoregulation of biological activity by photocromic reagents. II. Inhibitors of acetylcholinesterase.
1969-11-01

The enzymic activity of acetylcholinesterase can be photoregulated through the mediation of photochromic inhibitors of the enzyme. N-p-phenylazophenyl-N-phenylcarbamyl fluoride, an irreversible inhibitor of acetylcholinesterase, exists as two geometric isomers which are interconvertible through ...

PubMed

15
PHOTOREGULATION OF BIOLOGICAL ACTIVITY BY PHOTOCROMIC REAGENTS, II. INHIBITORS OF ACETYLCHOLINESTERASE*
1969-11-01

The enzymic activity of acetylcholinesterase can be photoregulated through the mediation of photochromic inhibitors of the enzyme. N-p-phenylazophenyl-N-phenylcarbamyl fluoride, an irreversible inhibitor of acetylcholinesterase, exists as two geometric isomers which are interconvertible through ...

PubMed Central

16
Regulation of Acetylcholine Receptors in Relation to Acetylcholinesterase in Neuroblastoma Cells
1973-10-01

Purified ? -toxin from Naja nigricollis snake venom labeled by [3H]acetylation binds specifically to the acetylcholine receptors of mouse neuroblastoma cells. Toxin binding was inhibited by inhibitors for nicotinic and muscarinic acetylcholine receptors. Clones of neuroblastoma cells were selected for low acetylcholinesterase (EC 3.1.1.7) activity with ...

NASA Astrophysics Data System (ADS)

17
[Acetylcholinesterase activity in erythrocytes of workers engaged in the production of iron-manganese alloys].
1992-01-01

The activity of acetylcholinesterase in the red blood cells of metallurgy workers producing iron-manganese alloys was statistically less significant than the activity of this enzyme in the control group. Work tenure and smoking intensity, measured using the smoking index method did not significantly affect the ...

PubMed

18
Effects of gamma radiation on solutions of acetylcholinesterase
1975-12-01

Dilute solutions of bovine erythrocyte acetylcholinesterase were irradiated by 30, 60, 90, and 120 krad of $sup 60$Co gamma rays under air at around 5$sup 0$C. The enzyme activity decreased progressively with radiation dose. Ultraviolet spectra measurements indicated conformational changes in the enzyme ...

Energy Citations Database

19
Solubilization of Erythrocyte Acetylcholinesterase by Ultrasonic Vibration
1967-05-01

ERYTHROCYTE acetylcholinesterase (AChE) is strongly bound to the cell membrane1. To isolate and purify this enzyme, it must be removed from the membrane and brought into solution. Methods used for this purpose have included treatment with butanol2, digestion with pancreatin3, or addition of a surface-active material4,5. More recently, ...

NASA Astrophysics Data System (ADS)

20
Long Route or Shortcut? A Molecular Dynamics Study of Traffic of Thiocholine within the Active-Site Gorge of Acetylcholinesterase

of acetylcholinesterase (AChE) is the termination of nerve impulse transmission at cholinergic synapses by rapid of acetic acid (3) (see Scheme 1). In accordance with its function, AChE is an extremely rapid enzyme (3). Being an essential enzyme, AChE is the target of a variety of potent natural and synthetic toxic

E-print Network

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21
Enzyme activities following chronic exposure to crude oil in a simulated ecosystem. II. Striped mullet
1979-10-01

Enzyme activities were investigated in brain, gill, liver, and muscle homogenates from striped mullet which had been exposed to crude oil for 10 months in a simulated estuarine ecosystem. Enzymes assayed included acetylcholinesterase, alkaline phosphatase, ..beta..-glucuronidase, glutamic-pyruvic transaminase, ...

Energy Citations Database

22
Effect of Photoperiod on Blood Cholinesterase Activity and Melatonin Concentrations in Adult Cats.
1993-01-01

Activity of synaptically released acetylcholine (Ach) is terminated by the degradative enzyme acetylcholinesterase (AChE), or true cholinesterase. There is a second class of cholinesterase found in living systems, pseudocholinesterase (butyrylcholinestera...

National Technical Information Service (NTIS)

23
Biological Synthesis of a Protein Analogue of Acetylcholinesterase: Monoclonal Anti-Idiotype Antibody Analogue of the Esteratic Site.
1986-01-01

The authors have studied the binding properties and inhibitory activity of AE-2, a monoclonal antibody which binds to acetylcholinesterase(AChE) and inhibits its activity by up to 50%. This antibody was compared to C1B7, another inhibitory enzyme. It was ...

National Technical Information Service (NTIS)

24
Expression of erythroid acetylcholinesterase in the K-562 leukemia cell line.
1983-11-01

Differentiation-dependent expression of enzyme loci was evaluated in two human leukemic cell lines, the pluripotent leukemia cell line K-562 and the promyelocytic-like cell line HL-60. Acetylcholinesterase, a marker of erythroid differentiation, was present in K-562 cells and absent in HL-60 cells. This difference between the two lines was apparently ...

PubMed

25
Typical and atypical antipsychotics alter acetylcholinesterase activity and ACHE expression in zebrafish (Danio rerio) brain.
2009-07-01

Antipsychotic agents are widely used for the treatment of psychotic symptoms in patients with several brain disorders. Antipsychotic drugs principally affect dopamine systems with the newer ones also affecting serotonin, norepinephrine, and histamine systems. Other transmitter systems can be involved with selected antipsychotic drugs but effects on cholinergic system are less known. Considerable ...

PubMed

26
The inhibition activity of selected beta-carboline alkaloids on enzymes of acetylcholinesterase and butyrylcholinesterase.
2011-06-01

This thesis deals with testing of inhibition activity beta-carboline alkaloids on activity of enzymes acetylcholinesterase (ACHE) and butyrylcholinesterase (BUCHE) using test "Fast Blue B salt" at TLC desk and Ellman's test using spectrophotometer. It was also investigated how dimethylsulfoxide used as a solvent in ...

PubMed

27
� Springer Science + Business Media B.V. 2009 STRUCTURAL STUDIES ON ACETYLCHOLINESTERASE

. The principal biological role of the synaptic enzyme, acetylcholinesterase (AChE), is to terminate synaptic for atherosclerosis.15 The solution of the crystal structures of Torpedo californica (Tc) AChE16 and, more recently). Although, as already mentioned, AChE displays very high catalytic activity, especially for a serine

E-print Network

28
Recombinant Human Acetylcholinesterase - Production and Post-Translational Processing.
1993-01-01

Genetic engineering techniques were employed for development of efficient expression systems of recombinant human acetylcholinesterase (rHuAChE). Human cell lines allowing production of 10-20 mg/liter of fully-active enzyme were established. Biotechnologi...

National Technical Information Service (NTIS)

29
Chemico-Biological Interactions 157�158 (2005) 247�252 Inhibition of acetylcholinesterase by the

or its metabolites with acetylcholinesterase (AChE). Kinetic studies indicated that CPT-11 was primarily of enzyme activity. Structural analogs of 4-piperidinopiperidine however, did not inhibit AChE, including be synthesized that do not inhibit AChE, or alternatively, that novel AChE inhibitors could be designed based

E-print Network

30
The readthrough variant of acetylcholinesterase remains very minor after heat shock, organophosphate inhibition and stress,

e dello Sviluppo, Universita` `La Sapienza', Roma, Italy Abstract Acetylcholinesterase (AChE) exists; we also analyzed the effects of heat shock and AChE inhibition on neuroblastoma cells. Active AChE, the acetylcholine hydrolyzing enzyme, acetyl- cholinesterase (AChE) presents various molecular forms. A single gene

E-print Network

31
Captopril modulates acetylcholinesterase in human keratinocytes.
2011-02-01

Human keratinocytes synthesize and secrete non-neuronal acetylcholine, which acts as a local cell signaling molecule, regulating functions like proliferation, cell adhesion, motility, desmosomal cell contact, and glandular activity. The keratinocyte acetylcholine axis is composed of the enzymes mediating acetylcholine synthesis (acetyltransferase) and ...

PubMed

32
New Inhibitors of the Peripheral Site in Acetylcholinesterase That Specifically Block Organophosphorylation.
2001-01-01

Acetyicholinesterase (AChE) is one of the most efficient enzymes known. The AChE active site consists of a narrow gorge with two separate ligand binding sites: an acylation site at the bottom of the gorge where substrate hydrolysis occurs and a peripheral...

National Technical Information Service (NTIS)

33
Mass Spectrometry to Identify New Biomarkers of Nerve Agent Exposure.
2010-01-01

The accepted target for oganophosphorus agent (OP) binding to enzymes is the active site serine in the consensus sequence GlyXSerXGly of acetylcholinesterase. By using mass spectrometry to fragment OP-labeled peptides, we have found that OP can make coval...

National Technical Information Service (NTIS)

34
Activity of Organophosphate Acid Anhydrase in Rangia cuneata.
1988-01-01

Enzymes capable of hydrolyzing diisopropyl fluorophosphate (DFP) and related acetylcholinesterase inhibitors, have been reported in the tissues of many animals and have recently been renamed as organophosphate acid (opa) anhydrases. Purified clam-digestiv...

National Technical Information Service (NTIS)

35
AN APPROACH FOR SCREENING CHOLINESTERASE INHIBITORS IN DRINKING WATER USING AN IMMOBILIZED ENZYME ASSAY

A simple, inexpensive and sensitive method for detecting organophosphate and carbamate insecticides is reported. Acetylcholinesterase was immobilized to PorexR Lateral-FloTM membrane material and remained active for several months at room temperature. The assay was sensitive ...

EPA Science Inventory

36
Acetylcholinesterase: diffusional encounter rate constants for dumbbell models of ligand.
1995-01-01

For some enzymes, virtually every substrate molecule that encounters the entrance to the active site proceeds to reaction, at low substrate concentrations. Such diffusion-limited enzymes display high apparent bimolecular rate constants ((kcat/KM)), which depend strongly upon solvent viscosity. Some experimental studies provide evidence ...

PubMed Central

37
Inhibition of acetylcholinesterase in guppies (Poecilia reticulata) by chlorpyrifos at sublethal concentrations: Methodological aspects
1989-04-01

Acetylcholinesterase activity is a potential biochemical indicator of toxic stress in fish and a sensitive parameter for testing water for the presence of organophosphates. A number of methodological aspects regarding the determination of the in vivo effect of chlorpyrifos on acetylcholinesterase in guppies have been investigated. It ...

Energy Citations Database

38
Mechanism of Acetylcholinesterase Inhibition by Fasciculin: A 5-ns Molecular Dynamics Simulation
2002-05-01

Our previous molecular dynamics simulation (10 ns) of mouse acetylcholinesterase (EC 3.1.1.7) revealed complex fluctuation of the enzyme active site gorge. Now we report a 5-ns simulation of acetylcholinesterase complexed with fasciculin 2. Fasciculin 2 binds to the gorge entrance of ...

Energy Citations Database

39
Reactivation of Acetylcholinesterase Activity and Its ...
2011-05-15

... 4. TITLE AND SUBTITLE Reactivation of acetylcholinesterase activity and its therapeutic benefits in nerve agent 5a. CONTRACT NUMBER ...

DTIC Science & Technology

40
Reactivation of Acetylcholinesterase Activity and Its ...

... Database of articles on military and naval science, operational warfare, joint ... of Acetylcholinesterase Activity and Its Therapeutic Benefits in Nerve ...

DTIC Science & Technology

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41
Electronic structure and PCA analysis of covalent and non-covalent acetylcholinesterase inhibitors.
2010-09-14

Hartree-Fock and density functional methods were used to analyze electronic and structural properties of known drugs to evaluate the influence of these data on acetylcholinesterase inhibition. The energies of the frontier orbitals and the distances between the more acidic hydrogen species were investigated to determine their contributions to the activity ...

PubMed

42
[Brain cholinesterases in marine mammals].

Substrate properties of brain cholinesterases were studied in ringed seal and beluga. Kinetic parameters of hydrolysis of thiocholine esters of carboxylic acids were determined. According to the substrate specificity, the enzyme from the brain of marine mammals can be assigned to acetylcholinesterases. Specific properties of the enzyme ...

PubMed

43
The efficiency of various detergents for extraction and stabilization of acetylcholinesterase from bovine erythrocytes.
1987-01-01

The efficiency of several nonionic detergents and a homologous series of zwitterionic detergents for the extraction of acetylcholinesterase (EC 3.1.1.7) from bovine erythrocyte membranes was examined. Of the nonionic detergents examined, the polyoxyethylene-based Tweens were the least effective solubilizing agents. Within this series, increasing the length of the saturated ...

PubMed

44
Cholinestrase test (image)

... evaluation. The lab evaluates the enzymes acetylcholinesterase and pseudocholinesterase, which act to break down acetylcholine. Acetylcholine is ...

MedlinePLUS

45
Kinetics of enzyme inhibition by active molluscicidal agents ferulic acid, umbelliferone, eugenol and limonene in the nervous tissue of snail Lymnaea acuminata.
2009-02-01

Ferulic acid, umbelliferone (Ferula asafoetida), eugenol (Syzygium aromaticum) and limonene (Carum carvi) are active molluscicidal components that inhibited the activity of alkaline phosphatase and acetylcholinesterase in in vivo and in vitro exposure of Lymnaea acuminata. It was observed that ferulic acid, umbelliferone and eugenol ...

PubMed

46
The Primary Sequence of Acetylcholinesterase and Selective ...
1991-06-07

... with each form of the enzyme have been prepared which revealed each enzyme species to be localized at distinct positions with the synapse. ...

DTIC Science & Technology

47
Shoot-and-Trap: Use of specific x-ray damage to study structural protein dynamics by

at the active site of the enzyme Torpedo californica acetylcholinesterase (TcAChE), and permitted monitoring of subsequent clearance of a radiolysis product from the active site. AChE terminates transmission-product expelled. Then, a water molecule regenerates the free enzyme with concomitant ...

E-print Network

48
Effects of Mixed Gamma-Neutron Radiation on the Activity of Brain Enzymes involved in Neurotransmitter Metabolism.
1973-01-01

Sprague-Dawley adult male rats were exposed to incapacitating doses (20,000 rads) of mixed gamma-neutron radiation in a single pulse from the AFRRI-TRIGA reactor. The activities of the enzymes choline acetyl transferase, acetylcholinesterase, monoamine ox...

National Technical Information Service (NTIS)

49
Kinetics of inhibition of acetylcholinesterase in the presence of acetonitrile.
2009-03-09

The hydrolysis of acetylthiocholine by acetylcholinesterase from Electrophorus electricus was investigated in the presence of the inhibitors tacrine, gallamine and compound 1. The interaction of the enzyme with the substrate and the inhibitors was characterized by the parameters K(I), alpha', b or beta, K(m) and V(max), which were determined directly and ...

PubMed

50
Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines.
2010-08-31

A series of tetracyclic thienopyrimidines (7-14) was prepared and investigated as inhibitors of acetylcholinesterase from Electrophorus electricus acetylcholinesterase (EeAChE), as well as human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). A new synthetic procedure was employed for the synthesis of the ...

PubMed

51
Enzyme activities following chronic exposure to crude oil in a simulated ecosystem. I. American oysters and brown shrimp
1979-10-01

Enzyme activities were investigated in whole-body homogenates from oysters and hepatopancreas homogenates from shrimp which had been exposed to crude oil for 8 months in a simulated estuarine ecosystem. Enzymes assayed included acetylcholinesterase, alkaline phosphatase, ..beta..-glucuronidase, glutamic-pyruvic ...

Energy Citations Database

52
Spontaneous reactivation of acetylcholinesterase following organophosphate inhibition. II. Characterization of the reactivating components.
1977-08-11

Repeated cycles of inhibition by a variety of organophosphates followed by spontaneous reactivation reveal a component of electric eel acetylcholinesterase (acetylcholine hydrolase, EC 3.1.1.7) which preferentially reactivates. That the observed enzymatic activity truly resides in acetylcholinesterase is indicated by its sensitivity to ...

PubMed

53
In vitro inhibition of acetylcholinesterase from four marine species by organophosphates and carbamates
1990-08-01

The literature on the biological, physical, and pharmaceutical chemistry of cholinesterase is considerable and includes data on activators and inhibitors. Most of the work on specific anticholinesterasic agents has been concerned with carbamates and organophosphates. Because of the sensitivity of acetylcholinesterase to carbamates and organophosphates, the ...

Energy Citations Database

54
Spectrophotometry in vivo, a technique for local and direct enzymatic assays: application to brain acetylcholinesterase.
1987-11-01

In vivo enzymology is not widely studied due to the lack of a well-adapted technology. We have developed a system that allows local and long-term spectrophotometric assays in brain tissue of live animals. It utilizes a miniaturized optical probe consisting of a multibarrel micropipette for reagent injections and optical fibers for light absorption measurements. We have applied this system to the ...

PubMed Central

55
Phytochemical and enzyme inhibitory studies on indigenous medicinal plant Rhazya stricta.
2010-03-01

A new triterpenoid 3alpha-hydroxy-ursane-5-ene (1) and a known steroid stigma sterol (2) have been isolated for the first time from the fruit of Rhazya stricta. The structures of these compounds were elucidated and identified by spectral studies. The crude ethanolic extract of R. stricta fruit has led to the determination of good results of antibacterial, lipoxygenase and ...

PubMed

56
Mechanistic toxicodynamic model for receptor-mediated toxicity of diazoxon, the active metabolite of diazinon, in Daphnia magna.
2011-05-03

The organothiophosphate diazinon inhibits the target site acetylcholinesterase only after activation to its metabolite diazoxon. Commonly, the toxicity of xenobiotics toward aquatic organisms is expressed as a function of the external concentration and the resulting effect on the individual level after fixed exposure times. This approach does not account ...

PubMed

57
In vitro effects of antiepileptic drugs on acetylcholinesterase and ectonucleotidase activities in zebrafish (Danio rerio) brain.
2010-03-31

Carbamazepine (CBZ), phenytoin (PHT), and gabapentine (GBP) are classical antiepileptic drugs (AEDs) that act through a variety of mechanisms. We have tested the in vitro effects of CBZ, PHT, and GBP at different concentrations on ectonucleotidase and acetylcholinesterase activities in zebrafish brain. CBZ inhibited ATP hydrolysis at 1000 microM (32%) ...

PubMed

58
Laboratory and field microassay of cholinesterases in whole blood, plasma, and erythrocytes.
1987-01-01

A straightforward method is described for determination of the activities of erythrocyte acetylcholinesterase and plasma cholinesterase from single 10-mul samples of highly diluted whole blood. The procedure is a spectrophotometric microassay adapted for use with microtitration plates. The use of an enzyme immunoassay reader ...

PubMed

59
Laboratory and field microassay of cholinesterases in whole blood, plasma, and erythrocytes
1987-01-01

A straightforward method is described for determination of the activities of erythrocyte acetylcholinesterase and plasma cholinesterase from single 10-?l samples of highly diluted whole blood. The procedure is a spectrophotometric microassay adapted for use with microtitration plates. The use of an enzyme immunoassay reader facilitates ...

PubMed Central

60
Compared Effects of Dithiothreitol on the Interaction of an Affinity-Labeling Reagent with Acetylcholinesterase and the Excitable Membrane of the Electroplax
1969-08-01

p-(trimethyl ammonium) benzene diazonium difluoroborate (TDF), an affinity-labeling reagent of the acetylcholine receptor site(s), which in the normal cell acts as an irreversible inhibitor becomes a reversible activator after in vivo exposure of the electroplax to dithiothreitol (DTT), a disulfide bond reducing agent. After in vitro exposure of ...

NASA Astrophysics Data System (ADS)

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61
Reactivation of aged organophosphorus inhibited acetylcholinesterase. Annual summary report, 1 August 1986-31 July 1987
1987-08-31

It has been argued that failure to regenerate native acetylcholinesterase from that which has been poisoned with derivatives of methylphosphonic acid (e.g., soman. sarin, and VX) through less-than-immediate treatment with 2-PAM (or its relatives such as toxogonin) may be due, in part, to aging. By this is meant that of the two ester groups extant in the phosphonylated ...

Energy Citations Database

62
Cholinesterases in neural development: new findings and toxicologic implications.
1999-02-01

Developing animals are more sensitive than adults to acute cholinergic toxicity from anticholinesterases, including organophosphorus pesticides, when administered in a laboratory setting. It is also possible that these agents adversely affect the process of neural development itself, leading to permanent deficits in the architecture of the central and peripheral nervous systems. Recent ...

PubMed Central

63
Age-Dependent Changes in Activity of Mallard Plasma Cholinesterases.
1991-01-01

Plasma acetylcholinesterase (AChE) and butrylcholinesterase (BChE) activity was measured repeatedly in 27 mallard (Anas platyrhynchos) ducklings between 7 and 85 days of age to determine age-dependent changes in enzyme activity. Plasma AChE, BChe, and tot...

National Technical Information Service (NTIS)

64
AGE-DEPENDENT CHANGES IN ACTIVITY OF MALLARD PLASMA CHOLINESTERASES

Plasma acetylcholinesterase (AChE) and butrylcholinesterase (BChE) activity was measured repeatedly in 27 mallard (Anas platyrhynchos) ducklings between 7 and 85 days of age to determine age-dependent changes in enzyme activity. Plasma AChE, BChe, and total cholinesterase (ChE) a...

EPA Science Inventory

65
X-ray structure of a transition state analog complex reveals the molecular origins of the catalytic power and substrate specificity of acetylcholinesterase
1996-03-13

The structure of a complex of Torpedo californica acetylcholinesterase with the transition state analog inhibitor m-(N, N,N-trimethylammonio)-2,2,2-trifluoroacetophenone has been solved by X-ray crystallographic methods to 2.8 A resolution. Since the inhibitor binds to the enzyme about 10{sup 10}-fold more tightly than the substrate acetylcholine, this ...

Energy Citations Database

66
Organophosphates and monocyte esterase deficiency.
1995-08-01

AIMS--To examine the possibility that monocyte esterase deficiency (MED) could be caused by exposure to organophosphates. METHODS--Pseudocholinesterase, paraoxonase and arylesterase activities were measured in the serum and acetylcholinesterase activity was measured in the red cells of a group of monocyte esterase deficient subjects ...

PubMed Central

67
THE EFFECT OF IONIZING RADIATION ON ACETYLCHOLINE METABOLISM IN MACACA- RHESUS MONKEYS
1961-11-01

In macaca-rhesus monkeys the normal content of free acetylcholine in the mucosa of the small intestine was higher, as it was in brain and liver, than bound acetyl choline. The total cholinesterase activity and, particularly, the activity of acetylcholinesterase and non-specific cholinesterase in control monkeys is highest in ...

Energy Citations Database

68
Perfusion immunoassay for acetylcholinesterase: analyte detection based on intrinsic activity.
1995-09-01

A quantitative, two-column, HPLC-based assay requiring only 30 min to complete is reported. Amniotic fluid proteins are first fractionated on a size-exclusion column; the fraction containing the M(r) 280,000 neural acetylcholinesterase (AChE) is then diverted to a second column, an ImmunoDetection cartridge derivatized with an anti-AChE antibody. The immobilized antibody traps ...

PubMed

69
Correlation between rate of enzyme-substrate diffusional encounter and average Boltzmann factor around active site.
1998-04-01

The utility of the average Boltzmann factor around the active site of an enzyme as the predictor of the electrostatic enhancement of the substrate binding rate is tested on a set of data on wild-type acetylcholinesterase and 18 charge mutants recently obtained by Brownian dynamics simulations. A good correlation between the average ...

PubMed

70
Toxic effects of chlorpyrifos on antioxidant enzymes and target enzyme acetylcholinesterase interaction in mosquito fish, Gambusia affinis.
2008-03-29

The recovery effect of chlorpyrifos (CPF) on antioxidant enzymes, locomotor behaviour and the target enzyme acetylcholinesterase (AChE) interaction were studied after exposure to 297?gL(-1) (LC(50) for 96h) in mosquito fish, Gambusia affinis. Activities of the antioxidant enzymes-superoxide ...

PubMed

71
Comparison of Human and Guinea Pig Acetylcholinesterase Sequences and Rates of Oxime-Assisted Reactivation.
2010-01-01

Poisoning via organophosphorus (OP) nerve agents occurs when the OP binds and inhibits the enzyme acetylcholinesterase (AChE). This enzyme is responsible for the metabolism of the neurotransmitter acetylcholine (ACh) which transmits signals between nerves...

National Technical Information Service (NTIS)

72
CONFORMATIONAL STUDIES ON THE ACTIVE SITE OF ...

... Title : CONFORMATIONAL STUDIES ON THE ACTIVE SITE OF ACETYLCHOLINESTERASE BY ELECTRON PARAMAGNETIC RESONANCE,. ...

DTIC Science & Technology

73
Synthesis and discovery of novel hexacyclic cage compounds as inhibitors of acetylcholinesterase.
2011-05-08

Hexacyclic derivatives share vital pharmacological properties, considered useful in Alzheimer's disease. The aim of this study was synthesis and its evaluation for acetyl cholinesterase inhibitory activity of novel hexacyclic analogues. Compound 4f, showed potent inhibitory activity against acetyl cholinesterase enzyme with IC(50) 0.72 ...

PubMed

74
Morphine-Induced Changes in the Activity of Enzymes Involved in Neutrotransmitter Metabolism in Specific Brain Regions of the Tolerant Rat.
1974-01-01

The activities of choline acetyl transferase (E.C.2.3.1.6.), acetylcholinesterase (E.C.3.1.1.7.) and monoamine oxidase (E.C.1.4.3.4.) were determined in the hippocampus, thalamus, hypothalamus, cerebral cortex and basal ganglia of groups of rats sacrifice...

National Technical Information Service (NTIS)

75
Substrate Preferences of Wild and a Mutant House Fly ...
1978-05-08

... Title : Substrate Preferences of Wild and a Mutant House Fly Acetylcholinesterase and a Comparison with the Bovine Erythrocyte Enzyme,. ...

DTIC Science & Technology

76
Subacute Low Dose Nerve Agent Exposure Causes DNA ...
2005-10-01

... Indeed, in the present study, increased DNA fragmentation could be ... action on acetylcholinesterase, the enzyme that degrades the neurotransmitter ...

DTIC Science & Technology

77
The relationship between the pharmacokinetics, cholinesterase inhibition and facilitation of twitch tension of the quaternary ammonium anticholinesterase drugs, neostigmine, pyridostigmine, edrophonium and 3-hydroxyphenyltrimethylammonium.
1979-08-01

1 The relationship between the concentration of drug in plasma, the inhibition of erythrocyte acetylcholinesterase and the facilitation of neuromuscular transmission has been studied in the rat after the administration of neostigmine, pyridostigmine, edrophonium and 3-hydroxyphenyltrimethyl-ammonium (3-OH PTMA). 2 After the administration of neostigmine or pyridostigmine, ...

PubMed Central

78
Study of the acetylcholinesterase activity of Ascaridia galli: kinetic properties and the effect of anthelmintics.
1991-01-01

Acetylcholinesterase (EC 3.1.1.7) activity was demonstrated in whole worm homogenates of adult Ascaridia galli with acetylthiocholine as substrate. The pH optimum was not measurable because of an autohydrolysis of the substrate. The Michaelis constant (Km) was 4 mM with saturation by excess substrate. Optimum enzyme ...

PubMed

79
In vitro enzyme inhibition activities of crude ethanolic extracts derived from medicinal plants of Pakistan.
2005-09-01

Twenty two crude ethanolic extracts from 14 indigenous medicinal plants were subjected to enzyme inhibition screening against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase enzymes (LO). Three extracts showed activity against AChE, nine extracts were found to be ...

PubMed

80
Screening the methanol extracts of some Iranian plants for acetylcholinesterase inhibitory activity

Acetylcholinesterase (AChE) is the main enzyme for the breakdown of acetylcholine. Nowadays, usage of the inhibitors of this enzyme is one of the most important types of treatment of mild to moderate neurodegenerative diseases such as Alzheimer�s disease. Herbal medicines can be a new source of inhibitors of this ...

PubMed Central

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81
Inhibitory effect of lithium on nucleotide hydrolysis and acetylcholinesterase activity in zebrafish (Danio rerio) brain.
2011-05-15

Lithium has been used as an effective antimanic drug in humans and it is well known for its effects on neuropsychiatric disorders and neuronal communication. ATP and adenosine are important signaling molecules, and most nerves release ATP as a fast co-transmitter together with classical neurotransmitters such as acetylcholine. In this study, we evaluated the in vitro and in vivo effects of lithium ...

PubMed

82
Inhibitory effect of Artemisia asiatica alkaloids on acetylcholinesterase activity from rat PC12 cells.
2000-06-30

We screened 42 Korean traditional tea plants to determine the inhibitory effect of acetylcholinesterase and attenuation of toxicity induced by amyloid-beta peptide, which were related to the treatment of Alzheimer's disease (AD). The methanolic extract from Artemisia asiatica among tested 42 tea plants, showed the highest inhibitory effect (48%) on ...

PubMed

83
Molecular Dynamics of Acetylcholinesterase Dimer complexed with Tacrine.
1997-01-01

We have studied the dynamic properties of acetylcholinesterase dimer from Torpedo californica liganded with tacrine (AChE-THA) in solution using molecular dynamics. The simulation reveals fluctuations in the width of the primary channel to the active site that are large enough to admit substrates. Alternative entries to the active ...

E-print Network

84
Acetylcholinesterase alterations reveal the fitness cost of mutations conferring insecticide resistance
2004-02-06

BackgroundInsecticide resistance is now common in insects due to the frequent use of chemicals to control them, which provides a useful tool to study the adaptation of eukaryotic genome to new environments. Although numerous potential mutations may provide high level of resistance, only few alleles are found in insect natural populations. Then, we hypothesized that only alleles linked to the ...

PubMed Central

85
Elongation index of erythrocytes, study of activity of chosen erythrocyte enzymes, and the levels of glutathione, malonyldialdehyde in polycythemia vera (PV).
2011-01-01

The principal aim of the study was to investigate rheological properties of erythrocytes obtained from patients admitted to the clinic, and diagnosed with polycythemia vera. The polycythemia vera diagnosis was based on the WHO criteria for polycythemia vera. Using a laser rheometer SSD Rheometer-Rheodyn, the elongation index of erythrocytes was determined, indicating an increased rigidity of the ...

PubMed

86
Screening of plants used in Danish folk medicine to treat memory dysfunction for acetylcholinesterase inhibitory activity.
2005-11-08

Aqueous and methanolic extracts of 11 plants, used in Danish folk medicine for improvement of memory and cognition, and 3 Corydalis species were tested for acetylcholinesterase inhibitory activity using the Ellman colorimetric method. Significant inhibitory activity in dose-dependent manner was observed for extracts of Corydalis cava, ...

PubMed

87
Distribution of the molecular forms of acetylcholinesterase in human brain: alterations in dementia of the Alzheimer type.
1986-03-01

Acetylcholinesterase (AChE), the enzyme that degrades acetylcholine, is a heterogeneous enzyme that can be separated into multiple molecular forms. A tetrameric membrane-bound form (G4) and a monomeric soluble form (G1) are the two predominant enzyme species in mammalian brain. The distribution of AChE molecular ...

PubMed

88
Acetylcholinesterase-ISFET based system for the detection of acetylcholine and acetylcholinesterase inhibitors.
2006-03-10

A bioelectronic hybrid system for the detection of acetylcholine esterase (AChE) catalytic activity was assembled by way of immobilizing the enzyme to the gate surface of an ion-sensitive field-effect transistor (ISFET). Photometric methods used to characterize bonded enzyme and linker layers on silicon substrates confirm the existence ...

PubMed

89
Continuum Simulations of Acetylcholine Diffusion with Reaction-determined Boundaries in

and postsynaptic mem- branes until they are hydrolyzed by acetylcholinesterase (AChE), the biomolec- ular off-switch for synaptic transmission. AChE is present as clusters of three tetramers suspended by collagen stalks bound molecules per second per AChE active site in the case of hu- man enzyme. Therefore, it provides a very

E-print Network

90
A Modular Treatment of Molecular Traffic Through the Active Site of Cholinesterase

of enzymes that fall broadly into two types: acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). They are distinguished pri- marily by their substrate specificity: AChE hydrolyzes the natural neurotransmitter substrates (Chatonnet and Lockridge, 1989). Vertebrates contain both AChE and BChE, which prob- ably

E-print Network

91
Biochemical Monitoring of Acetylcholinesterase Sensitivity to Organophosphorus Insecticides in Glassy-Winged ...

... is described that measures the sensitivity of acetylcholinesterase (AChE) activity to inhibition by organophosphorus (OP) insecticides in ... for resistant individuals. The technique will also measure ACh...

NBII National Biological Information Infrastructure

92
Acetylcholinesterase Inhibitors on the Spinal Cord: Actions of ...
1990-08-22

... C.-Y., and Wu, M.-T. (1986) Kinetic studies and strcture activity relationships akbispyddinium oximes Srseactivator of acetylcholin-esterase inhibited ...

DTIC Science & Technology

93
A Simple and Rapid Chromatographic Method for the Immobilization of Acetylcholinesterase from Electric Eel.
1975-01-01

Acetylcholinesterase from electric eel is selectively immobilized on Amberlite IR-120 resin with Al(3+) ions. Immobilized acetylcholinesterase activity is stable at least for 85 days in the wet state at 10 C and for 180 days in the dry state at room tempe...

National Technical Information Service (NTIS)

94
Cholinesterases as markers of inflammatory process in rats infected with Leptospira interrogans sorovar icterohaemorrhagiae.
2011-09-15

The aim of this study was evaluate changes in the cholinesterase activity in blood, lymphocytes and serum of rats infected whit Leptospira interrogans sorovar icterohaemorrhagiae. Sixty adult Wistar rats were divided into six uniform groups, three control groups and three test groups. The animals from test group were intraperitoneally inoculated with 1 ml of medium containing ...

PubMed

95
A Comparative Study of Spin-Labeled Serine Enzymes ...
1971-12-01

... Title : A Comparative Study of Spin-Labeled Serine Enzymes: Acetylcholinesterase, Trypsin, alpha-Chymotrypsin, Elastase, and Subtilisin. ...

DTIC Science & Technology

96
An evaluation of the inhibition of human butyrylcholinesterase and acetylcholinesterase by the organophosphate chlorpyrifos oxon
2009-12-01

Acetylcholinesterase (EC 3.1.1.7) and butyrylcholinesterase (EC 3.1.1.8) are enzymes that belong to the superfamily of alpha/beta-hydrolase fold proteins. While they share many characteristics, they also possess many important differences. For example, whereas they have about 54% amino acid sequence identity, the active site gorge of ...

Energy Citations Database

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