... Title : Acetylcholinesterase Inhibitors on the Spinal Cord: Actions of Organophosphates in the Mammalian Spinal Cord. ...
DTIC Science & Technology
... Abstract : This report describes studies on organophosphorus (OP) inhibitors of acetylcholinesterase (AChE) in the mammalian spinal cord in which ...
The role of butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE) in regulating acetylcholine (ACh) lifetime was investigated by use of selective cholinesterase (ChE) inhibitors. Addition of tetraisopropylpyrophosphoramide (iso-OMPA) led to a 98% ...
National Technical Information Service (NTIS)
... Accession Number : AD0771149. Title : A Screening Program for Selective Inhibitors of the Phosphorylation of Acetylcholinesterase. ...
Neurofibrillary tangles and amyloid plaques express acetylcholinesterase and butyrylcholinesterase activity in Alzheimer disease. We previously reported that traditional acetylcholinesterase inhibitors such as BW284C51, tacrine, and physostigmine were more potent inhibitors of the ...
PubMed Central
.3 Acetylcholinesterase (AChE)..........................................................................13 1.3.1 Role acetylcholine AChE acetylcholinesterase AChR acetylcholine receptor ADP,ATP adenosine diphosphate extracytoplasmicions,respectively #12;vii EeAChE Electrophorus electricus AChE FT-IR fourier transform infrared
E-print Network
: Acetylcholinesterase (AChE) plays a crucial physiological role in termination of impulse transmission at cho- linergicE inhibitors. Thus ACHE is an obvious candidate gene for pharmacogenetic study of AD treatment. However, AChE polymorphism, SNP, Alzheimer's disease, adverse drug reaction. INTRODUCTION ...
Page 1. AD-A252 694 AD 111111111111111l111111111l1l111111111l1 -- e ACETYLCHOLINESTERASE INHIBITORS ON THE SPINAL CORD ...
... Organochlorine and organophosphorus compounds (inhibitors of acetylcholinesterases) including DDT, chlordane, and malathion at subtoxic ...
... of cholinergic agonists such as pilocarpine (pilo) and carbachol or acetylcholinesterase inhibitors, such as physostigmine and neostigmine (6), ...
Hypobaric hypoxia is encountered at high altitude. It has a deleterious effect on cognitive functions. An important cause of memory impairment at high altitude is the impairment of neurotransmission. The present study investigates the role of cholinergic markers in hypobaric hypoxia-induced memory impairment. Rats were exposed to hypobaric hypoxia at 6100m for 7days in a ...
PubMed
... Abstract : Lethal or near-lethal doses of acetylcholinesterase (AChE) inhibitors cause respiratory depression and cardiovascular collapse. ...
... C.-Y., and Wu, M.-T. (1986) Kinetic studies and strcture activity relationships akbispyddinium oximes Srseactivator of acetylcholin-esterase inhibited ...
Acetylcholinesterase is an enzyme responsible for the timely termination of acetylcholine action at muscarinic and nicotinic receptors, so it is essential for the normal function of cholinergic synapses. Naturally occurring acetylcholinesterase inhibitors are relatively rare, but several synthetic ...
The antagonism of acetylcholinesterase inhibitor toxicity was studied in mice. Hemicholinium-3 (HC-3) antagonized the toxicity of physostigmine and neostigmine by shifting the dose-response curve to the right, thus increasing the LD50. However, hemicholin...
Molecular docking is a frequently used method in structure-based rational drug design. It is used for evaluating the complex formation of small ligands with large biomolecules, predicting the strength of the bonding forces and finding the best geometrical arrangements. The major goal of this advanced undergraduate biochemistry laboratory exercise is to illustrate the importance and application of ...
ERIC Educational Resources Information Center
The effect of electrophilic ketones on acetylcholinesterase activity has been investigated. For example, 1-phenoxy-2-propanone, 1-chloro-3-phenoxy-2-propane, and 1-fluoro-3-phenoxy-2-propanone are competitive acetylcholinesterase inhibitors with K sub I v...
In developing antidotes to poisoning by cholinesterase (ChE) inhibitors, several potential target sites at the cholinergic synapse have been studied, including the postsynaptic receptor and acetylcholinesterase (AchE) itself. Muscarinic receptor blocking ...
This report describes continued studies on organophosphorus (OP) inhibitors of acetylcholinesterase (AChE) in the mammalian spinal cord. The mechanism and site of action of the potentiation and/or depression of synaptic transmission by the OPs are being r...
This report describes studies on organophosphorus (OP) inhibitors of acetylcholinesterase (AChE) in the mammalian spinal cord in which the mechanism and site of action of the OPs on synaptic transmission were studied with selective agonists and antagonist...
The dissociation constants have been determined and compared for a series of reversible (noncovalent) inhibitors of eel acetylcholinesterase that are structurally related to the very potent inhibitor, 1,2,3,4-tetrahydro-9-aminoacridine (THA). It is conclu...
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 ...
... Title : Screening of Organophosphorus Acid Anhydrases ... Sources by Western Blot Analysis. ... eg, acetylcholinesterase inhibitors, pesticides, and G ...
... such adaptive mechanisms are too slow to prevent the development of toxicity. Acceleration of presynaptic down-regulation by pharmacologic ...
The invention relates to improvements in the treatment of diseases, and more particularly to compounds which are potent inhibitors of acetylcholinesterase and butyrylcholinesterase.
... Title : Gene Expression Profiling of Rat Hippocampus Following Exposure to the Acetylcholinesterase Inhibitor Soman. ...
... the utility of the DRL schedule to other compounds of military relevance, including the reversible acetylcholinesterase inhibitor physostigmine. ...
... Title : Circadian Rhythms of Heart Rate and Locomotion After Treatment With Low-Dose Acetylcholinesterase Inhibitors. ...
... Page 16. 12 ACKNOWLEDGEMENTS We thank P. Burgoon, M. Quigley, PD Neifer and B. Cadarette for their technical support ...
A common feature in the Alzheimer�s disease (AD) brain is the presence of acetylcholinesterase (AChE) which is commonly associated with ?-amyloid plaques and neurofibrillary tangles (NFT). Although our understanding of the relationship between AChE and the pathological features of AD is incomplete, increasing evidence suggests that both ?-amyloid protein (A?) and abnormally ...
A radiometric method for screening acetylcholinesterase inhibitors has been described. The method is based on the production of (/sup 14/C)carbon dioxide from the hydrolysis of acetylcholine. The inhibitory concentration at 50% (IC50) values for several known acetylcholinesterase inhibitors were in agreement with ...
Energy Citations Database
... by block number) FIELD gGROUIP SU"-ROUP ~cetylcholinesterase Inhibitor Toxicity, Soman, 06 01 lonidine, Physostigmine Trihexyphenidyl, Rat ...
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 acetylcholinesterase ...
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
Examination of the enzyme structure for acetylcholinesterase (AChE) reveals two sites of ligand interaction: The peripheral site (P-site) located at the entrance of the gorge, and the acylation site (A-site) at the base of the gorge. Our goal is to develo...
Linarin (acacetin-7-O-beta-d-rutinoside) from the flower extract of Mentha arvensis showed selective dose dependent inhibitory effect on acetylcholinesterase. PMID:16815640
Organophosphorus compounds (OPs) are potent inhibitors of acetylcholinesterase (AChE). Treatment for OP poisoning is by administration of atropine sulfate, an oxime, and diazepam. Oximes such as 2-PAM are used to reactivate OP-inhibited AChE so as to rest...
Lethal or near-lethal doses of acetylcholinesterase (AChE) inhibitors cause respiratory depression and cardiovascular collapse. Lower doses, however, evoke a centrally-mediated increase in blood pressure. This hypertensive response occurs in a variety of ...
Exposure to organophosphate pesticides (OP) has been associated with sleep disorders: insomnia and ?excessive dreaming'. However neuronal mechanisms of these effects have not been analyzed. OP inhibit acetylcholinesterase activity leading to a hyperativity of the brain cholin...
EPA Science Inventory
Our previous studies on cationic and uncharged substrates and reversible aliphatic and aromatic inhibitors led to the conclusions (1) that the subsite at which the trimethylammonio group of acetylcholine (AcCh) binds to acetylcholinesterase (AcChE) is not...
The inhibitory effect of 3-diethylaminophenyl-N-methylcarbamate methiodide on rat brain acetylcholinesterase and horse plasma butyrylcholinesterase was studied in vitro. This quaternary carbamate is a more potent inhibitor of acetylcholinesterase than butyrylcholinesterase. Complete inhibition of ...
The acetylcholinesterase enzyme (AChE) was immobilized on a chromatographic support to study the effect of magnesium on the binding mechanism of five AChE inhibitors (donepezil, tacrine, galanthamine, physostigmine and huperzine). The determination of the enthalpy and entropy changes of this binding at different magnesium concentration values suggested ...
Application of acetylcholinesterase (AChE) inhibitors is the primary treatment for Alzheimer's disease. Alkaloids, such as physostigmine, galanthamine, and huperzine A, play an important role as AChE inhibitors. The aim of this work was to evaluate Himatanthus lancifolius (Muell. Arg.) Woodson, a Brazilian species ...
The roots of the Thai medicinal plant, Tabernaemontana divaricata (L.) R. Br. ex Roem. & Schult., were investigated for their content of acetylcholinesterase inhibitors. Bioassay-guided fractionation using the Ellman colorimetric method led to the isolation of two bisindole alkaloids, 19,20-dihydrotabernamine and 19,20-dihydroervahanine A. The ...
, USA) alone or in the presence of 100 lM huperzine-A (LC Laboratories) for 45 min before being fixed, when 100 nM ACh was used in conjunction with the acetylcholinesterase (AChE) inhibitor huperzine-A (100M carbachol in the absence (PI � 0.87 � 0.03, n � 3) or presence (PI � 0.87 � 0.07; n � 3) of huperzine-A (Fig
acetylcholinesterase (AChE) inhibitor, with one of the highest affinities reported for a reversible inhibitor, and a carbobicyclic moiety resembling that of another AChE inhibitor, (-)-huperzine A. Cocrystallization of huprine X with Torpedo californica AChE yielded crystals whose 3D structure was determined to 2.1 ...
The role of the rare soluble splice variant of acetylcholinesterase (AChE-R) in anxiety behavior was assayed using the elevated plus maze (EPM). The effects of pretreatment with restraint stress and the acetylcholinesterase inhibitor diisopropylfluorophosphate (DFP) were tested, as these treatments are known to ...
Acetylcholinesterase (AChE) inhibitors played an important role in developing a cure for Alzheimer' s disease. In order to study on the influence of modifications at different groups and side chains on the AChE inhibitory ability and the active sites of 7H-thiazolo[3,2-b][1,2,4]triazin-7-one derivatives, fourteen ...
The activity of acetylcholinesterase (AchE) increases rapidly after the gastrula stage of sea urchin development. In this report, changes in activity and in the molecular differentiation of AchE were investigated. AchE activity increased slightly during gastrulation and rose sharply thereafter, and was dependent on new RNA synthesis. No activity of butyrylcholinesterase was ...
... For example, 1-phenoxy-2-propanone, 1-chloro-3-phenoxy-2-propane, and 1-fluoro-3-phenoxy-2-propanone are competitive acetylcholinesterase ...
Various compounds were tested for effects on the toxicity of the insect repellent N, N-diethyl-m-toluamide (DEET) in German cockroaches, Blattella germanica (L.). Organophosphate and carbamate acetylcholinesterase inhibitors carbaryl, DEF, eserine (physostigmine, malathion and pyridostigmine bromide synergized DEET toxicity also synergized the toxicity of ...
The invention relates to substituted phenylcarbamate or naphthylcarbamate tricyclic compounds which provide highly potent and selective cholinergic agonist and blocking activity and their use as pharmaceutical agents. The invention further relates to impr...
... Keywords: Acetylcholinesterase; Acetylcholine; Radiometric ChE assay; Physostigmine; Irreversible ChE inhibitors; Titrametric ChE assay. ...
With the object of finding prophylactic drugs to prevent organophosphorus anticholinesterase poisoning, six unsymmetrical bisquaternary compounds containing large lipophilic groups were compared for their ability to inhibit phenylacetate hydrolysis and th...
... SCIENCES. Personal Author(s) : Freeman,JJ ; Kosh,JW. Report Date : 31 OCT 1983. Pagination or Media Count : 51. Abstract ...
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 the action of light. ...
... using the CHARMm module of QUANTA96 (conjugate k-st >> ak2; k-- >> k3; km >> bk3; 32; 33; see ref 22). This gradient). ...
... Abstract : The key objective of these studies is to determine the neurotoxic risk of combining acetylcholinesterase inhibitors (AChEIs) and N-methyl ...
... Abbreviations: Ach, acetylcholine; AChE, acetylcholinesterase; AChEI, acetylcholin- esterase inhibitor; ATR, atropine sulfate; AUC, area under curve ...
The Amarylidacea alkaloid galanthamine (1a) is an acetylcholinesterase inhibitor that has been evaluated as a potential agent for the treatment of Alzheimer's disease. We report a very efficient synthesis of (+ or -)-galanthamine (+ OR -)-1A from readily ...
The chemical composition and the biomolecular properties of a crude plant extract were altered through bromination leading to the discovery of an acetylcholinesterase inhibitor. PMID:21395346
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... Tacrine is a tertiary inhibitor which can penetrate the blood brain barrier, and is currently being evaluated for management of Alzheimer's disease. ...
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 potent inhibition of ...
Snake venoms are cocktails of enzymes and non-enzymatic proteins used for both the immobilization and digestion of prey. The most common snake venom enzymes include acetylcholinesterases, l-amino acid oxidases, serine proteinases, metalloproteinases and phospholipases A(2) . Higher catalytic efficiency, thermal stability and resistance to proteolysis make these enzymes ...
This article examines the role of innervation in regulating expression of acetylcholinesterase (AchE), butylcholinesterase (BuchE), and the muscarinic acetylcholine receptor (mAchR) in avian heart. Two distinct approaches are taken. The first approach exa...
Acetylcholinesterase (ACHE) is an enzyme long noted for its essential role in the termination of neurotransmission at cholinergic synapses and neuromuscular junctions. Because acetylcholinesterase is the target protein for a variety of neurotoxic compound...
To study the yet unknown role of the ubiquitous family of cholinesterases (ChoEases) in developing blood cells, the recently isolated cDNAs encoding human acetylcholinesterase and butyrylcholinesterase were used in blot hybridization with peripheral blood DNA from various leukemic patients. Hybridization signals and modified restriction patterns were ...
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 of a group of ...
... Title : Size of Acyl Group in Choline Esters Determines the Role of Choline Esters in Decarbamoylation of Alkylcarbamoyl-Acetylcholinesterase. ...
The cholinergic system is crucial for cognitive processes and the deficient acetylcholine (ACh) function has been implicated in Alzheimer�s disease (AD). Inhibitors of acetylcholinesterase (AChE), which act to enhance cholinergic function by prolonging the action of endogenously released ACh, have been used as the major therapy of AD. To understand the ...
Science Publishers Ltd. Bivalent Ligands Derived from Huperzine A as Acetylcholinesterase Inhibitors H occurring alkaloid Huperzine A (HupA) is an acetylcholinesterase (AChE) inhibitor that has been used ligand; chelate effect; huperzine A; hupyridone; tacrine; E2020. INTRODUCTION (�)-Huperzine A [(�)-Hup
Five subjects exercised on a cycle ergometer for 30 min at 55% peak VO2 on two occasions in a slightly warm environment. Pyridostigmine bromide (PYR), an acetylcholinesterase (AChE) inhibitor, was ingested (30 mg) approximately 150 min before one experime...
Three-dimensional Quantitative Structure-Activity Relationship models were designed for irreversible and reversible acetylcholinesterase inhibitors by molecular modeling methods. In case of irreversible inhibitors CoMFA (the comparative analysis of molecular fields) or CoMSIA (the comparative analysis of indexes of molecular ...
This final technical report summarizes research on application of ab initio quantum chemical techniques to enzyme inhibitors such as acetylcholinesterase. Computational techniques have been developed, tested and applied to (1) chemically related series of...
were obtained. Different from the unbinding of other AChE inhibitors, such as Huperzine from other AChE inhibitors, such as Huperzine A (HupA), which binds to the acylation site, E2020
The role of blood acetylcholinesterase in moderating the effects of organophosphate challenge in rats were tested. Adult male rats (n=42) were injected (i.v.) either with monoclonal antibodies (MAb) to rat acetylcholinesterase (EC 3.1.1.7; AChE) or normal...
The role of blood acetylcholinesterase in moderating the effects of organophosphate challenge in rats were tested. dult male rats (n=42) were injected (i.v.) either with monoclonal antibodies (MAb) to rat acetylcholinesterase (EC 3.1.1.7; AChE) or normal mouse IgG (controls). wo ...
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 activity. The ...
of the acetylcholinesterase (AChE) monolayer at the air/aqueous interface. The results show that it is the ionogenic groups/aqueous interface rather than an organized AChE monolayer. Furthermore, the AFM images of the AChE LB film prepared Acetylcholinesterase (AChE) is an essential enzyme for nerve tissue. Its principal biological ...
... of Matrix Metalloproteinases and Their Tissue Inhibitors in Human Breast Adenocarcinoma. ... in check by inhibitors in the tissues (tissue inhibitors of ...
One of the major neuropathological hallmarks in Alzheimer's disease (AD) is the loss of cholinergic neurones of the nucleus basalis of Meynert (NbM). This consistent finding gave rise to the 'cholinergic' hypothesis of AD and lead to the subsequent development of acetylcholinesterase (AChE) inhibitors; the first class of drug to be approved for the ...
The involvement of the cholinergic system in learning and memory in honeybees has been well established using olfactory conditioning. We examined the effect of Methyl Parathion (MeP), an acetylcholinesterase inhibitor of the organo-phosphate family, on the learning and recall of visual and olfactory discrimination tasks in honeybees. One of our ...
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 degradation ...
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)
Vascular dementia (VaD) is a disorder with no cure and limited treatment options. Similarities between VaD and Alzheimer's disease (AD) arise on a number of levels. Both involve progressive decline in cognition, functional ability, and behavior, and there is evidence for a central role of reduced cholinergic neurotransmission in the two illnesses. Treatment strategies in VaD ...
BackgroundAlzheimer's disease (AD) is the most common cause of dementia characterized by progressive cognitive impairment in the elderly people. The most dramatic abnormalities are those of the cholinergic system. Acetylcholinesterase (AChE) plays a key role in the regulation of the cholinergic system, and hence, inhibition of AChE has emerged as one of ...
Butyrylcholinesterase (BChE), a serine hydrolase biochemically related to the cholinergic enzyme Acetylcholinesterase (AChE), is found in many mammalian tissues, such as serum and central nervous system, but its physiological role is still unclear. BChE is an important human plasma esterase, where it has detoxifying roles. Furthermore, ...
A computation docking study of the highly potent, non-nitrogen containing, acetylcholinesterase inhibitor (+)-Arisugacin A is presented. The model suggests that (+)-arisugacin A is a dual binding site covalent inhibitor of AChE. These findings are examined in the context of Alzheimer's disease-modifying therapeutic design. ...
Acute toxicity (96-h LC50) of malathion was tested using five species of freshwater fish, namely, topmouth gudgeon (Pseudorasbora parva), goldfish (Carassius auratus), nile tilapia (Tilapia nilotica), mosquitofish (Gambusia affinis), and rainbow trout (Salmo gairdneri). Correlation was found between susceptibility and biochemical parameters such as activity of brain ...
