Butyrylthiocholine
Acetylcholinesterase
Cholinesterase Inhibitors
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
Tetraisopropylpyrophosphamide
Thiocholine
Sarin
Soman
Chemical Warfare Agents
Cholinesterase Reactivators
Dimethoate
Organothiophosphorus Compounds
Organophosphate Poisoning
Acetylthiocholine
Organophosphorus Compounds
Isoflurophate
Echothiophate Iodide
Organophosphates
Carbon-containing phosphoric acid derivatives. Included under this heading are compounds that have CARBON atoms bound to one or more OXYGEN atoms of the P(=O)(O)3 structure. Note that several specific classes of endogenous phosphorus-containing compounds such as NUCLEOTIDES; PHOSPHOLIPIDS; and PHOSPHOPROTEINS are listed elsewhere.
Chlorpyrifos
Succinylcholine
A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.
Cocaine
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.
Oximes
Phenylcarbamates
Tacrine
Torpedo
Insecticides
Tritolyl Phosphates
Pralidoxime Compounds
Various salts of a quaternary ammonium oxime that reconstitute inactivated acetylcholinesterase, especially at the neuromuscular junction, and may cause neuromuscular blockade. They are used as antidotes to organophosphorus poisoning as chlorides, iodides, methanesulfonates (mesylates), or other salts.
Physostigmine
Enzyme Reactivators
Obidoxime Chloride
Antibodies
Citrus sinensis
Citrus
Camellia sinensis
Monoamine Oxidase
An enzyme that catalyzes the oxidative deamination of naturally occurring monoamines. It is a flavin-containing enzyme that is localized in mitochondrial membranes, whether in nerve terminals, the liver, or other organs. Monoamine oxidase is important in regulating the metabolic degradation of catecholamines and serotonin in neural or target tissues. Hepatic monoamine oxidase has a crucial defensive role in inactivating circulating monoamines or those, such as tyramine, that originate in the gut and are absorbed into the portal circulation. (From Goodman and Gilman's, The Pharmacological Basis of Therapeutics, 8th ed, p415) EC 1.4.3.4.
Tea
Medical Laboratory Science
Technology, High-Cost
Laboratories, Dental
Neuroprotective Agents
Drugs intended to prevent damage to the brain or spinal cord from ischemia, stroke, convulsions, or trauma. Some must be administered before the event, but others may be effective for some time after. They act by a variety of mechanisms, but often directly or indirectly minimize the damage produced by endogenous excitatory amino acids.
Genetic analysis of collagen Q: roles in acetylcholinesterase and butyrylcholinesterase assembly and in synaptic structure and function. (1/406)
Acetylcholinesterase (AChE) occurs in both asymmetric forms, covalently associated with a collagenous subunit called Q (ColQ), and globular forms that may be either soluble or membrane associated. At the skeletal neuromuscular junction, asymmetric AChE is anchored to the basal lamina of the synaptic cleft, where it hydrolyzes acetylcholine to terminate synaptic transmission. AChE has also been hypothesized to play developmental roles in the nervous system, and ColQ is also expressed in some AChE-poor tissues. To seek roles of ColQ and AChE at synapses and elsewhere, we generated ColQ-deficient mutant mice. ColQ-/- mice completely lacked asymmetric AChE in skeletal and cardiac muscles and brain; they also lacked asymmetric forms of the AChE homologue, butyrylcholinesterase. Thus, products of the ColQ gene are required for assembly of all detectable asymmetric AChE and butyrylcholinesterase. Surprisingly, globular AChE tetramers were also absent from neonatal ColQ-/- muscles, suggesting a role for the ColQ gene in assembly or stabilization of AChE forms that do not themselves contain a collagenous subunit. Histochemical, immunohistochemical, toxicological, and electrophysiological assays all indicated absence of AChE at ColQ-/- neuromuscular junctions. Nonetheless, neuromuscular function was initially robust, demonstrating that AChE and ColQ do not play obligatory roles in early phases of synaptogenesis. Moreover, because acute inhibition of synaptic AChE is fatal to normal animals, there must be compensatory mechanisms in the mutant that allow the synapse to function in the chronic absence of AChE. One structural mechanism appears to be a partial ensheathment of nerve terminals by Schwann cells. Compensation was incomplete, however, as animals lacking ColQ and synaptic AChE failed to thrive and most died before they reached maturity. (+info)The anticancer prodrug CPT-11 is a potent inhibitor of acetylcholinesterase but is rapidly catalyzed to SN-38 by butyrylcholinesterase. (2/406)
Patients treated with high doses of CPT-11 rapidly develop a cholinergic syndrome that can be alleviated by atropine. Although CPT-11 was not a substrate for acetylcholinesterase (AcChE), in vitro assays confirmed that CPT-11 inhibited both human and electric eel AcChE with apparent K(i)s of 415 and 194 nM, respectively. In contrast, human or equine butyryl-cholinesterase (BuChE) converted CPT-11 to SN-38 with K(m)s of 42.4 and 44.2 microM for the human and horse BuChE, respectively. Modeling of CPT-11 within the predicted active site of AcChE and BuChE corroborated experimental results indicating that, although the drug was oriented correctly for activation, the constraints dictated by the active site gorge were such that CPT-11 would be unlikely to be activated by AcChE. (+info)Cholinesterases in neural development: new findings and toxicologic implications. (3/406)
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 observations indicate that organophosphorus exposure can affect DNA synthesis and cell survival in neonatal rat brain. New evidence that acetylcholinesterase may have a direct role in neuronal differentiation provides additional grounds for interest in the developmental toxicity of anticholinesterases. For example, correlative anatomic studies show that transient bursts of acetylcholinesterase expression often coincide with periods of axonal outgrowth in maturing avian, rodent, and primate brain. Some selective cholinesterase inhibitors effectively suppress neurite outgrowth in model systems like differentiating neuroblastoma cells and explanted sensory ganglia. When enzyme expression is altered by genetic engineering, acetylcholinesterase levels on the outer surface of transfected neurons correlate with ability to extend neurites. Certain of these "morphogenic" effects may depend on protein-protein interactions rather than catalytic acetylcholinesterase activity. Nonetheless, it remains possible that some pesticides interfere with important developmental functions of the cholinesterase enzyme family. (+info)Failure to confirm a synergistic effect between the K-variant of the butyrylcholinesterase gene and the epsilon4 allele of the apolipoprotein gene in Japanese patients with Alzheimer's disease. (4/406)
To confirm a synergistic effect between the polymorphic K variant of the butyrylcholinesterase (BChE-K) gene and the epsilon4 allele of the apolipoprotein E (APOE) gene in Alzheimer's disease, the frequency of the BChE-K allele was re-examined in a large series of Japanese patients with Alzheimer's disease and controls. Two hundred and three patients with Alzheimer's disease and 288 age and sex matched controls were genotyped by polymerase chain reaction and restriction fragment length polymorphism for BChE-K and APOE. No changes were found in the frequency of BChE-K, either in the Alzheimer's disease group as a whole (0.17 v 0.14; p=0.36) or in early (0.16 v 0.16; p=0.98) or late (0.17 v 0.13; p=0.24) onset patients compared with age matched controls. The study failed to confirm the findings of a previous study which found a significantly higher incidence of BChE-K in patients with Alzheimer's disease with APOE epsilon4 allele than in controls. In the Japanese population studied here, there was no association between BChE-K and Alzheimer's disease, nor an interaction between BChE-K and APOE epsilon4 allele. (+info)Anticholinesterase effects of huperzine A, E2020, and tacrine in rats. (5/406)
AIM: To compare the anticholinesterase effects of huperzine A (Hup A), E2020, and tacrine in rats. METHODS: Spectrophotometry was used to determine AChE activity in brain and BuChE activity in serum. RESULTS: Following intragastric gavage, Hup A, E2020, and tacrine all produced dose-dependent inhibitions of brain AChE. Oral Hup A exhibited a higher inhibition than E2020 and tacrine. Tacrine was more effective in inhibiting serum BuChE correlated with severe peripheral adverse effects. The BuChE activity was less affected by Hup A and E2020. After a single oral dose of Hup A, a relatively steady state of AChE inhibition produced, which was longer than that after E2020 and tacrine. No change in the cholinesterase inhibition was seen for the 3 drugs following repeated i.g. medications. CONCLUSION: Hup A i.g. exhibited a higher efficacy, a longer duration of action, and a more selective inhibition on AChE than E2020 and tacrine. (+info)Effects of synthetic (-)-huperzine A on cholinesterase activities and mouse water maze performance. (6/406)
AIM: To compare the effects of synthetic and natural (-)-huperzine A (Hup A) on cholinesterase and mouse water maze performance. METHODS: Spectrophotometry was used to determine cholinesterase activity. Mouse water maze was used to evaluate nootropic effect. RESULTS: The IC50 of synthetic Hup A for acetylcholinesterase (AChE) of rat cortex and rat erythrocyte membrane determined in vitro were 64.7 (52.6-79.5) and 53.9 (43.6-66.6) nmol.L-1, respectively, and for butyrylcholinesterase of rat serum was 53.6 (44.9-63.8) mumol.L-1. Synthetic Hup A 0.12-0.48 mg.kg-1 ig produced a dose-dependent inhibition of brain AChE in mice. Synthetic Hup A 0.05 mg.kg-1 ig attenuated scopolamine-induced impairment of spatial memory. The efficacy of synthetic Hup A was the same as natural Hup A. CONCLUSION: Synthetic Hup A yielded an in vitro and in vivo pharmacological profile of activities similar to that of natural Hup A. (+info)Characteristics of recombinant human butyrylcholinesterase. (7/406)
AIM: To study the biochemical-pharmacological properties of the recombinant human butyrylcholinesterase (rhBChE) and thereby to size up the potential possibility of using it as a detoxifying agent in succinylcholine intoxication. METHODS: CHO-dhfr cells were transfected with plasmids by electroporation. BChE activity was determined colorimetrically by 5, 5'-dithiobis-(2-nitrobenzoic acid) (DTNB) method. Antigenicity was estimated by enzyme-linked immunosorbent assay and Western blot. RESULTS: The maximal expression amounted to 25.83 ng.h-1/10(6) cells. The rhBChE was highly similar to the native human BChE (nhBChE) in terms of its catalytic property, substrate affinity, inhibitor sensitivity, reactivation, stability, and immunoreactivity with anti-nhBChE antibodies. Mice challenged with 1.5 lethal dose of succinylcholine preincubated with rhBChE survived without any symptoms of intoxication. CONCLUSION: The rhBChE and nhBChE exhibit similar biochemical-pharmacological features. It is of potential value in practical use. (+info)Inhibitory effects of huperzine B on cholinesterase activity in mice. (8/406)
AIM: To determine the anticholinesterase properties of huperzine B (Hup B) and compare with tacrine in vitro and in vivo. METHODS: Spectrophotometry was used to determine ChE activity. RESULTS: Hup B showed much more selective inhibition to acetylcholinesterase (AChE) than tacrine. The IC50 ratios of Hup B and tacrine for butyrylcholinesterase (BuChE): AChE were 65.8 and 0.54, respectively. Hup B ig exhibited higher efficacy on the inhibition of brain AChE than that of tacrine. Tacrine was more effective in the inhibition of serum BuChE in mice with severe concomitant peripheral adverse effects than Hup B. A single ig dose of Hup B produced steady state of AChE inhibition in 4 h. CONCLUSION: Hup B exhibits higher selectivity and efficacy in the inhibition of AChE, and lower toxicity in mice than tacrine. (+info)
Liver and serum butyrylcholinesterase activity in scorbutic guinea pigs
Butyrylcholinesterase: Substrates
Butyrylcholinesterase/BCHE Products: R&D Systems
Assessment of platelets morphological changes and serum butyrylcholinesterase activity in children with diabetic ketoacidosis:...
Association between butyrylcholinesterase K variant and the Alzheimer type neuropathological changes in apolipoprotein E ε4...
Overlapping drug interaction sites of human butyrylcholinesterase dissected by site-directed mutagenesis. - Semantic Scholar
Comparison of the Inhibition of Monoamine Oxidase and Butyrylcholinesterase Activities by Infusions from Green Tea and Some...
Flavonoids as Inhibitors of Human Butyrylcholinesterase Variants
Microcalorimetric study of the inhibition of butyrylcholinesterase by paraoxon. - Université de Limoges
Structural aspects of 4-aminoquinolines as reversible inhibitors of human acetylcholinesterase and butyrylcholinesterase
Molecules | Free Full-Text | Novel Bisquaternary Oximes-Reactivation of Acetylcholinesterase and Butyrylcholinesterase...
Butyrylcholinesterase Genetic Variants: Association with Cocaine Dependence and Related Phenotypes - pdf descargar
PharmAthenes Recombinant Butyrylcholinesterase (rBChE) May Play A Neuroprotective Role in Alzheimer... ( ANNAPOLIS Md....
中国科学院大连化学物理研究所机构知识库(DICP OpenIR): Fundamental Reaction Pathway and Free Energy Profile for Butyrylcholinesterase-Catalyzed...
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Dysregulated cholinergic network as a novel biomarker of poor prognostic in patients with head and neck squamous cell carcinoma...
RCSB PDB
- 4B0P: Crystal structure of soman-aged human butyrylcholinesterase in complex with methyl 2-...
1p0m - Proteopedia, life in 3D
Wild-Type and A328W Mutant Human Butyrylcholinesterase Tetramers Expressed in Chinese Hamster Ovary Cells Have a 16-Hour Half...
4b0p - Proteopedia, life in 3D
Butyrylcholinesterase/BCHE Antibody (3E8) - BSA Free (NBP1-05127): Novus Biologicals
Dokument bez názvu
Genetic Analysis of Collagen Q: Roles in Acetylcholinesterase and Butyrylcholinesterase Assembly and in Synaptic Structure and...
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Candidate gene association studies of genes involved in neuronal cholinergic transmission in Alzheimers disease suggests...
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HUP 13 - AdisInsight
Article abstract | Medical Science Monitor
Inhibicija kolinesterazâ karbamatom albuterola | Repozitorij Prirodoslovno-matematičkog fakulteta
Wiley: Anticholinesterase Pesticides: Metabolism, Neurotoxicity, and Epidemiology - Tetsuo Satoh, Ramesh C. Gupta
Publications | Computational Biology and Drug Design Group
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OriGene - BCHE (BC099977) shRNA
Anti-Cocaine [K2-3]
Opinel 10 Carbon Buche - CO2air.de
BCHE 7 W 2R2 10%: 2-1623732-8 CGS | TE Connectivity
Dibucaine number - Wikipedia
Acetylcholinesterase Inhibitors with Photoswitchable Inhibition of β‑Amyloid Aggregation - University of Regensburg...
Most Efficient Cocaine Hydrolase Designed by Virtual Screening of Transition States | Drugs-Forum
Synthesis of Some New 4,5-Diphenyl 3-(2H) Pyridazinone Derivatives and Evaluation of Their Inhibitory Activities on...
Glial-derived proteins activate cultured astrocytes and enhance beta amyloid-induced glial activation.
Recette Buche De Noel Sans Chocolat - De délicieuses recettes faciles
Recette Buche De Noel Original - De délicieuses recettes faciles
Ellman RFS<...
Journal Describes Anti-Cocaine Vaccine - Redorbit
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Article
Buche de Noel (Yule Log) » Cooking Queen
Mocha Buche de Noel - Yule Log Recipe
Echothiophate Iodide Ophthalmic - Side Effects, Dosage, Interactions - Drugs - Everyday Health
What is the association of cocaine toxicity with trauma?
What is the association of cocaine toxicity with trauma?
substrate activation - oi
BCHE - ddPCR Primer Pair - EvaGreen - Digital PCR | PrimePCR | Bio-Rad
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Ellman Surgitron FFPF EMC Repair Evaluation - All States M.E.D.
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Slices of life: Life when the A goes *w*y - Jacksonville Journal-Courier
Structural Stability of Human Butyrylcholinesterase under High Hydrostatic Pressure. - Bentham
Human butyrylcholinesterase is a nonspecific enzyme of clinical, pharmacological and toxicological significance. Although the ... This transient process in native butyrylcholinesterase presumably involves conformational changes of the enzyme at both ... Structural Stability of Human Butyrylcholinesterase under High Hydrostatic Pressure. Biochimica et Biophysica Acta (BBA)- ... hydrostatic pressure dependence of the intrinsic tryptophan fluorescence in native and salted human butyrylcholinesterase was ...
Butyrylcholinesterase K variant and Alzheimer's disease - Murdoch University Research Repository
The butyrylcholinesterase K variant was found to be of increased allele frequency in patients with sporadic Alzheimers disease ... 1999) Butyrylcholinesterase K variant and Alzheimers disease. Journal of Neurology, 246 (5). pp. 369-370. ... This study attempted to corroborate findings on the association between butyrylcholinesterase K variant and Alzheimers disease ...
Decreased Activity of Circulating Butyrylcholinesterase in Blood Is an Independent Prognostic Marker in Pancreatic Cancer...
Erratum: Butyrylcholinesterase K variant on chromosome 3q is associated with Type II diabetes in white Caucasian subjects ...
Structural modifications of 4-aryl-4-oxo-2-aminylbutanamides and their acetyl- and butyrylcholinesterase inhibitory activity....
Structural modifications of 4-aryl-4-oxo-2-aminylbutanamides and their acetyl- and butyrylcholinesterase inhibitory activity. ... and butyrylcholinesterase inhibitory activity. Structural variations included cycloalkylamino group attached to C2 position of ... and butyrylcholinesterase inhibitory activity. Structural variations included cycloalkylamino group attached to C2 position of ... and butyrylcholinesterase inhibitory activity. Investigation of AChE-ligand interactions by docking calculations and molecular ...
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Određivanje antioksidacijske aktivnosti i inhibicijskog djelovanja vodenog ekstrakta gorke naranče (Citrus aurantium L.) na...
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Funding - McDonald/Nandi Lab
... expressing recombinant butyrylcholinesterase (rBChE). Goal: Production of recombinant butyrylcholinesterase (rBChE) in rice ... Goal: Production of recombinant butyrylcholinesterase (rBChE) in rice cell suspension culture. Agency: SAIC, Inc. ... Title: Alternative Manufacturing Processes for Recombinant Human Butyrylcholinesterase. ... in vitro sialylation technology for plant expressed proteins and to demonstrate proof of concept using butyrylcholinesterase ( ...
2WIK | Genus
dichlorvos spider mites
A suitable detergent for tissue extraction as it does not inhibit butyrylcholinesterase % respectively 1974. Ops also occurs ... L EC butyrylcholinesterase ( Boeck et al few decades later, the mites unaffected! Peppermint soap RUP ) and crotoxyphos, ... Tween 20 is a suitable detergent for tissue extraction as it does not inhibit butyrylcholinesterase. The initial stages of ...
Novel 20(S)-sulfonylamidine derivatives of camptothecin and the use thereof as a potent antitumor agent: a patent evaluation of...
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Publications | The Douglas Research Centre
Publications | The Douglas Research Centre
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Memory impairment is the cardinal early feature of Alzheimer's disease (AD) - Discovery of Small-Molecule Inhibitors of Receptor
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EP300 - Gentaur
BChE2
- We estimated the frequencies of serum butyrylcholinesterase (BChE) alleles in three tribes of Mapuche Indians from southern Chile, using enzymatic methods, and we estimated the frequency of allele BCHE*K in one tribe using primer reduced restriction analysis (PCR-PIRA). (uai.cl)
- Background: The inhibition of both hydrolysis products of acetylcholine (ACh), Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE), is essential for successful treatment of Alzhemier patients. (sakarya.edu.tr)
Inhibitory4
- Structural modifications of 4-aryl-4-oxo-2-aminylbutanamides and their acetyl- and butyrylcholinesterase inhibitory activity. (ac.rs)
- Congeneric set of thirty-eight 4-aryl-4-oxo-2-(N-aryl/cycloalkyl)butanamides has been designed, synthesized and evaluated for acetyl- and butyrylcholinesterase inhibitory activity. (ac.rs)
- TY - JOUR AU - Vitorović-Todorović, Maja D. AU - Koukoulitsa, Catherine AU - Juranić, Ivan AU - Mandić, Ljuba M. AU - Drakulić, Branko PY - 2014 UR - http://cer.ihtm.bg.ac.rs/handle/123456789/2688 AB - Congeneric set of thirty-eight 4-aryl-4-oxo-2-(N-aryl/cycloalkyl)butanamides has been designed, synthesized and evaluated for acetyl- and butyrylcholinesterase inhibitory activity. (ac.rs)
- PB - Elsevier France-Editions Scientifiques Medicales Elsevier, Paris T2 - European Journal of Medicinal Chemistry T1 - Structural modifications of 4-aryl-4-oxo-2-aminylbutanamides and their acetyl- and butyrylcholinesterase inhibitory activity. (ac.rs)
Enzyme2
- Human butyrylcholinesterase is a nonspecific enzyme of clinical, pharmacological and toxicological significance. (bentham.co.uk)
- This transient process in native butyrylcholinesterase presumably involves conformational changes of the enzyme at both tertiary and secondary structure levels. (bentham.co.uk)
Activity1
- Decreased Activity of Circulating Butyrylcholinesterase in Blood Is an Independent Prognostic Marker in Pancreatic Cancer Patients. (limcr.at)
Human2
- Structural Stability of Human Butyrylcholinesterase under High Hydrostatic Pressure. (bentham.co.uk)
- In this work, hydrostatic pressure dependence of the intrinsic tryptophan fluorescence in native and salted human butyrylcholinesterase was studied up to the maximum pressure at ambient temperature of about 1200 MPa. (bentham.co.uk)
Patients1
- The butyrylcholinesterase K variant was found to be of increased allele frequency in patients with sporadic Alzheimer's disease. (edu.au)
Association1
- This study attempted to corroborate findings on the association between butyrylcholinesterase K variant and Alzheimer's disease. (edu.au)