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cholinesterase inhibitor

Hiroyuki Ohbe, Taisuke Jo, Hiroki Matsui, Kiyohide Fushimi, Hideo Yasunaga
INTRODUCTION: In contrast to information on the effects of organophosphate, pesticide, or environmental exposures, data on cholinergic crisis caused by pharmaceutical cholinesterase inhibitors are sparse. The present study aimed to describe the characteristics, demographics, and mortality of patients with cholinergic crisis caused by pharmaceutical cholinesterase inhibitors using a nationwide inpatient database in Japan. METHODS: We identified patients diagnosed with cholinergic crisis as a result of taking cholinesterase inhibitor medications in the Japanese Diagnosis Procedure Combination inpatient database from July 2010 to March 2016...
June 15, 2018: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
Rafael Blesa, Kazuhiro Toriyama, Kengo Ueda, Sean Knox, George Grossberg
INTRODUCTION: Alzheimer's disease (AD) is the most common cause of dementia, characterized by a progressive decline in cognition and function. Current treatment options for AD include the cholinesterase inhibitors (ChEIs) donepezil, galantamine, and rivastigmine, as well as the N-methyl-D-aspartate receptor antagonist memantine. Treatment guidelines recommend the use of ChEIs as standard of care first-line therapy. Several randomized clinical studies have demonstrated the benefits of ChEIs on cognition, global function, behavior and activities of daily living...
June 12, 2018: Current Alzheimer Research
Giacobini Ezio, Pepeu Giancarlo
This review has two aims. First, to examine whether or not sex and gender may influence the brain cholinergic system in animals and in humans. Second, to examine the available evidence of sexually dimorphic response to the therapeutic and toxic effects of cholinesterase inhibitors. Animal research reveals no marked difference in the general morphology of the brain cholinergic system but subtle functional gender differences have been reported. In humans, gender differences in nucleus basalis of Meynert (NBM) exist...
June 12, 2018: Current Alzheimer Research
Chamseddine Derabli, Imen Boualia, Ahmed B Abdelwahab, Raouf Boulcina, Chawki Bensouici, Gilbert Kirsch, Abdelmadjid Debache
In this work, we describe the preparation of some new Tacrine analogues modified with a pyranopyrazole moiety. A one-pot multicomponent reaction of 3-methyl-1H-pyrazol-5(4H)-one, aryl(or hetero)aldehydes, malononitrile and cyclohexanone involving a Friedländer condensation led to the title compounds. The synthesized heterocyclic analogues of this molecule were evaluated in vitro for their AChE and BChE inhibitory activities in search for potent cholinesterase enzyme inhibitors. Most of the synthesized compounds displayed remarkable AChE inhibitory activities with IC50 values ranging from 0...
June 1, 2018: Bioorganic & Medicinal Chemistry Letters
Ehsan Ullah Mughal, Asif Javid, Amina Sadiq, Shahzad Murtaza, Muhammad Naveed Zafar, Bilal Ahmad Khan, Sajjad Hussain Sumra, Muhammad Nawaz Tahir, Kanwal, Khalid Mohammed Khan
The prime objective of this research work is to prepare readily soluble synthetic analogues of naturally occurring 3-O-flavonol glycosides and then investigate the influence of various substituents on biological properties of synthetic compounds. In this context, a series of varyingly substituted 3-O-flavonol glycosides have been designed, synthesized and characterized efficiently. The structures of synthetic molecules were unambiguously corroborated by IR, 1 H, 13 C NMR and ESI-MS spectroscopic techniques...
June 1, 2018: Bioorganic & Medicinal Chemistry
Hsiao Shan Cho, Li Kai Huang, Yao Tung Lee, Lung Chan, Chien Tai Hong
Objectives: Cholinesterase inhibitors (ChEIs) are the mainstream treatment for delaying cognitive decline in Alzheimer's disease (AD). Low vitamin B12 is associated with cognitive dysfunction, and its supplementation has been applied as the treatment for certain types of reversible dementia. The present study hypothesized that baseline serum vitamin B12 is associated with the deterioration of cognitive function in people with AD undergoing ChEI treatment. Materials and methods: Between 2009 and 2016, medical records from 165 Taiwanese with mild to moderate AD who underwent ChEI treatment for at least 2 years were reviewed...
2018: Frontiers in Neurology
Manizheh Mostofi, Ghodsi Mohammadi Ziarani, Negar Lashgari
A series of bezofuran appended 1,5-benzothiazepine compounds 7a-v was designed, synthesized and evaluated as cholinesterase inhibitors. The biological assay experiments showed that most of the compounds displayed a clearly selective inhibition for butyrylcholinesterase (BChE), while a weak or no effect towards acetylcholinesterase (AChE) was detected. All analogs exhibited varied BChE inhibitory activity with IC50 value ranging between 1.0 ± 0.01 and 72 ± 2.8 μM when compared with the standard donepezil (IC50 , 2...
March 1, 2018: Bioorganic & Medicinal Chemistry
Sudhakar R Subramaniam, Iddo Magen, Nicholas Bove, Chunni Zhu, Vincent Lemesre, Garima Dutta, Chris Jean Elias, Henry A Lester, Marie-Francoise Chesselet
In addition to dopaminergic and motor deficits, patients with Parkinson's disease (PD) suffer from non-motor symptoms, including early cognitive and social impairment, that do not respond well to dopaminergic therapy. Cholinergic deficits may contribute to these problems, but cholinesterase inhibitors have limited efficacy. Mice over-expressing α-synuclein, a protein critically associated with PD, show deficits in cognitive and social interaction tests, as well as a decrease in cortical acetylcholine. We have evaluated the effects of chronic administration of nicotine in mice over-expressing wild type human α-synuclein under the Thy1-promoter (Thy1-aSyn mice)...
May 31, 2018: Neurobiology of Disease
Junyi Li, Di Rao, Robert B Gibbs
Cholinergic projections have been shown to interact with estrogens in ways that influence synaptic plasticity and cognitive performance. The mechanisms are not well understood. The goal of this study was to investigate whether cholinergic projections influence brain estrogen production by affecting aromatase (ARO), or influence estrogen signaling by affecting estrogen receptor expression. In the first experiment, ovariectomized rats received intraseptal injection of the selective immunotoxin 192IgG-saporin to destroy cholinergic inputs to the hippocampus...
May 28, 2018: Neuroscience
Ahmet Turan Isik, Pinar Soysal, Brendon Stubbs, Marco Solmi, Cristina Basso, Stefania Maggi, Patricia Schofield, Nicola Veronese, Christoph Mueller
OBJECTIVES: To evaluate the cardiovascular (CV) effects of acetylcholinesterase inhibitors (AChEIs) in individuals with dementia DESIGN: Systematic review and meta-analysis. SETTING: Two authors independently searched major electronic databases from inception until June 17, 2017, for longitudinal (without a control group) and cohort (with a control group) studies reporting CV outcomes in relation to AChEIs. Randomized controlled trials were excluded because they included relatively healthy subjects...
May 30, 2018: Journal of the American Geriatrics Society
Harald Hampel, M-Marsel Mesulam, A Claudio Cuello, Martin R Farlow, Ezio Giacobini, George T Grossberg, Ara S Khachaturian, Andrea Vergallo, Enrica Cavedo, Peter J Snyder, Zaven S Khachaturian
Cholinergic synapses are ubiquitous in the human central nervous system. Their high density in the thalamus, striatum, limbic system, and neocortex suggest that cholinergic transmission is likely to be critically important for memory, learning, attention and other higher brain functions. Several lines of research suggest additional roles for cholinergic systems in overall brain homeostasis and plasticity. As such, the brain's cholinergic system occupies a central role in ongoing research related to normal cognition and age-related cognitive decline, including dementias such as Alzheimer's disease...
May 29, 2018: Brain: a Journal of Neurology
Adam Kostelnik, Miroslav Pohanka
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are two enzymes sensitive to various chemical compounds having ability to bind to crucial parts of these enzymes. Boldine is a natural alkaloid and it was mentioned in some older works that it can inhibit some kinds of AChE. We reinvestigated this effect on AChE and also on BChE using acetyl (butyryl) thiocholine and Ellman's reagents as standard substances for spectrophotometric assay. We found out IC50 of AChE equal to 372  μ mol/l and a similar level to BChE, 321  μ mol/l...
2018: BioMed Research International
Deguo Wang, Yong Wu, Ancai Wang, Yueyun Chen, Ting Zhang, Nengwei Hu
Objective: Donepezil, a widely used cholinesterase inhibitor for treating Alzheimer's disease, has been reported to induce bradyarrhythmias and torsade de pointes. In this study, we aimed at determining electrocardiogram changes of donepezil administration in elderly patients with ischemic heart disease, who tend to suffer from cognitive disorders. Methods: Sixty patients with ischemic heart disease and mild cognitive impairment were treated with donepezil (5 mg/day) and followed up for at least four weeks...
2018: Cardiology Research and Practice
Lukáš Matějovský, Vladimír Pitschmann
Cholinesterase inhibitors are widely used as pesticides in agriculture, but also form a group of organophosphates known as nerve chemical warfare agents. This calls for close attention regarding their detection, including the use of various biosensors. One such biosensor made in the Czech Republic is the Detehit, which is based on a cholinesterase reaction that is assessed using a colour indicator-the Ellman's reagent-which is anchored on cellulose filter paper together with the substrate. With the use of this biosensor, detection is simple, quick, and sensitive...
May 30, 2018: Biosensors
Rita Khoury, Noam Grysman, Jake Gold, Kush Patel, George T Grossberg
Despite recent advances in Alzheimer's disease (AD) research, no breakthrough treatments have been discovered. Cholinesterase inhibitors and the NMDA-receptor antagonist memantine are currently the two approved symptomatic treatments for AD. 5HT-6 receptor antagonism has recently emerged as a promising treatment strategy to improve cognition in AD, with a modest side effect profile. Areas Covered: 5-HT6 receptors, exclusively found in the central nervous system, modulate primarily GABA and glutamate levels, facilitating the secondary release of other neurotransmitters including dopamine, noradrenaline and acetylcholine, all of which are compromised in AD...
May 31, 2018: Expert Opinion on Investigational Drugs
Makaía M Papasergi-Scott, Hannah M Stoveken, Lauren MacConnachie, Pui-Yee Chan, Meital Gabay, Dorothy Wong, Robert S Freeman, Asim A Beg, Gregory G Tall
Resistance to inhibitors of cholinesterase-8A (Ric-8A) and Ric-8B are essential biosynthetic chaperones for heterotrimeric G protein α subunits. We provide evidence for the direct regulation of Ric-8A cellular activity by dual phosphorylation. Using proteomics, Western blotting, and mutational analyses, we determined that Ric-8A was constitutively phosphorylated at five serines and threonines by the protein kinase CK2. Phosphorylation of Ser435 and Thr440 in rat Ric-8A (corresponding to Ser436 and Thr441 in human Ric-8A) was required for high-affinity binding to Gα subunits, efficient stimulation of Gα subunit guanine nucleotide exchange, and mediation of Gα subunit folding...
May 29, 2018: Science Signaling
Benjamin Baccus, Stéphane Auvin, Frédéric Dorandeu
Organophosphorus compounds (OP) are irreversible inhibitors of both central and peripheral cholinesterases (ChE). They still represent a major health issue in some countries as well as a terrorist and military threat. In order to design appropriate medical counter-measures, a better understanding of the pathophysiology of the poisoning is needed. Little to nothing is known regarding the impact of the genetic background on OP-induced seizures and seizure-related cell injury. Using two different mouse strains, Swiss and C57BL/6J, exposed to a convulsing dose of the OP pesticide paraoxon-ethyl (POX), our study focused on seizure susceptibility, especially the occurrence of SE and related mortality...
May 22, 2018: Chemico-biological Interactions
V А Sizonov, L E Dmitrieva
Parameters of cardiac activity after administration of the cholinesterase inhibitor physostigmine were analyzed in newborn rats and on day 16 of postnatal development. The type of cardiovascular response to acetylcholine excess in newborns and 16-day-old rats were similar, but they significantly differed by the magnitude, which suggests that that maturation of cholinergic structures involved in the regulation of cardiac activity is completed during the early postnatal ontogeny.
May 24, 2018: Bulletin of Experimental Biology and Medicine
María Julia Castro, Victoria Richmond, María Belén Faraoni, Ana Paula Murray
A set of triterpenoids with different grades of oxidation in the lupane skeleton were prepared and evaluated as cholinesterase inhibitors. Allylic oxidation with selenium oxide and Jones's oxidation were employed to obtain mono-, di- and tri-oxolupanes, starting from calenduladiol (1) and lupeol (3). All the derivatives showed a selective inhibition of butyrylcholinesterase over acetylcholinesterase (BChE vs. AChE). A kinetic study proved that compounds 2 and 9, the more potent inhibitors of the series, act as competitive inhibitors...
May 17, 2018: Bioorganic Chemistry
Burcu Kilic, Merve Erdogan, Hayrettin O Gulcan, Fatma Aksakal, Nihan Oruklu, E Umit Bagriacik, Deniz S Dogruer
Backround: With respect to the increase in the average life expectancy, Alzheimer Disease (AD), the most common form of age-related dementia, has become a major threat to the population over the age of 65 during the past several decades. The majority of AD treatments are focused on cholinergic and amyloid hypotheses. OBJECTIVE: In this study, three series of diphenyl-2-(2-(4-substitutedpiperazin-1-yl)ethyl)pyridazin-3(2H)-one derivatives were designed, synthesized and investigated for their ability to inhibit both cholinesterase enzymes and amyloid-β aggregation...
May 23, 2018: Medicinal Chemistry
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