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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/29143695/an-overview-of-systematic-reviews-of-pharmacological-and-non-pharmacological-interventions-for-the-treatment-of-behavioral-and-psychological-symptoms-of-dementia
#1
Suzanne M Dyer, Stephanie L Harrison, Kate Laver, Craig Whitehead, Maria Crotty
BACKGROUND: This systematic overview reports findings from systematic reviews of randomized controlled trials of pharmacological and non-pharmacological interventions for behavioural and psychological symptoms of dementia (BPSD). METHODS: The Cochrane Database of Systematic Reviews, DARE, Medline, EMBASE, and PsycINFO were searched to September 2015. RESULTS: Fifteen systematic reviews of eighteen different interventions were included. A significant improvement in BPSD was seen with: functional analysis-based interventions (GRADE quality of evidence moderate; standardized mean difference (SMD) -0...
November 16, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29142396/antioxidant-and-cholinesterase-inhibitory-activities-of-ethyl-acetate-extract-of-terminalia-chebula-cell-free-in-vitro-and-in-silico-studies
#2
Mohamed Asik Rajmohamed, Suganthy Natarajan, Premkumar Palanisamy, Akbarsha Mohammad Abdulkader, Archunan Govindaraju
Background: Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by memory loss and impaired cognitive function. Cholinergic enzyme deficiency and oxidative stress are the two major factors implicated in the pathogenesis of AD. The symptomatic treatment, as of now, is the use of cholinesterase inhibitors toward cholinergic "downturn." Therefore, there is a search for compounds that will be useful in focused therapies. There has been suggestion that Terminalia chebula fruit would be a potential source...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29135926/proline-based-carbamates-as-cholinesterase-inhibitors
#3
Hana Pizova, Marketa Havelkova, Sarka Stepankova, Andrzej Bak, Tereza Kauerova, Violetta Kozik, Michal Oravec, Ales Imramovsky, Peter Kollar, Pavel Bobal, Josef Jampilek
Series of twenty-five benzyl (2S)-2-(arylcarbamoyl)pyrrolidine-1-carboxylates was prepared and completely characterized. All the compounds were tested for their in vitro ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and the selectivity of compounds to individual cholinesterases was determined. Screening of the cytotoxicity of all the compounds was performed using a human monocytic leukaemia THP-1 cell line, and the compounds demonstrated insignificant toxicity. All the compounds showed rather moderate inhibitory effect against AChE; benzyl (2S)-2-[(2-chlorophenyl)carbamoyl]pyrrolidine-1-carboxylate (IC50 = 46...
November 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29127449/determining-a-threshold-sub-acute-dose-leading-to-minimal-physiological-alterations-following-prolonged-exposure-to-the-nerve-agent-vx-in-rats
#4
E Bloch-Shilderman, I Rabinovitz, I Egoz, G Yacov, N Allon, U Nili
VX, a potent inhibitor of cholinesterase (ChE), is considered as one of the most toxic, persistent and least volatile nerve agents. VX is absorbed in various environmental surfaces and is gradually released long after its initial dispersal. Its toxicity is mainly caused by disrupting central and peripheral cholinergic nervous system activity, leading to potential long-term detrimental effects on health. The primary objective of the present study was to assess the threshold VX dose leading to minimal physiological alterations following prolonged VX exposure...
November 10, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29126732/2-arylbenzofurans-from-artocarpus-lakoocha-and-methyl-ether-analogs-with-potent-cholinesterase-inhibitory-activity
#5
Umalee Namdaung, Anan Athipornchai, Thongchai Khammee, Mayuso Kuno, Sunit Suksamrarn
In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0...
October 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29125188/the-mouse-passive-transfer-model-of-musk-myasthenia-gravis-disrupted-musk-signaling-causes-synapse-failure
#6
REVIEW
Nazanin Ghazanfari, Sofie Trajanovska, Marco Morsch, Simon X Liang, Stephen W Reddel, William D Phillips
While the majority of myasthenia gravis patients express antibodies targeting the acetylcholine receptor, the second most common cohort instead displays autoantibodies against muscle-specific kinase (MuSK). MuSK is a transmembrane tyrosine kinase found in the postsynaptic membrane of the neuromuscular junction. During development, MuSK serves as a signaling hub, coordinating the alignment of the pre- and postsynaptic components of the synapse. Adult mice that received repeated daily injections of IgG from anti-MuSK(+) myasthenia gravis patients developed muscle weakness, associated with neuromuscular transmission failure...
November 10, 2017: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/29116600/recent-progress-in-the-pharmacotherapy-of-alzheimer-s-disease
#7
Rita Khoury, Kush Patel, Jake Gold, Stephanie Hinds, George T Grossberg
Alzheimer's disease is the most common major neurocognitive disorder with substantial social and economic impacts. This article is an update on current pharmacotherapy, advancements in biomarker use, and drugs in the pipeline for this disease. To date, no new drug has qualified to be added to the current therapeutic arsenal comprising cholinesterase inhibitors and the NMDA receptor antagonist memantine. Drugs in the pipeline include symptomatic therapies that are neurotransmitter-based, but mostly disease-modifying therapies...
November 7, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/29109645/neostigmine-induced-coronary-artery-spasm-a-case-report-and-literature-review
#8
Shimon Kolker, Dan Tzivoni, David Rosenmann, Shmuel Meyler, Alexander Ioscovich
Neostigmine is a cholinesterase inhibitor which does not cross the blood brain barrier and a commonly used for reversal of nondepolarizing muscle relaxants. In the following case report, we present a patient who developed coronary artery spasm, after the administration of repeated doses of neostigmine. Ours is the first case to demonstrate such a longstanding coronary artery vasospasm that lasted several hours in response to neostigmine, resulting in myocardial damage and left ventricular dysfunction. We would like to draw the attention of the anesthesiologists to this rare effect that may lead to perioperative cardiac complications...
July 2017: Journal of Anaesthesiology, Clinical Pharmacology
https://www.readbyqxmd.com/read/29102759/preclinical-profile-of-a-dopamine-d1-potentiator-suggests-therapeutic-utility-in-neurological-and-psychiatric-disorders
#9
Robert F Bruns, Stephen N Mitchell, Keith A Wafford, Alex J Harper, Elaine A Shanks, Guy Carter, Michael J O'Neill, Tracey K Murray, Brian J Eastwood, John M Schaus, James P Beck, Junliang Hao, Jeffrey M Witkin, Xia Li, Eyassu Chernet, Jason S Katner, Hong Wang, John W Ryder, Meghane E Masquelin, Linda K Thompson, Patrick L Love, Deanna L Maren, Julie F Falcone, Michelle M Menezes, Linli Zhang, Charles R Yang, Kjell A Svensson
DETQ, an allosteric potentiator of the dopamine D1 receptor, was tested in therapeutic models that were known to respond to D1 agonists. Because of a species difference in affinity for DETQ, all rodent experiments used transgenic mice expressing the human D1 receptor (hD1 mice). When given alone, DETQ reversed the locomotor depression caused by a low dose of reserpine. DETQ also acted synergistically with L-DOPA to reverse the strong hypokinesia seen with a higher dose of reserpine. These results indicate potential as both monotherapy and adjunct treatment in Parkinson's disease...
October 26, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29098902/design-synthesis-and-pharmacological-evaluation-of-2-amino-5-nitrothiazole-derived-semicarbazones-as-dual-inhibitors-of-monoamine-oxidase-and-cholinesterase-effect-of-the-size-of-aryl-binding-site
#10
Rati K P Tripathi, Vishnu M Sasi, Sukesh K Gupta, Sairam Krishnamurthy, Senthil R Ayyannan
A series of 2-amino-5-nitrothiazole derived semicarbazones were designed, synthesised and investigated for MAO and ChE inhibition properties. Most of the compounds showed preferential inhibition towards MAO-B. Compound 4, (1-(1-(4-Bromophenyl)ethylidene)-4-(5-nitrothiazol-2-yl)semicarbazide) emerged as lead candidate (IC50 = 0.212 µM, SI = 331.04) against MAO-B; whereas compounds 21 1-(5-Bromo-2-oxoindolin-3-ylidene)-4-(5-nitrothiazol-2-yl)semicarbazide (IC50 = 0.264 µM) and 17 1-((4-Chlorophenyl) (phenyl)methylene)-4-(5-nitrothiazol-2-yl)semicarbazide (IC50 = 0...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29093288/synthesis-of-amide-and-ester-derivatives-of-cinnamic-acid-and-its-analogs-evaluation-of-their-free-radical-scavenging-and-monoamine-oxidase-and-cholinesterase-inhibitory-activities
#11
Koichi Takao, Kazuhiro Toda, Takayuki Saito, Yoshiaki Sugita
A series of cinnamic acid derivatives, amides (1-12) and esters (13-22), were synthesized, and structure-activity relationships for antioxidant activity, and monoamine oxidases (MAO) A and B, acetylcholinesterase, and butyrylcholinesterase (BChE) inhibitory activities were analyzed. Among the synthesized compounds, compounds 1-10, 12-18, and rosmarinic acid (23), which contained catechol, o-methoxyphenol or 5-hydroxyindole moieties, showed potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29081417/change-in-odor-identification-impairment-is-associated-with-improvement-with%C3%A2-cholinesterase-inhibitor-treatment-in%C3%A2-mild-cognitive-impairment
#12
D P Devanand, Cody Lentz, Richard E Chunga, Adam Ciarleglio, Jennifer M Scodes, Howard Andrews, Peter W Schofield, Yaakov Stern, Edward D Huey, Karen Bell, Gregory H Pelton
BACKGROUND: Anticholinergic challenge can induce odor identification impairment that indicates Alzheimer's disease pathology. OBJECTIVE: To determine if decline in odor identification ability with anticholinergic challenge can predict improvement with donepezil, a cholinesterase inhibitor (ChEI), in patients with mild cognitive impairment (MCI). METHODS: At baseline, the University of Pennsylvania Smell identification Test (UPSIT) was administered before and after an anticholinergic atropine nasal spray challenge...
October 21, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/29069924/phytol-loaded-plga-nanoparticle-as-a-modulator-of-alzheimer-s-toxic-a%C3%AE-peptide-aggregation-and-fibrillation-associated-with-impaired-neuronal-cell-function
#13
Sethuraman Sathya, Balakrishnan Shanmuganathan, Shanmugasundram Saranya, Sethuraman Vaidevi, Kandasamy Ruckmani, Kasi Pandima Devi
Alzheimer's disease (AD) is an unfavourable neurological condition of the brain leading to the loss of behavioural and cognitive skills of the aging population. At present, drugs representing cholinesterase inhibitors provide lateral side effects to AD patients. Hence, there is a need for improved fabrication of drugs without side effects, for which nanoencapsulated bioactive compounds that can cross the blood-brain barrier offer new hope as novel alternative treatment strategy for AD. This study involved synthesis of phytol loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles by solvent evaporation method...
October 25, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29067315/tolerability-of-orm-12741-and-effects-on-episodic-memory-in-patients-with-alzheimer-s-disease
#14
Juha O Rinne, Keith Wesnes, Jeffrey L Cummings, Pasi Hakulinen, Merja Hallikainen, Jutta Hänninen, Michael Murphy, Henry Riordan, Mika Scheinin, Hilkka Soininen, Juha Rouru
INTRODUCTION: ORM-12741 is a novel selective antagonist of alpha-2C adrenoceptors. This trial evaluated the safety and efficacy of ORM-12741 in patients with Alzheimer's disease (AD). METHODS: A randomized, double-blind, placebo-controlled, exploratory phase 2a trial was conducted in 100 subjects with AD and neuropsychiatric symptoms. Participants were randomized to receive one of two flexible doses of ORM-12741 (30-60 mg or 100-200 mg) or placebo b.i.d. for 12 weeks in addition to standard therapy with cholinesterase inhibitors...
January 2017: Alzheimer's & Dementia: Translational Research & Clinical Interventions
https://www.readbyqxmd.com/read/29066367/brain-metabolic-correlates-of-csf-tau-protein-in-a-large-cohort-of-alzheimer-s-disease-patients-a-csf-and-fdg-pet-study
#15
Agostino Chiaravalloti, Gaetano Barbagallo, Maria Ricci, Alessandro Martorana, Francesco Ursini, Pasqualina Sannino, Georgios Karalis, Orazio Schillaci
AIMS: physiopathological mechanisms of Alzheimer's disease (AD) are still matter of debate. Especially the role of amyloid β and tau pathology in the development of the disease are still matter of debate. Changes in tau and amyloid β peptide concentration in cerebrospinal fluid (CSF) and hypometabolic patterns at fluorine-18 fluorodeoxyglucose ((18)F-FDG) PET scanning are considered as biomarkers of AD. The present study was aimed to evaluate the relationships between the concentrations of CSF total Tau (t-Tau), phosphorilated Tau (p-Tau) and Aβ1-42 amyloid peptide with (18)F-FDG brain distribution in a group of patients with AD...
October 21, 2017: Brain Research
https://www.readbyqxmd.com/read/29059136/successful-use-of-escitalopram-for-the-treatment-of-visual-hallucinations-in-patients-with-parkinson-disease
#16
Joseph Bergman, Paul P Lerner, Shmuel Sokolik, Vladimir Lerner, Anatoly Kreinin, Chanoch Miodownik
INTRODUCTION: Patients with Parkinson disease (PD) frequently experience visual hallucinations (VH). Visual hallucinations are most often viewed as an adverse effect of antiparkinsonian treatment. Possible treatments for this disturbance include a reduction of antiparkinsonian medications, adding atypical antipsychotics, or cholinesterase inhibitors. Some studies demonstrated that selective serotonin reuptake inhibitors may be an optional treatment for patients experiencing psychosis or agitation in dementia...
November 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/29056913/anti-alzheimer-s-studies-on-%C3%AE-sitosterol-isolated-from-polygonum-hydropiper-l
#17
Muhammad Ayaz, Muhammad Junaid, Farhat Ullah, Fazal Subhan, Abdul Sadiq, Gowhar Ali, Muhammad Ovais, Muhammad Shahid, Ashfaq Ahmad, Abdul Wadood, Mohamed El-Shazly, Nisar Ahmad, Sajjad Ahmad
The family Polygonaceae is known for its traditional use in the management of various neurological disorders including Alzheimer's disease (AD). In search of new anti-AD drugs, β-sitosterol isolated from Polygonum hydropiper was subjected to in vitro, in vivo, behavioral and molecular docking studies to confirm its possibility as a potential anti-Alzheimer's agent. The in vitro AChE, BChE inhibitory potentials of β-sitosterol were investigated following Ellman's assay. The antioxidant activity was tested using DPPH, ABTS and H2O2 assays...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29044771/alkaloids-of-amaryllidaceae-as-inhibitors-of-cholinesterases-aches-and-bches-an-integrated-bioguided-study
#18
Natalie Cortes, Karina Sierra, Fernando Alzate, Edison H Osorio, Edison Osorio
INTRODUCTION: Enzymatic inhibition of acetylcholinesterase (AChE) is an essential therapeutic target for the treatment of Alzheimer's disease (AD) and AChE inhibitors are the first-line drugs for it treatment. However, butyrylcholinesterase (BChE), contributes critically to cholinergic dysfunction associated with AD. Thus, the development of novel therapeutics may involve the inhibition of both cholinesterase enzymes. OBJECTIVE: To evaluate, in an integrated bioguided study, cholinesterases alkaloidal inhibitors of Amaryllidaceae species...
October 17, 2017: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/29034839/pharmacogenetics-of-angiotensin-converting-enzyme-inhibitors-in-patients-with-alzheimer-s-disease-dementia
#19
Fabricio Ferreira de Oliveira, Elizabeth Suchi Chen, Marilia Cardoso Smith, Paulo Henrique Ferreira Bertolucci
BACKGROUND: While the angiotensin-converting enzyme degrades amyloid-β, angiotensin-converting enzyme inhibitors (ACEis) may slow cognitive decline by way of cholinergic effects, by increasing brain substance P and boosting the activity of neprilysin, and by modulating glucose homeostasis and augmenting the secretion of adipokines to enhance insulin sensitivity in patients with Alzheimer's disease dementia (AD). We aimed to investigate whether ACE gene polymorphisms rs1800764 and rs4291 are associated with cognitive and functional change in patients with AD, while also taking APOE haplotypes and anti-hypertensive treatment with ACEis into account for stratification...
October 16, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29033232/design-synthesis-and-biological-evaluation-of-phthalimide-alkylamine-derivatives-as-balanced-multifunctional-cholinesterase-and-monoamine-oxidase-b-inhibitors-for-the-treatment-of-alzheimer-s-disease
#20
Zhipei Sang, Keren Wang, Huifang Wang, Lintao Yu, Huijuan Wang, Qianwen Ma, Mengyao Ye, Xue Han, Wenmin Liu
A series of novel phthalimide-alkylamine derivatives were synthesized and evaluated as multi-functions inhibitors for the treatment of Alzheimer's disease (AD). The results showed that compound TM-9 could be regarded as a balanced multi-targets active molecule. It exhibited potent and balanced inhibitory activities against ChE and MAO-B (huAChE, huBuChE, and huMAO-B with IC50 values of 1.2μM, 3.8μM and 2.6 μM, respectively) with low selectivity. Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-9 binds simultaneously to the catalytic active site and peripheral anionic site of AChE...
November 15, 2017: Bioorganic & Medicinal Chemistry Letters
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