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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/28820005/inhibition-of-endocannabinoid-metabolizing-enzymes-in-peripheral-tissues-following-developmental-chlorpyrifos-exposure-in-rats
#1
Robert W Buntyn, Navatha Alugubelly, Rachel L Hybart, Afzaal N Mohammed, Carole A Nail, Greta C Parker, Matthew K Ross, Russell L Carr
Repeated developmental exposure to the organophosphate (OP) insecticide chlorpyrifos (CPF) inhibits brain fatty acid amide hydrolase (FAAH) activity at low levels, whereas at higher levels, it inhibits brain monoacylglycerol lipase (MAGL) activity. FAAH and MAGL hydrolyze the endocannabinoids anandamide (AEA) and 2-arachidonylglycerol (2-AG), respectively. Peripherally, AEA and 2-AG have physiological roles in the regulation of lipid metabolism and immune function, and altering the normal levels of these lipid mediators can negatively affect these processes...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28801274/mannich-base-approach-to-5-methoxyisatin-3-4-isopropylphenyl-hydrazone-a-water-soluble-prodrug-for-a-multitarget-inhibition-of-cholinesterases-beta-amyloid-fibrillization-and-oligomer-induced-cytotoxicity
#2
Leonardo Pisani, Annalisa De Palma, Nicola Giangregorio, Daniela V Miniero, Paolo Pesce, Orazio Nicolotti, Francesco Campagna, Cosimo D Altomare, Marco Catto
Targeting protein aggregation for the therapy of neurodegenerative diseases remains elusive for medicinal chemists, despite a number of small molecules known to interfere in amyloidogenesis, particularly of amyloid beta (Aβ) protein. Starting from previous findings in the antiaggregating activity of a class of indolin-2-ones inhibiting Aβ fibrillization, 5-methoxyisatin 3-(4-isopropylphenyl)hydrazone 1 was identified as a multitarget inhibitor of Aβ aggregation and cholinesterases with IC50s in the low μM range...
August 8, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28790827/the-effects-of-memantine-on-behavioral-disturbances-in-patients-with-alzheimer-s-disease-a-meta-analysis
#3
Taro Kishi, Shinji Matsunaga, Nakao Iwata
BACKGROUND: Memantine is effective in the treatment of behavioral disturbances in patients with Alzheimer's disease. It has not yet been fully determined which behavioral disturbances respond best to memantine. METHODS: We conducted a meta-analysis of memantine vs control (placebo or usual care) for the treatment of individual behavioral disturbances (delusion, hallucination, agitation/aggression, dysphoria, anxiety/phobia, euphoria, apathy, disinhibition, irritability/lability, aberrant motor activity/activity disturbances, nighttime disturbance/diurnal rhythm disturbances, and eating disturbances)...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28782481/rational-approaches-design-strategies-structure-activity-relationship-and-mechanistic-insights-for-esterase-inhibitors
#4
Harbinder Singh, Jatinder Vir Singh, Navdeep Kaur, Mohit Sanduja, Gurpreet Singh, Preet Mohinder Singh Bedi, Sahil Sharma
BACKGROUND: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of esterases are present in human body to control diverse set of cellular processes and execute their specific functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe pathological conditions like Alzheimer disease, hypercholesterolemia etc. OBJECTIVE: Numerous esterase inhibitors have been developed and reported by the researchers around the globe, but not systematically summarized yet...
August 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28770024/metformin-and-its-sulfenamide-prodrugs-inhibit-human-cholinesterase-activity
#5
Magdalena Markowicz-Piasecka, Joanna Sikora, Łukasz Mateusiak, Elżbieta Mikiciuk-Olasik, Kristiina M Huttunen
The results of epidemiological and pathophysiological studies suggest that type 2 diabetes mellitus (T2DM) may predispose to Alzheimer's disease (AD). The two conditions present similar glucose levels, insulin resistance, and biochemical etiologies such as inflammation and oxidative stress. The diabetic state also contributes to increased acetylcholinesterase (AChE) activity, which is one of the factors leading to neurodegeneration in AD. The aim of this study was to assess in vitro the effects of metformin, phenformin, and metformin sulfenamide prodrugs on the activity of human AChE and butyrylcholinesterase (BuChE) and establish the type of inhibition...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28760642/galantamine-administration-reduces-reactive-astrogliosis-and-upregulates-the-anti-oxidant-enzyme-catalase-in-rats-submitted-to-neonatal-hypoxia-ischemia
#6
F K Odorcyk, F Nicola, L E Duran-Carabali, F Figueiró, J Kolling, A Vizuete, E L Konrath, C A Gonçalves, A T S Wyse, C A Netto
Neonatal hypoxia ischemia (HI) plays a role in the etiology of several neurological pathologies and causes severe sequelae. Acetylcholine is a neurotransmitter in the central nervous system and cholinesterase inhibitors have demonstrated a positive action over HI induced deficits. In order to evaluate the effects of pre and post-hypoxia administrations of galantamine, a cholinesterase inhibitor, in a model of perinatal HI, Wistar rats in the post-natal day 7 (PND7) were subjected to a combination of unilateral occlusion of the right carotid artery with the exposure to a 1h hypoxia...
July 29, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28756012/design-synthesis-and-pharmacological-evaluation-of-a-novel-series-of-hormone-sensitive-lipase-inhibitor
#7
Tomoko Ogiyama, Mitsuhiro Yamaguchi, Nobuya Kurikawa, Shoko Honzumi, Koji Terayama, Nobumi Nagaoka, Yuka Yamamoto, Takako Kimura, Daisuke Sugiyama, Shin-Ichi Inoue
HSL inhibition is a promising approach to the treatment of dyslipidemia. As a result of re-optimization of lead compound 2, we identified novel compound 25a exhibiting potent inhibitory activity against HSL enzyme and cell with high selectivity for cholinesterases (AChE and BuChE). Reflecting its potent in vitro activity, compound 25a exhibited antilipolytic effect in rats at 1mg/kg p.o., which indicated that this novel compound is the most potent orally active HSL inhibitor. Moreover, compound 25a did not show bioactivation liability...
July 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28752503/trends-in-drug-prescription-rates-for-dementia-an-observational-population-based-study-in-france-2006-2014
#8
Mathilde François, Jonathan Sicsic, Alexis Elbaz, Nathalie Pelletier Fleury
BACKGROUND: Since the 2011 French guidance updates, cholinesterase inhibitors and memantine are considered optional in the management of dementia and leave physicians free to prescribe based on their clinical expertise. OBJECTIVES: The aims of this study were to analyze the influence of these recent guidance updates on the prescription rates of these drugs and to quantify the impact of potential changes on healthcare expenditures. METHODS: Patients over 65 years old from a representative sample of a national administrative claims database, the French national health insurance database, were retrospectively included from 2006 to 2014...
July 27, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28751142/design-synthesis-and-biological-evaluation-of-dual-acetylcholinesterase-and-phosphodiesterase-5a-inhibitors-in-treatment-for-alzheimer-s-disease
#9
Li-Yun Zhou, Yao Zhu, Yu-Ren Jiang, Xiong-Jie Zhao, Dong Guo
With the recent research advances in molecular biology and technology, multiple credible hypotheses about the progress of Alzheimer's disease (AD) have been proposed; multi-target drugs have emerged as an innovative therapeutic approach for AD. Current clinical therapy for AD patients is mainly palliative treatment targeting acetylcholinesterase (AChE). Inhibition of phosphodiesterase 5A (PDE5A) has recently been validated as a potentially novel therapeutic approach for Alzheimer's disease (AD). In this work, series of new compounds were designed, synthesized and evaluated as dual cholinesterase and PDE5A inhibitor...
July 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28749013/physiological-versus-pharmacological-signalling-to-myosin-phosphorylation-in-airway-smooth-muscle
#10
Ning Gao, Ming-Ho Tsai, Audrey N Chang, Weiqi He, Cai-Ping Chen, Minsheng Zhu, Kristine E Kamm, James T Stull
Ca(2+) /calmodulin activation of myosin light chain kinase (MLCK) initiates myosin regulatory light chain (RLC) phosphorylation for smooth muscle contraction with subsequent dephosphorylation for relaxation by myosin light chain phosphatase (MLCP) containing regulatory (MYPT1) and catalytic (PP1cδ) subunits. RLC phosphorylation-dependent force development is regulated by distinct signalling modules involving protein phosphorylations. We investigated responses to cholinergic agonist treatment versus neurostimulation by electric field stimulation (EFS) in bovine tracheal smooth muscle...
July 27, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28741230/new-therapeutic-strategies-for-lewy-body-dementias
#11
REVIEW
Latha Velayudhan, Dominic Ffytche, Clive Ballard, Dag Aarsland
This article reviews current treatment strategies and recent advances for the Lewy body dementias (LBDs). Current available symptom treatment strategies are based on monoaminergic, cholinergic and glutaminergic neurotransmitter systems. Relatively robust evidence exists for cholinesterase inhibitors for cognitive impairment in LBD and in Parkinson's disease for antidepressants, clozapine and recently pimavanserin for psychosis. interpidine (RVT 101) and nelotanserin are currently under investigation. Non-pharmacological interventions, such as cognitive stimulation, physical exercises and neuromodulation strategies, may be useful in Parkinson's disease but have not yet been tested in dementias...
September 2017: Current Neurology and Neuroscience Reports
https://www.readbyqxmd.com/read/28740390/brain-regions-associated-with-anosognosia-for-memory-disturbance-in-alzheimer-s-disease-a-magnetic-resonance-imaging-study
#12
Hiroshi Fujimoto, Teruyuki Matsuoka, Yuka Kato, Keisuke Shibata, Kaeko Nakamura, Kei Yamada, Jin Narumoto
BACKGROUND AND OBJECTIVE: Patients with Alzheimer's disease (AD) are frequently unaware of their cognitive symptoms and medical diagnosis. The term "anosognosia" is used to indicate a general lack of awareness of one's disease or disorder. The neural substrate underlying anosognosia in AD is unclear. Since anosognosia for memory disturbance might be an initial sign of AD, it is important to determine the neural correlates. This study was designed to investigate the characteristics and neural correlates of anosognosia for memory disturbance in patients with mild AD...
2017: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/28737687/new-cinchona-oximes-evaluated-as-reactivators-of-acetylcholinesterase-and-butyrylcholinesterase-inhibited-by-organophosphorus-compounds
#13
Maja Katalinić, Antonio Zandona, Alma Ramić, Tamara Zorbaz, Ines Primožič, Zrinka Kovarik
For the last six decades, researchers have been focused on finding efficient reactivators of organophosphorus compound (OP)-inhibited acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). In this study, we have focused our research on a new oxime scaffold based on the Cinchona structure since it was proven to fit the cholinesterases active site and reversibly inhibit their activity. Three Cinchona oximes (C1, C2, and C3), derivatives of the 9-oxocinchonidine, were synthesized and investigated in reactivation of various OP-inhibited AChE and BChE...
July 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28733759/management-of-gait-changes-and-fall-risk-in-mci-and-dementia
#14
REVIEW
Gilles Allali, Joe Verghese
Gait disorders and falls are very prevalent in aging, especially in older adults with cognitive impairment: older adults with dementia are 2-3 times more likely to fall than their non-demented counterparts. The management of gait disorders and falls in older adults with mild cognitive impairment (MCI) or dementia begins by their identification with the use of specific screening tools, such as measuring gait speed, use of dual-task gait tests, or diagnosing motoric cognitive risk syndrome, a newly described pre-dementia syndrome...
September 2017: Current Treatment Options in Neurology
https://www.readbyqxmd.com/read/28715142/cholinesterase-inhibition-reduces-arrhythmias-in-asymptomatic-chagas-disease
#15
Renata Rodrigues Teixeira de Castro, Graciema Porphirio, Sergio Salles Xavier, Ruy Silveira Moraes, Elton Luis Ferlin, Jorge Pinto Ribeiro, Antonio Claudio Lucas da Nóbrega
INTRODUCTION: Parasympathetic dysfunction may play a role in the genesis of arrhythmias in Chagas disease. AIM: This study evaluates the acute effects of pyridostigmine (PYR), a reversible cholinesterase inhibitor, on the occurrence of arrhythmias in patients with Chagas cardiac disease. METHOD: Following a double-blind, randomized, placebo-controlled, cross-over protocol, 17 patients (age 50±2 years) with Chagas cardiac disease type B underwent 24-hour Holter recordings after oral administration of either pyridostigmine bromide (45 mg, 3 times/day) or placebo (PLA)...
July 17, 2017: Cardiovascular Therapeutics
https://www.readbyqxmd.com/read/28714881/assessment-of-enzyme-inhibition-a-review-with-examples-from-the-development-of-monoamine-oxidase-and-cholinesterase-inhibitory-drugs
#16
REVIEW
Rona R Ramsay, Keith F Tipton
The actions of many drugs involve enzyme inhibition. This is exemplified by the inhibitors of monoamine oxidases (MAO) and the cholinsterases (ChE) that have been used for several pharmacological purposes. This review describes key principles and approaches for the reliable determination of enzyme activities and inhibition as well as some of the methods that are in current use for such studies with these two enzymes. Their applicability and potential pitfalls arising from their inappropriate use are discussed...
July 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28714400/cholinesterase-inhibitory-activity-of-some-semi-rigid-spiro-heterocycles-pom-analyses-and-crystalline-structure-of-pharmacophore-site
#17
Taibi Ben Hadda, Oualid Talhi, Artur S M Silva, Fatma Sezer Senol, Ilkay Erdogan Orhan, Abdur Rauf, Yahia N Mabkhot, Khaldoun Bachari, Ismail Warad, Thoraya A Farghaly, Ismail I Althagafi, Mohammad S Mubarak
Cholinesterase family consists of two sister enzymes; acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which hydrolyze acetylcholine. Since deficit of acetylcholine has been evidenced in the patients of Alzheimer's disease (AD), cholinesterase inhibitors are currently the most prescribed drug class for the treatment of AD. In the present study, five compounds (2-6) with spiro skeleton have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 25 mg/mL...
July 13, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28711758/assessing-the-binding-of-cholinesterase-inhibitors-by-docking-and-molecular-dynamics-studies
#18
M Rejwan Ali, Mostafa Sadoqi, Simon G Møller, Allal Boutajangout, Mihaly Mezei
In this report we assessed by docking and molecular dynamics the binding mechanisms of three FDA-approved Alzheimer drugs, inhibitors of the enzyme acetylcholinesterase (AChE): donepezil, galantamine and rivastigmine. Dockings by the softwares Autodock-Vina, PatchDock and Plant reproduced the docked conformations of the inhibitor-enzyme complexes within 2Å of RMSD of the X-ray structure. Free-energy scores show strong affinity of the inhibitors for the enzyme binding pocket. Three independent Molecular Dynamics simulation runs indicated general stability of donepezil, galantamine and rivastigmine in their respective enzyme binding pocket (also referred to as gorge) as well as the tendency to form hydrogen bonds with the water molecules...
June 29, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28699213/acetamide-derivatives-of-chromen-2-ones-as-potent-cholinesterase-inhibitors
#19
Suchita Prasad, Bipul Kumar, Shiv Kumar, Karam Chand, Shashank S Kamble, Hemant K Gautam, Sunil K Sharma
Alzheimer's disease (AD), a neurodegenerative disorder, is a serious medical issue worldwide with drastic social consequences. Inhibition of cholinesterase is one of the rational and effective approaches to retard the symptoms of AD and, hence, consistent efforts are being made to develop efficient anti-cholinesterase agents. In pursuit of this, a series of 19 acetamide derivatives of chromen-2-ones were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potential...
July 12, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28698023/inhibitory-effects-of-serratene-type-triterpenoids-from-lycopodium-complanatum-on-cholinesterases-and-%C3%AE-secretase-1
#20
Van Thu Nguyen, Bing Tian Zhao, Su Hui Seong, Jeong Ah Kim, Mi Hee Woo, Jae Sui Choi, Byung Sun Min
Phytochemical investigation of Lycopodium complanatum whole plants led to the isolation of two new serratene-type triterpenoids (1 and 2) along with eight known triterpenoids (3-10). Their structures were established using 1D and 2D NMR spectroscopic techniques and mass spectrometry. These compounds did not inhibit acetylcholinesterases (AChE) and butyrylcholinesterase (BChE), but did inhibit β-secretase 1 (BACE1). Compounds 1 and 6 showed potent BACE1 inhibition with IC50 values of 2.79 ± 0.28 and 2.49 ± 0...
July 8, 2017: Chemico-biological Interactions
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