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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/28631100/co-modulation-of-an-allosteric-modulator-of-nicotinic-receptor-cholinesterase-inhibitor-galantamine-and-a-5-ht4-receptor-agonist-rs-67333-effect-on-scopolamine-induced-memory-deficit-in-the-mouse
#1
Thomas Freret, Véronique Lelong-Boulouard, Pierre Lecouflet, Katia Hamidouche, François Dauphin, Michel Boulouard
AIM: It is widely assumed that the upcoming therapeutics for Alzheimer's disease will require to act on more than one target to be effective. We investigated here whether a combination of the nicotinic receptor allosteric modulator/cholinesterase inhibitor galantamine can act synergistically with the type 4 serotonin receptor (5-HT4R) partial agonist, RS-67333, to counterbalance deficits in short- and long-term memory. To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task...
June 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28629119/cholinesterase-inhibitory-activities-of-adamantyl-based-derivatives-and-their-molecular-docking-studies
#2
Huey Chong Kwong, Siau Hui Mah, Tze Shyang Chia, Ching Kheng Quah, Gin Keat Lim, C S Chidan Kumar
Adamantyl-based compounds are clinically important for the treatments of type 2 diabetes and for their antiviral abilities, while many more are under development for other pharmaceutical uses. This study focused on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of adamantyl-based ester derivatives with various substituents on the phenyl ring using Ellman's colorimetric method. Compound 2e with a 2,4-dichloro electron-withdrawing substituent on the phenyl ring exhibited the strongest inhibition effect against AChE, with an IC50 value of 77...
June 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28626471/early-versus-late-onset-alzheimer-disease-long-term-functional-outcomes-nursing-home-placement-and-risk-factors-for-rate-of-progression
#3
Carina Wattmo, Åsa K Wallin
BACKGROUND/AIMS: Whether age at onset influences functional deterioration in Alzheimer disease (AD) is unclear. We, therefore, investigated risk factors for progression in activities of daily living (ADL) and nursing home placement (NHP) in cholinesterase inhibitor (ChEI)-treated patients with early-onset AD (EOAD) versus late-onset AD (LOAD). METHODS: This 3-year, prospective, observational, multicenter study included 1,017 participants with mild-to-moderate AD; 143 had EOAD (onset <65 years) and 874 LOAD (onset ≥65 years)...
January 2017: Dementia and Geriatric Cognitive Disorders Extra
https://www.readbyqxmd.com/read/28606768/genetic-analysis-of-the-ric3-gene-in-han-chinese-patients-with-parkinson-s-disease
#4
Dan He, Pengzhi Hu, Xiong Deng, Zhi Song, Lamei Yuan, Xiuhong Yuan, Hao Deng
Parkinson's disease (PD) is the second-most common etiologically complex neurodegenerative disease. Genetic abnormalities are thought to play an important role in the development of PD. Recently, mutations in the resistance to inhibitors of cholinesterase 3 gene (RIC3) have been reported to cause autosomal-dominant PD in Indian population. To determine whether RIC3 gene coding variant(s) are associated with PD in Han Chinese population, the RIC3 gene coding region in 218 mainland Han Chinese patients with PD and the identified variants in 242 normal controls were examined using direct sequencing analysis...
June 9, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28603772/compensatory-shifts-in-visual-perception-are-associated-with-hallucinations-in-lewy-body-disorders
#5
Alan Robert Bowman, Vicki Bruce, Christopher J Colbourn, Daniel Collerton
Visual hallucinations are a common, distressing, and disabling symptom of Lewy body and other diseases. Current models suggest that interactions in internal cognitive processes generate hallucinations. However, these neglect external factors. Pareidolic illusions are an experimental analogue of hallucinations. They are easily induced in Lewy body disease, have similar content to spontaneous hallucinations, and respond to cholinesterase inhibitors in the same way. We used a primed pareidolia task with hallucinating participants with Lewy body disorders (n = 16), non-hallucinating participants with Lewy body disorders (n = 19), and healthy controls (n = 20)...
2017: Cognitive Research: Principles and Implications
https://www.readbyqxmd.com/read/28589255/potential-anti-cholinesterase-and-%C3%AE-site-amyloid-precursor-protein-cleaving-enzyme-1-inhibitory-activities-of-cornuside-and-gallotannins-from-cornus-officinalis-fruits
#6
Himanshu Kumar Bhakta, Chan Hum Park, Takako Yokozawa, Takashi Tanaka, Hyun Ah Jung, Jae Sue Choi
Cholinesterase (ChE) and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors are promising agents for the treatment of Alzheimer's disease (AD). In the present study, we examined the inhibitory activity of seven compounds isolated from the fruits of Cornus officinalis, cornuside, polymeric proanthocyanidins, 1,2,3-tri-O-galloyl-β-D-glucose, 1,2,3,6-tetra-O-galloyl-β-D-glucose, tellimagrandin I, tellimagrandin II, and isoterchebin, against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and BACE1...
June 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28585866/design-synthesis-and-evaluation-of-novel-cinnamic-acid-derivatives-bearing-n-benzyl-pyridinium-moiety-as-multifunctional-cholinesterase-inhibitors-for-alzheimer-s-disease
#7
Jin-Shuai Lan, Jian-Wei Hou, Yun Liu, Yue Ding, Yong Zhang, Ling Li, Tong Zhang
A novel family of cinnamic acid derivatives has been developed to be multifunctional cholinesterase inhibitors against AD by fusing N-benzyl pyridinium moiety and different substituted cinnamic acids. In vitro studies showed that most compounds were endowed with a noteworthy ability to inhibit cholinesterase, self-induced Aβ (1-42) aggregation, and to chelate metal ions. Especially, compound 5l showed potent cholinesterase inhibitory activity (IC50, 12.1 nM for eeAChE, 8.6 nM for hAChE, 2.6 μM for eqBuChE and 4...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28573890/resorcinol-catechol-and-saligenin-based-bronchodilating-%C3%AE-2-agonists-as-inhibitors-of-human-cholinesterase-activity
#8
Anita Bosak, Anamarija Knežević, Ivana Gazić Smilović, Goran Šinko, Zrinka Kovarik
We investigated the influence of bronchodilating β2-agonists on the activity of human acetylcholinesterase (AChE) and usual, atypical and fluoride-resistant butyrylcholinesterase (BChE). We determined the inhibition potency of racemate and enantiomers of fenoterol as a resorcinol derivative, isoetharine and epinephrine as catechol derivatives and salbutamol and salmeterol as saligenin derivatives. All of the tested compounds reversibly inhibited cholinesterases with Ki constants ranging from 9.4 μM to 6...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28571775/critical-role-of-ca1-muscarinic-receptors-on-memory-acquisition-deficit-induced-by-total-tsd-and-rem-sleep-deprivation-rsd
#9
Bibi-Zahra Javad-Moosavi, GholamHassan Vaezi, Mohammad Nasehi, Seyed-Ali Haeri-Rouhani, Mohammad-Reza Zarrindast
AIM: Despite different theories regarding sleep physiological function, an overall census indicates that sleep is useful for neural plasticity which eventually strengthens cognition and brain performance. Different studies show that sleep deprivation (SD) leads to impaired learning and hippocampus dependent memory. According to some studies, cholinergic system plays an important role in sleep (particularly REM sleep), learning, memory, and its retrieval. So this study has been designed to investigate the effect of CA1 Cholinergic Muscarinic Receptors on memory acquisition deficit induced by total sleep deprivation (TSD) and REM sleep deprivation (RSD)...
May 29, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28566624/distigmine-bromide-produces-sustained-potentiation-of-guinea-pig-urinary-bladder-motility-by-inhibiting-cholinesterase-activity
#10
Keisuke Obara, Daisuke Chino, Yoshio Tanaka
Distigmine is a cholinesterase (ChE) inhibitor used for the treatment of detrusor underactivity in Japan. Distigmine's pharmacological effects are known to be long-lasting, but the duration of its effect on urinary bladder contractile function has not been fully elucidated. The present study aimed to determine these effects in relation to the plasma concentrations of distigmine and its inhibition of ChE activities in blood, plasma, and bladder tissue. Intravesical pressures were recorded in anesthetized guinea-pigs for 12 h after the intravenous administration of saline or distigmine (0...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28550260/living-alone-with-alzheimer-s-disease-data-from-svedem-the-swedish-dementia-registry
#11
Pavla Cermakova, Maja Nelson, Juraj Secnik, Sara Garcia-Ptacek, Kristina Johnell, Johan Fastbom, Lena Kilander, Bengt Winblad, Maria Eriksdotter, Dorota Religa
BACKGROUND: Many people with Alzheimer's disease (AD) live alone in their own homes. There is a lack of knowledge about whether these individuals receive the same quality of diagnostics and treatment for AD as patients who are cohabiting. OBJECTIVES: To investigate the diagnostic work-up and treatment of community-dwelling AD patients who live alone. METHODS: We performed a cross-sectional cohort study based on data from the Swedish Dementia Registry (SveDem)...
May 25, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28545383/quinolinic-carboxylic-acid-derivatives-as-potential-multi-target-compounds-for-neurodegeneration-monoamine-oxidase-and-cholinesterase-inhibition
#12
Nehal Afreen Khan, Imtiaz Khan, Syed Mobasher Ali Abid, Sumera Zaib, Aliya Ibrar, Hina Andleeb, Shahid Hameed, Jamshed Iqbal
BACKGROUND: Parkinson&#039;s disease (PD), a debilitating and progressive disorder, is among the most challenging and devastating neurodegenerative diseases predominantly affecting the people over 60 years of age. OBJECTIVES: To confront PD, an advanced and operational strategy is to design single chemical functionality able to control more than one target instantaneously. METHODS: In this endeavor, for the exploration of new and efficient inhibitors of Parkinson&#039;s disease, we synthesized a series of quinoline carboxylic acids (3a‒j) and evaluated their in-vitro monoamine oxidase and cholinesterase inhibitory activities...
May 25, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28544873/3d-qsar-studies-of-some-reversible-acetyl-cholinesterase-inhibitors-based-on-comfa-and-ligand-protein-interaction-fingerprints-using-pc-ls-svm-and-pls-ls-svm
#13
Hamidreza Ghafouri, Mohsen Ranjbar, Amirhossein Sakhteman
A great challenge in medicinal chemistry is to develop different methods for structural design based on the pattern of the previously synthesized compounds. In this study two different QSAR methods were established and compared for a series of piperidine acetylcholinesterase inhibitors. In one novel approach, PC-LS-SVM and PLS-LS-SVM was used for modeling 3D interaction descriptors, and in the other method the same nonlinear techniques were used to build QSAR equations based on field descriptors. Different validation methods were used to evaluate the models and the results revealed the more applicability and predictive ability of the model generated by field descriptors (Q(2)LOO-CV=1, R(2)ext=0...
May 10, 2017: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/28544619/design-and-synthesis-of-some-acridine-piperazine-hybrids-for-the-improvement-of-cognitive-dysfunction
#14
Anuradha Sharma, Poonam Piplani
A novel series of hybrid molecules (5a-5m) was designed, synthesized and evaluated as multifunctional cholinesterase (ChE) inhibitors against cognitive dysfunction. Heterocyclic moieties acridine and piperazine were conjugated with suitable linkers in a single scaffold and the structures of the target compounds were confirmed by IR, (1) H NMR, (13) C NMR and LC-MS analysis. The pharmacological activity of synthesized compounds was evaluated using behavioral models of amnesia viz. step down passive avoidance and elevated plus maze at a dose 0...
May 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28535697/identification-of-peptides-present-in-sour-milk-whey-that-ameliorate-scopolamine-induced-memory-impairment-in-mice
#15
Kazuhito Ohsawa, Naoto Uchida, Kohji Ohki, Hidehiko Yokogoshi
Cognitive impairment is treated with cholinesterase inhibitors that slow cognitive decline but cause significant adverse effects. Functional foods that improve memory without such effects would therefore be valuable. We reported that unidentified components of sour milk whey produced by fermentations using Lactobacillus helveticus and Saccharomyces cerevisiae improved memory in a mouse model of scopolamine-induced memory impairment. Here, we show that casein-derived peptides were the most active components of orally administered fractions of this milk product...
May 23, 2017: International Journal of Food Sciences and Nutrition
https://www.readbyqxmd.com/read/28534003/new-pharmacological-approaches-to-treating-non-motor-symptoms-of-parkinson-s-disease
#16
Michael A Kelberman, Elena M Vazey
PURPOSE OF REVIEW: Non-motor symptoms in patients with Parkinson's Disease (PD) are better predictors of quality of life changes, caregiver burden, and mortality than motor symptoms. Levodopa has limited, and sometimes detrimental, effects on these symptoms. In this review we discuss recent evidence on pharmacological treatments for non-motor symptoms. RECENT FINDINGS: Breakthroughs have been made in the treatment of psychosis and sleep dysfunction. Pimavanserin has become the first FDA approved drug for PD psychosis...
December 2016: Current Pharmacology Reports
https://www.readbyqxmd.com/read/28524136/-clinical-evaluation-of-the-effectiveness-of-cholinesterase-inhibition-with-neuromidin-in-the-treatment-of-primary-glaucoma-patients
#17
I A Zakharova, R V Avdeev, V A Pristavka, S N Surnin, V Yu Makhmutov, I I Savrasova
AIM: to investigate neuromidin effectiveness in the treatment of patients with primary glaucoma and compensated intraocular pressure (IOP). MATERIAL AND METHODS: A total of 40 patients (80 eyes) were examined. Of them, 10 eyes with early glaucoma, 36 eyes with moderate-stage glaucoma, 33 eyes with advanced glaucoma, and 1 eye with end-stage glaucoma. In 19 eyes, IOP was controlled through beta-blockers, in 11 eyes - through carbonic anhydrase inhibitors, in 10 eyes - through prostaglandin analogues, and in 39 eyes - through combination drugs...
2017: Vestnik Oftalmologii
https://www.readbyqxmd.com/read/28514891/synergistic-effect-of-rapamycin-and-metformin-against-age-dependent-oxidative-stress-in-rat-erythrocyte
#18
Abhishek Kumar Singh, Geetika Garg, Sandeep Singh, Syed Ibrahim Rizvi
Erythrocytes are particularly vulnerable towards age-dependent oxidative stress mediated damage. Caloric restriction mimetics (CRMs) may provide a novel strategy for the maintenance of redox balance as well as effective treatment of age associated diseases. Herein, we have investigated the beneficial effect of co-treatment of CRM-candidate drugs, rapamycin (an immunosuppressant drug and inhibitor of mammalian target of rapamycin) and metformin (an anti-diabetic biguanide and activator of adenosine monophosphate kinase) against aging-induced oxidative stress in erythrocytes and plasma of aging rats...
May 17, 2017: Rejuvenation Research
https://www.readbyqxmd.com/read/28511871/effect-of-distigmine-on-the-contractile-response-of-guinea-pig-urinary-bladder-to-electrical-field-stimulation
#19
Keisuke Obara, Yurina Kobayashi, Daisuke Chino, Yoshio Tanaka
Distigmine bromide (distigmine) is a reversible carbamate group cholinesterase (ChE) inhibitor. Although mainly used clinically for the treatment of myasthenia gravis, distigmine is also indicated for detrusor underactivity in Japan. According to the pharmacological classification of distigmine, its therapeutic effect against detrusor underactivity appears to be produced by enhanced urinary bladder smooth muscle (UBSM) contractility due to an increased concentration of acetylcholine between parasympathetic nerve endings and UBSM cells...
May 13, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28508250/a-real-world-analysis-of-treatment-patterns-for-cholinesterase-inhibitors-and-memantine-among-newly-diagnosed-alzheimer-s-disease-patients
#20
Nawal Bent-Ennakhil, Florence Coste, Lin Xie, Myrlene Sanon Aigbogun, Yuexi Wang, Furaha Kariburyo, Ann Hartry, Onur Baser, Peter Neumann, Howard Fillit
INTRODUCTION: Alzheimer's disease (AD) is the most common neurodegenerative form of dementia. Pharmacological therapies for symptomatic treatment, such as acetylcholinesterase inhibitors (AChEIs) and memantine, have been available in the USA since 2000. Over the past decade, few studies have analyzed real-world anti-dementia treatment patterns in the USA. This study evaluated monotherapy AChEIs and memantine treatment patterns among newly diagnosed AD patients. METHODS: A retrospective cohort study was conducted using Medicare data and the Minimum Data Set from 2008 to 2012...
June 2017: Neurology and Therapy
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