keyword
MENU ▼
Read by QxMD icon Read
search

Cholinesterase inhibitors

keyword
https://www.readbyqxmd.com/read/28416036/exploring-dementia-management-attitudes-in-primary-care-a-key-informant-survey-to-primary-care-physicians-in-25-european-countries
#1
Ferdinando Petrazzuoli, Shlomo Vinker, Tuomas H Koskela, Thomas Frese, Nicola Buono, Jean Karl Soler, Jette Ahrensberg, Radost Asenova, Quintí Foguet Boreu, Gülsen Ceyhun Peker, Claire Collins, Miro Hanževački, Kathryn Hoffmann, Claudia Iftode, Donata Kurpas, Jean Yves Le Reste, Bjørn Lichtwarck, Davorina Petek, Daniel Pinto, Diego Schrans, Sven Streit, Eugene Yee Hing Tang, Athina Tatsioni, Péter Torzsa, Pemra C Unalan, Harm van Marwijk, Hans Thulesius
BACKGROUND: Strategies for the involvement of primary care in the management of patients with presumed or diagnosed dementia are heterogeneous across Europe. We wanted to explore attitudes of primary care physicians (PCPs) when managing dementia: (i) the most popular cognitive tests, (ii) who had the right to initiate or continue cholinesterase inhibitor or memantine treatment, and (iii) the relationship between the permissiveness of these rules/guidelines and PCP's approach in the dementia investigations and assessment...
April 18, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/28413513/huperzine-a-inhibits-immediate-addictive-behavior-but-not-behavioral-sensitization-following-repeated-morphine-administration-in-rats
#2
Jinling Sun, Lin Tian, Ruisi Cui, Xinwang Li
Acetylcholinesterase inhibitors are regarded as promising therapeutic agents to treat addiction. The current study aimed to examine the effects of huperzine A, a cholinesterase inhibitor, on behavioral sensitization induced by repeated morphine administration and relapse induced by contextual conditioning. The present study also assessed whether the state-dependency hypothesis may explain the results. Adult rats were divided into four groups (n=8) and intraperitoneally injected with 0.2, 0.3 or 0.4 mg/kg huperzine A or saline (1 ml/kg, control), for 5 days...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28406525/an-improved-radiosynthesis-of-o-2-18-f-fluoroethyl-o-p-nitrophenyl-methylphosphonate-a-first-in-class-cholinesterase-pet-tracer
#3
Kiel D Neumann, Charles M Thompson, Joseph E Blecha, John M Gerdes, Henry F VanBrocklin
O-(2-Fluoroethyl)-O-(p-nitrophenyl) methylphosphonate 1 is an organophosphate (OP) cholinesterase inhibitor, which creates a phosphonyl-serine covalent adduct at the enzyme active site blocking cholinesterase activity in vivo. The corresponding radiolabeled O-(2-[(18) F]fluoroethyl)-O-(p-nitrophenyl) methylphosphonate, [(18) F]1, has been previously prepared and found to be an excellent positron emission tomography (PET) imaging tracer for assessment of cholinesterases in live brain, peripheral tissues and blood...
April 12, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28404526/stereospecific-cholinesterase-inhibition-by-o-s-diethylphenylphosphonothioate
#4
Ahmed Mohammed, Jennifer Sneathen, Sara Glazier Frojen, Louis Kuo, Cynthia M Dupureur
The inhibition kinetics and stereospecificity of the chiral nerve agent derivative O,S-diethylphenylphosphonothioate (DEPP) were examined for two forms of acetylcholinesterase (human and eel) and equine butyrylcholinesterase. Both S- and R-DEPP are poor inhibitors of eel AChE (IC50 150μM), consistent with a large, nondiscriminatory binding interaction in the active site of this enzyme. However, S-DEPP is active against human and equine AChE with low μM IC50s. DEPP stereospecificities (S/R) toward these enzymes are moderate (20) relative to other cholinesterase-organophosphate (OP) systems...
March 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28400237/cytochrome-p450-binding-studies-of-novel-tacrine-derivatives-predicting-the-risk-of-hepatotoxicity
#5
Alanna McEneny-King, Wesseem Osman, Andrea N Edginton, Praveen P N Rao
The 1,2,3,4-tetrahydroacridine derivative tacrine was the first drug approved to treat Alzheimer's disease (AD). It is known to act as a potent cholinesterase inhibitor. However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2. Despite these challenges, tacrine serves as a useful template in the development of novel multi-targeting anti-AD agents. In this regard, we sought to evaluate the risk of hepatotoxicity in a series of C9 substituted tacrine derivatives that exhibit cholinesterase inhibition properties...
April 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28388521/design-synthesis-and-biological-activity-of-novel-donepezil-derivatives-bearing-n-benzyl-pyridinium-moiety-as-potent-and-dual-binding-site-acetylcholinesterase-inhibitors
#6
Jin-Shuai Lan, Tong Zhang, Yun Liu, Jing Yang, Sai-Sai Xie, Jing Liu, Ze-Yang Miao, Yue Ding
A series of new donepezil derivatives were designed synthesized and evaluated as multifunctional cholinesterase inhibitors against Alzheimer's disease (AD). In vitro studies showed that most of them exhibited significant potency to inhibit acetylcholinesterase and self-induced β-amyloid (Aβ) aggregation, and moderate antioxidant activity. Especially, compound 5b presented the greatest ability to inhibit cholinesterase (IC50, 1.9 nM for eeAChE and 0.8 nM for hAChE), good inhibition of Aβ aggregation (53...
March 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28387023/simultaneous-usage-of-dementia-medications-and-anticholinergics-among-asians-and-pacific-islanders
#7
Brian R Schultz, Junji Takeshita, Deborah Goebert, Steven Takeshita, Brett Y Lu, Alexandre Guilloux, Joy Higa
BACKGROUND: The simultaneous use of dementia medications and anticholinergic medications occurs frequently. Cholinesterase inhibitors and anticholinergic medications likely counteract one another, potentially exposing patients to medications with decreased benefit, more adverse effects, and higher cost of care. We identified the rate of concurrent prescriptions of cholinesterase inhibitors/memantine with anticholinergics in an urban hospital setting with a large Asian and Pacific Islander population...
April 7, 2017: Psychogeriatrics: the Official Journal of the Japanese Psychogeriatric Society
https://www.readbyqxmd.com/read/28358738/%C3%AE-7-nicotinic-acetylcholine-receptor-inhibition-by-indinavir-implications-for-cognitive-dysfunction-in-treated-hiv-disease
#8
Sean Ekins, Paul Mathews, Erin K Saito, Natalie Diaz, David Naylor, Julia Chung, Aaron M McMurtray
OBJECTIVE: This study set out to determine if the human immunodeficiency virus (HIV) protease inhibitor, indinavir, alters responsiveness of α7-nicotinic acetylcholine receptors to acetylcholine. DESIGN: Treatment with highly active antiretroviral therapy has dramatically reduced development of HIV associated dementia and more severe forms of cognitive impairment. However, many individuals continue to experience cognitive decline of uncertain etiology. Previous studies have failed to demonstrate significant alterations of functional brain connectivity, structural brain changes, or changes in cerebral blood flow sufficient to explain cognitive decline in virally suppressed individuals...
March 29, 2017: AIDS
https://www.readbyqxmd.com/read/28356027/natural-polyphenols-in-the-treatment-of-alzheimer-s-disease
#9
Syed Badrul Syarifah Noratiqah, Isa Naina-Mohamed, Mohamed S Zulfarina, H M S Qodriyah
Neurodegenerative disease is an incurable disease which involves the degeneration or death of the nerve cells. Alzheimer's Disease (AD) is a neurodegenerative disease discovered in 1906 by Alois Alzheimer, a German clinical psychiatrist and neuroanatomist. The main pathological hallmarks of this disease are the formation of extracellular amyloid β (Aβ) plaques and intracellular neurofibrillary tangle (NFT). The accumulation of the amyloid protein aggregates in the brain of AD patients leads to oxidative stress and inflammation...
March 28, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28351483/surface-modified-nano-lipid-drug-conjugates-of-positive-allosteric-modulators-of-m1-muscarinic-acetylcholine-receptor-for-the-treatment-of-alzheimer-s-disease
#10
Pavan Kumar Chintamaneni, Praveen T Krishnamurthy, Pachava Vengal Rao, SaiKiran S S Pindiprolu
Acetyl Cholinesterase (AChE) inhibitors such as Donepezil, Rivastigmine and Galantamine are approved by US-FDA as first line drugs to treat the cognitive symptoms of Alzheimer's disease (AD). Their beneficial effects are attributed to their ability to elevate endogenous acetylcholine (ACh) at the M1 muscarinic receptor in the brain. However, their side effects such as nausea, vomiting, dizziness, insomnia, loss of appetite and altered heart rate are related to non-specific activation of M2-M5 muscarinic subtypes in various tissues...
April 2017: Medical Hypotheses
https://www.readbyqxmd.com/read/28341540/clinical-meaningfulness-of-alzheimer-s-disease-assessment-scale-cognitive-subscale-change-in-relation-to-goal-attainment-in-patients-on-cholinesterase-inhibitors
#11
Kenneth Rockwood, Susan E Howlett, Deborah Hoffman, Rachel Schindler, Arnold Mitnitski
INTRODUCTION: The clinical meaningfulness of Alzheimer's Disease Assessment Scale-Cognitive subscale (ADAS-Cog) subscale change is disputed. We compared 2- to 4-point ADAS-Cog changes with changes in Goal Attainment Scaling (GAS) and everyday function across initial ADAS-Cog scores and treatment responses. METHODS: This exploratory analysis evaluated mild-moderate Alzheimer's disease patients treated with donepezil (12 months) or galantamine (8 months). Clinical meaningfulness was defined as concomitant ADAS-Cog and GAS changes of ±3 points and/or functional improvement...
March 21, 2017: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
https://www.readbyqxmd.com/read/28336568/cholinergic-but-not-dopaminergic-or-noradrenergic-enhancement-sharpens-visual-spatial-perception-in-humans
#12
Caterina Gratton, Sahar Yousef, Esther Aarts, Deanna L Wallace, Mark D'Esposito, Michael A Silver
The neuromodulator acetylcholine modulates spatial integration in visual cortex by altering the balance of inputs that generate neuronal receptive fields. These cholinergic effects may provide a neurobiological mechanism underlying the modulation of visual representations by visual spatial attention. However, the consequences of cholinergic enhancement on visuospatial perception in humans are unknown. We conducted two experiments to test whether enhancing cholinergic signaling selectively alters perceptual measures of visuospatial interactions in human subjects...
April 19, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28328690/the-first-use-of-pralidoxime-in-a-child-with-rivastigmine-poisoning
#13
Eylem Ulaş Saz, Ali Yurtseven, Mehmet Arda Kilinç, Yusuf Sari, Hasan Ağin
The aim of this report is to describe the successful use of pralidoxime in a pediatric patient who accidentally ingested 12 mg of rivastigmine and presented to the emergency department with weakness, drowsiness, hyporeactivity to environmental stimuli, and full cholinergic syndrome. CASE: The patient presented to the emergency department 2 hours after a suspected ingestion of rivastigmine. He was sleepy but oriented and cooperative, hypotonic, and hyporeflexic and has a Glasgow Coma Scale score of 13 (E3M6V4)...
March 21, 2017: Pediatric Emergency Care
https://www.readbyqxmd.com/read/28321840/association-of-proton-pump-inhibitors-usage-with-risk-of-pneumonia-in-dementia-patients
#14
Sai-Wai Ho, Ying-Hock Teng, Shun-Fa Yang, Han-Wei Yeh, Yu-Hsun Wang, Ming-Chih Chou, Chao-Bin Yeh
OBJECTIVES: To determine the association between usages of proton pump inhibitors (PPIs) and subsequent risk of pneumonia in dementia patients. DESIGN: Retrospective cohort study. SETTING: Taiwanese National Health Insurance Research Database. PARTICIPANTS: The study cohort consisted of 786 dementia patients with new PPI usage and 786 matched dementia patients without PPI usage. MEASUREMENTS: The study endpoint was defined as the occurrence of pneumonia...
March 21, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28302511/design-synthesis-and-biological-evaluation-of-multifunctional-tacrine-curcumin-hybrids-as-new-cholinesterase-inhibitors-with-metal-ions-chelating-and-neuroprotective-property
#15
Zhikun Liu, Lei Fang, Huan Zhang, Shaohua Gou, Li Chen
Total sixteen tacrine-curcumin hybrid compounds were designed and synthesized for the purpose of searching for multifunctional anti-Alzheimer agents. In vitro studies showed that these hybrid compounds showed good cholinesterase inhibitory activity. Particularly, the potency of K3-2 is even beyond tacrine. Some of the compounds exhibited different selectivity on acetylcholinesterase or butyrylcholinesterase due to the structural difference. Thus, the structure and activity relationship is summarized and further discussed based on molecular modeling studies...
March 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28299395/phenyl-valerate-esterase-activity-of-human-butyrylcholinesterase
#16
Iris Mangas, Eugenio Vilanova, Jorge Estévez
Phenyl valerate is used for detecting and measuring neuropathy target esterase (NTE) and has been used for discriminating esterases as potential target in hen model of organophosphorus delayed neuropathy. In previous studies we observed that phenyl valerate esterase (PVase) activity of an enzymatic fraction in chicken brain might be due to a butyrylcholinesterase protein (BuChE), and it was suggested that this enzymatic fraction could be related to the potentiation/promotion phenomenon of the organophosphate-induced delayed neuropathy (OPIDN)...
March 15, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28274859/longitudinal-lipid-profile-variations-and-clinical-change-in-alzheimer-s-disease-dementia
#17
Fabricio Ferreira de Oliveira, Elizabeth Suchi Chen, Marilia Cardoso Smith, Paulo Henrique Ferreira Bertolucci
Hypercholesterolemia and statin use have been unevenly associated with clinical change in Alzheimer's disease dementia. In this longitudinal study, 192 consecutive outpatients with late-onset Alzheimer's disease dementia were stratified according to APOE haplotypes, and followed for one year to investigate associations of lipid profile variations and lipophilic statin therapy with changes in cognition, caregiver burden, basic and instrumental functionality. Overall, 102 patients (53.1%) carried APOE4+ haplotypes and 90 (46...
April 12, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28274151/pharmacophore-based-design-and-discovery-of-meptazinol-carbamates-as-dual-modulators-of-cholinesterase-and-amyloidogenesis
#18
Qiong Xie, Zhaoxi Zheng, Biyun Shao, Wei Fu, Zheng Xia, Wei Li, Jian Sun, Wei Zheng, Weiwei Zhang, Wei Sheng, Qihong Zhang, Hongzhuan Chen, Hao Wang, Zhuibai Qiu
Multifunctional carbamate-type acetylcholinesterase (AChE) inhibitors with anti-amyloidogenic properties like phenserine are potential therapeutic agents for Alzheimer's disease (AD). We reported here the design of new carbamates using pharmacophore model strategy to modulate both cholinesterase and amyloidogenesis. A five-feature pharmacophore model was generated based on 25 carbamate-type training set compounds. (-)-Meptazinol carbamates that superimposed well upon the model were designed and synthesized, which exhibited nanomolar AChE inhibitory potency and good anti-amyloidogenic properties in in vitro test...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28271317/cholinergic-anti-inflammatory-pathway-does-not-contribute-to-prevention-of-ulcerative-colitis-by-novel-indoline-carbamates
#19
Helena Shifrin, Odelia Mouhadeb, Nathan Gluck, Chen Varol, Marta Weinstock
Indoline carbamates, AN680 and AN917 decrease cytokines, TNF-α and IL-6 in peritoneal macrophages activated by lipopolysaccharide (LPS) and in mouse tissues after LPS injection. They prevent nuclear translocation of nuclear factor κB (NF-κB) and activator protein 1. Only AN917 inhibits cholinesterase (ChE) at relevant concentrations. ChE inhibitors decrease NF-κB by activating α7 nicotinic acetylcholine receptors (α7nAChR). The current study compared the effect of rivastigmine, a ChE inhibitor, AN680 and AN917 on ulcerative colitis induced in mice by ingestion of dextran sodium sulfate (4...
March 7, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/28267984/pyridoxine-resveratrol-hybrids-mannich-base-derivatives-as-novel-dual-inhibitors-of-ache-and-mao-b-with-antioxidant-and-metal-chelating-properties-for-the-treatment-of-alzheimer-s-disease
#20
Xia Yang, Xiaoming Qiang, Yan Li, Li Luo, Rui Xu, Yunxiaozhu Zheng, Zhongcheng Cao, Zhenghuai Tan, Yong Deng
A series of pyridoxine-resveratrol hybrids Mannich base derivatives as multifunctional agents have been designed, synthesized and evaluated for cholinesterase (ChE) and monoamine oxidase (MAO) inhibitory activity. To further explore the multifunctional properties of the new derivatives, their antioxidant activities and metal-chelating properties were also tested. The results showed that most of these compounds could selectively inhibit acetylcholinesterase (AChE) and MAO-B. Among them, compounds 7d and 8b exhibited the highest potency for AChE inhibition with IC50 values of 2...
February 28, 2017: Bioorganic Chemistry
keyword
keyword
16265
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"