keyword
MENU ▼
Read by QxMD icon Read
search

Cholinesterase inhibitors

keyword
https://www.readbyqxmd.com/read/28328690/the-first-use-of-pralidoxime-in-a-child-with-rivastigmine-poisoning
#1
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
#2
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
#3
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
#4
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
#5
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...
March 6, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28274151/pharmacophore-based-design-and-discovery-of-meptazinol-carbamates-as-dual-modulators-of-cholinesterase-and-amyloidogenesis
#6
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
#7
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
#8
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
https://www.readbyqxmd.com/read/28266279/synthesis-characterization-and-cholinesterase-inhibition-studies-of-new-arylidene-aminothiazolylethanone-derivatives
#9
Jamshed Iqbal, Ghulam Shabir, Fayaz A Larik, Shafi Ullah Khan, Aamer Saeed, Muhammad S Shah, Pervaiz A Channar
BACKGROUND: Alzheimer's disease is caused by the destruction or loss of cholinergic cells that produce or use ACh in the brain, thereby reducing the availability of enzyme to other cells. The major treatment strategy for AD is to decrease the level of cholinesterase in the brain. OBJECTIVE: The aim of this study was to describe the effect of novel series of thiazole derivatives i.e. arylidene aminothiazolylethanones (3a-h) as cholinesterase inhibitors (CEIs). METHODS: A novel series of thiazole derivatives i...
March 6, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28255308/development-of-a-nanoprecipitation-method-for-the-entrapment-of-a-very-water-soluble-drug-into-eudragit-rl-nanoparticles
#10
Sara Salatin, Jaleh Barar, Mohammad Barzegar-Jalali, Khosro Adibkia, Farhad Kiafar, Mitra Jelvehgari
Rivastigmine hydrogen tartrate (RHT), one of the potential cholinesterase inhibitors, has received great attention as a new drug candidate for the treatment of Alzheimer's disease. However, the bioavailability of RHT from the conventional pharmaceutical forms is low because of the presence of the blood brain barrier. The main aim of the present study was to prepare positively charged Eudragit RL 100 nanoparticles as a model scaffold for providing a sustained release profile for RHT. The formulations were evaluated in terms of particle size, zeta potential, surface morphology, X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC)...
February 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28253832/emerging-chemical-therapies-targeting-5-hydroxytryptamine-in-the-treatment-of-alzheimer-s-disease
#11
Amanda Calhoun, Je Ko, George T Grossberg
Alzheimer's disease (AD) is a major neuropsychiatric disorder affecting more than 5 million Americans over age 65. By the year 2050, AD is expected to affect over 30 million. Characterized by neuronal cell death accompanied by the accumulation of neurofibrillary tangles and neuritic plaques, AD results in devastating clinical symptomatology with a lasting psychosocial and financial impact. Studies have shown that the current treatments for AD, cholinesterase inhibitors (ChEI's) and NMDA receptor antagonists, have limited efficacy...
March 2017: Expert Opinion on Emerging Drugs
https://www.readbyqxmd.com/read/28245905/synthesis-of-readily-available-fluorophenylalanine-derivatives-and-investigation-of-their-biological-activity
#12
Martin Krátký, Šárka Štěpánková, Katarína Vorčáková, Lucie Navrátilová, František Trejtnar, Jiřina Stolaříková, Jarmila Vinšová
A series of thirty novel N-acetylated fluorophenylalanine-based aromatic amides and esters was synthesized using N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide or phosphorus trichloride in pyridine. They were characterized by spectral methods and screened against various microbes (Mycobacterium tuberculosis, non-tuberculous mycobacteria, other bacteria, fungi), for their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and cytotoxicity. All amino acids derivatives revealed a moderate inhibition of both cholinesterases with IC50 values for AChE and BChE of 57...
February 21, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28238772/assessment-of-anti-cholinesterase-activity-and-cytotoxicity-of-cagaita-eugenia-dysenterica-leaves
#13
Cristian A Gasca, Willian O Castillo, Catarina Satie Takahashi, Christopher W Fagg, Pérola O Magalhães, Yris M Fonseca-Bazzo, Dâmaris Silveira
Eugenia dysenterica ex DC Mart. (Myrtaceae) is a Brazilian tree with pharmacological and biological properties. The aqueous leaf extract, rich in polyphenols, was tested in the human neuroblastoma cell line SH-SY5Y to evaluate its effect on cell viability. The extract and two isolated compounds were also assessed for the potential inhibitory activity on acetylcholinesterase, an enzyme related to Alzheimer's disease. A simple chromatographic method using Sephadex LH-20 was developed to separate catechin and quercetin from the aqueous leaf extract of E...
February 24, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28236784/effects-of-donepezil-on-sleep-disturbances-in-patients-with-dementia-with-lewy-bodies-an-open-label-study-with-actigraphy
#14
Hiroaki Kazui, Hiroyoshi Adachi, Hideki Kanemoto, Kenji Yoshiyama, Tamiki Wada, Keiko Tokumasu Nomura, Toshihisa Tanaka, Manabu Ikeda
We investigated whether donepezil, a cholinesterase inhibitor, can be used to treat sleep disturbances in patients with dementia with Lewy bodies (DLB). Sleep disturbances were evaluated with the sleep disturbances item of the Neuropsychiatric inventory (NPI) and an actigraph in 16 DLB patients and 24 normal elderly control (NC) subjects. The presence/absence of nine kinds of sleep symptoms, such as dream enactment, were also evaluated in the DLB patients. The DLB patients were then given 5mg/day donepezil for 14 weeks and evaluated again...
February 20, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28235599/diazinon-and-parathion-diverge-in-their-effects-on-development-of-noradrenergic-systems
#15
Theodore A Slotkin, Samantha Skavicus, Frederic J Seidler
Organophosphate pesticides elicit developmental neurotoxicity through mechanisms over and above their shared property as cholinesterase inhibitors. We compared the consequences of neonatal exposure (postnatal days PN1-4) to diazinon or parathion on development of norepinephrine systems in rat brain, using treatments designed to produce equivalent effects on cholinesterase, straddling the threshold for barely-detectable inhibition. Norepinephrine levels were measured throughout development from the immediate posttreatment period (PN5), to early adolescence (PN30), young adulthood (PN60) and full adulthood (PN100); we assessed multiple brain regions containing all the major noradrenergic synaptic projections...
February 21, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28228653/drug-prescription-appropriateness-in-the-elderly-an-italian-study
#16
Nicola Allegri, Federica Rossi, Federica Del Signore, Paolo Bertazzoni, Roberto Bellazzi, Giorgio Sandrini, Tomaso Vecchi, Davide Liccione, Alessia Pascale, Stefano Govoni
PURPOSE: Correct drug prescription in the elderly is a difficult task that requires careful survey of the current pharmacological therapies. In this article, we reviewed the drug prescriptions provided to 860 persons aged 65 years or over, residing in a small city of Lombardy, Italy. METHODS: Subjects were recruited from a local nursing home, the Pavia and Vigevano Neuropsychological Center for Alzheimer's Disease, general practitioners' offices, and the local University of the Third Age...
2017: Clinical Interventions in Aging
https://www.readbyqxmd.com/read/28222858/bioprofiling-of-salicaceae-bud-extracts-through-high-performance-thin-layer-chromatography-hyphenated-to-biochemical-microbiological-and-chemical-detections
#17
Salim Hage, Gertrud E Morlock
The buds of poplars (Populus L.) and willows (Salix L.), both from the same family (Salicaceae Mirbel), are increasingly used in gemmotherapy and importantly contribute to the production of the physiologically active propolis by European bee Apis mellifera L. In order to study their phenolic profiles, polar extracts of buds from P. nigra L. were compared to those of P. alba L. and S. alba L. through high-performance thin-layer chromatography (HPTLC). Five chemotypical patterns were distinguished after derivatisation with the Natural Product reagent and confirmed by principal component analysis...
February 14, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28222815/cognitive-stimulation-therapy-as-a-sustainable-intervention-for-dementia-in-sub-saharan-africa-feasibility-and-clinical-efficacy-using-a-stepped-wedge-design
#18
Stella-Maria Paddick, Sarah Mkenda, Godfrey Mbowe, Aloyce Kisoli, William K Gray, Catherine L Dotchin, Laura Ternent, Adesola Ogunniyi, John Kissima, Olaide Olakehinde, Declare Mushi, Richard W Walker
BACKGROUND: Cognitive stimulation therapy (CST) is a psychosocial group-based intervention for dementia shown to improve cognition and quality of life with a similar efficacy to cholinesterase inhibitors. Since CST can be delivered by non-specialist healthcare workers, it has potential for use in low-resource environments, such as sub-Saharan Africa (SSA). We aimed to assess the feasibility and clinical effectiveness of CST in rural Tanzania using a stepped-wedge design. METHODS: Participants and their carers were recruited through a community dementia screening program...
February 22, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/28201726/discontinuation-efficacy-and-safety-of-cholinesterase-inhibitors-for-alzheimer-s-disease-a-meta-analysis-and-meta-regression-of-44-randomized-clinical-trials-enrolling-16-245-patients
#19
Lídia Blanco-Silvente, Xavier Castells, Marc Saez, Maria Antònia Barceló, Josep Garre-Olmo, Joan Vilalta-Franch, Dolors Capellà
No abstract text is available yet for this article.
February 13, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28198801/inhibitory-effects-of-cholinesterase-inhibitor-donepezil-on-the-kv1-5-potassium-channel
#20
Kai Li, Neng Cheng, Xian-Tao Li
Kv1.5 channels carry ultra-rapid delayed rectifier K(+) currents in excitable cells, including neurons and cardiac myocytes. In the current study, the effects of cholinesterase inhibitor donepezil on cloned Kv1.5 channels expressed in HEK29 cells were explored using whole-cell recording technique. Exposure to donepezil resulted in a rapid and reversible block of Kv1.5 currents, with an IC50 value of 72.5 μM. The mutant R476V significantly reduced the binding affinity of donepezil to Kv1.5 channels, showing the target site in the outer mouth region...
February 13, 2017: Scientific Reports
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"