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https://www.readbyqxmd.com/read/27911310/cholinergic-modification-of-neurogenesis-and-gliosis-improves-the-memory-of%C3%A2-a%C3%AE-ppswe-psen1de9-alzheimer-s-disease-model-mice-fed-a-high-fat-diet
#1
Takeshi Matsuda, Tatsuhiro Hisatsune
We previously reported that neuroinflammation contributes to the amnesia of AβPPswe/PSEN1dE9 Alzheimer's disease model mice fed a high-fat diet to induce type-2 diabetes (T2DM-AD mice), but the underlying mechanism for the memory decline remained unclear. Recent studies have suggested that cholinergic modulation is involved in neuroinflammatory cellular reactions including neurogenesis and gliosis, and in memory improvement. In this study, we administered a broad-spectrum cholinesterase inhibitor, rivastigmine (2 mg/kg/day, s...
November 28, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27910192/novel-tacrine-based-pyrano-3-4-5-6-pyrano-2-3-b-quinolinones-synthesis-and-cholinesterase-inhibitory-activity
#2
Roshanak Hariri, Zahra Afshar, Mohammad Mahdavi, Maliheh Safavi, Mina Saeedi, Zahra Najafi, Reyhaneh Sabourian, Elahe Karimpour-Razkenari, Najmeh Edraki, Farshad Homayouni Moghadam, Abbas Shafiee, Mahnaz Khanavi, Tahmineh Akbarzadeh
In order to develop effective anti-cholinesterase compounds, a novel series of pyrano[3',4':5,6]pyrano[2,3-b]quinolinones were designed, synthesized, and evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All derivatives showed very good AChE inhibitory (AChEI) activity (IC50  = 0.37-5.62 μM) compared with rivastigmine (IC50  = 11.07 μM). Among them, 11-amino-12-(2,3-dichlorophenyl)-3-methyl-7,8,9,10-tetrahydropyrano[3',4':5,6]pyrano[2,3-b]quinolin-1(12H)-one (6f) displayed the best inhibitory activity...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27899389/high-dose-rivastigmine-in-the-symptom-management-of-lewy-body-dementia
#3
Joseph Marwan Nour, Leonidas Chouliaras, Lilian Hickey
A man presented in late 2004 at the age of 65 with a decline in memory. He was diagnosed with Lewy body dementia and started on 3 mg rivastigmine a day, which made a marked clinical improvement. He lived with the illness for 10 years, over which time the dose of acetylcholinesterase inhibitors (ChEI) he took rose to two 9.5 mg rivastigmine patches and 7.5 mg donepezil, significantly above British National Formulary (BNF) limits. He demonstrated clear clinical response to ChEI and showed improvements in alertness and functioning...
November 29, 2016: BMJ Case Reports
https://www.readbyqxmd.com/read/27896785/prescription-patterns-of-medications-for-alzheimer-s-disease-in-japan-from-2010-to-2015-a-descriptive-pharmacy-claims-database-study
#4
Kimiko Kadohara, Izumi Sato, Yuko Doi, Masaru Arai, Yosuke Fujii, Toshiyuki Matsunaga, Koji Kawakami
INTRODUCTION: Although four kinds of Alzheimer's disease (AD) drugs are available at present there was only one drug until 2011 in Japan. This study aimed to elucidate prescription trends of these medications for AD in Japanese outpatients before and after the new drug releases in 2011. METHODS: This descriptive study of pharmacy claims databases analyzed outpatient prescription data from community pharmacies across Japan. The study patients were 20 years or older and first administered medications for AD (donepezil, memantine, rivastigmine, or galantamine) between January 2010 and September 2014...
November 28, 2016: Neurology and Therapy
https://www.readbyqxmd.com/read/27876467/a-review-on-tacrine-based-scaffolds-as-multi-target-drugs-mtdls-for-alzheimer-s-disease
#5
REVIEW
Bilqees Sameem, Mina Saeedi, Mohammad Mahdavi, Abbas Shafiee
Alzheimer's disease (AD) is a multifactorial neurological disorder among elderly people and combinatorial factors such as genetic, lifestyle, and environmental are involved in onset and disease progression. It has been demonstrated that loss of cholinergic transmission is one of the most significant causes of AD. One strategy currently being investigated for the development of new therapeutics relates to the enhancement of cholinergic system through several ways. At this juncture, anticholinesterase inhibitors have absorbed lots of attention and different marketed drugs such as donepezil, rivastigmine, tacrine, and galantamine have been developed...
October 28, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27865771/cholinergic-activation-affects-the-acute-and-chronic-antinociceptive-effects-of-morphine
#6
Kinga Gawel, Ewa Gibula-Bruzda, Marcin Dziedzic, Malgorzata Jenda-Wojtanowska, Marta Marszalek-Grabska, Jerzy Silberring, Jolanta H Kotlinska
Current studies indicate that the cholinergic and opioid systems interact to modulate pain. In the present work, we investigated the influence of the cholinesterase inhibitors, donepezil (0.5; 1 or 3mg/kg, i.p.) and rivastigmine (0.03; 0.5 or 1mg/kg, i.p.), on the acute antinociceptive effects of morphine (5mg/kg, i.p.) in the hot plate test in mice. Herein, both inhibitors were found to enhance and prolong the analgesic effects of morphine without affecting latencies themselves. In an extension of this work, we determined which cholinergic receptors subtype mediates the enhancement of analgesic effects of morphine, following inhibition of cholinesterases...
November 16, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27856236/design-synthesis-biological-evaluation-and-molecular-modeling-studies-of-chalcone-rivastigmine-hybrids-as-cholinesterase-inhibitors
#7
Ling Wang, Yu Wang, Yiguang Tian, Jinling Shang, Xiaoou Sun, Hongzhuan Chen, Hao Wang, Wen Tan
A series of novel chalcone-rivastigmine hybrids were designed, synthesized, and tested in vitro for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. Most of the target compounds showed hBChE selective activity in the micro- and submicromolar ranges. The most potent compound 3 exhibited comparable IC50 to the commercially available drug (rivastigmine). To better understand their structure activity relationships (SAR) and mechanisms of enzyme-inhibitor interactions, kinetic and molecular modeling studies including molecular docking and molecular dynamics (MD) simulations were carried out...
November 5, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27786552/use-of-antidementia-drugs-and-risk-of-pneumonia-in-older-persons-with-alzheimer-s-disease
#8
Pasi Lampela, Anna-Maija Tolppanen, Antti Tanskanen, Jari Tiihonen, Piia Lavikainen, Sirpa Hartikainen, Heidi Taipale
INTRODUCTION: Persons with Alzheimer's disease are at an increased risk of pneumonia, but the comparative risks during specific antidementia treatments are not known. We compared the risk of pneumonia in use of donepezil, rivastigmine (oral, transdermal), galantamine and memantine. PATIENTS AND METHODS: We used data from a nationwide cohort of community-dwelling individuals diagnosed with Alzheimer's disease during 2005-2011 in Finland, who initiated monotherapy with acetylcholinesterase inhibitor or memantine (n = 65481)...
October 27, 2016: Annals of Medicine
https://www.readbyqxmd.com/read/27785919/pharmacotherapies-for-parkinson-s-disease-symptoms-related-to-cholinergic-degeneration
#9
Santiago Perez-Lloret, María Cecilia Peralta, Francisco J Barrantes
Dopamine depletion is one of the most important features of Parkinson's Disease (PD). However, insufficient response to dopaminergic replacement therapy suggests the involvement of other neurotransmitter systems in the pathophysiology of PD. Cholinergic degeneration contributes to gait impairments, cognitive impairment, psychosis, and REM-sleep disturbances, among other symptoms. Areas covered: In this review, we explore the idea that enhancing cholinergic tone by pharmacological or neurosurgical procedures could be a first-line therapeutic strategy for the treatment of symptoms derived from cholinergic degeneration in PD...
November 7, 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27736684/discovery-of-novel-rivastigmine-hydroxycinnamic-acid-hybrids-as-multi-targeted-agents-for-alzheimer-s-disease
#10
Ziwei Chen, Maria Digiacomo, Yalin Tu, Qiong Gu, Shengnan Wang, Xiaohong Yang, Jiaqi Chu, Qiuhe Chen, Yifan Han, Jingkao Chen, Giulia Nesi, Simona Sestito, Marco Macchia, Simona Rapposelli, Rongbiao Pi
A series of rivastigmine-caffeic acid and rivastigmine-ferulic acid hybrids were designed, synthesized, and evaluated as multifunctional agents for Alzheimer's disease (AD) in vitro. The new compounds exerted antioxidant neuroprotective properties and good cholinesterases (ChE) inhibitory activities. Some of them also inhibited amyloid protein (Aβ) aggregation. In particular, compound 5 emerged as promising drug candidates endowed with neuroprotective potential, ChE inhibitory, Aβ self-aggregation inhibitory and copper chelation properties...
September 17, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27732893/two-cholinesterase-inhibitors-trigger-dissimilar-effects-on-behavior-and-body-weight-in-c57bl-6-mice-the-case-of-chlorpyrifos-and-rivastigmine
#11
Pia Basaure, Fiona Peris-Sampedro, Maria Cabré, Ingrid Reverte, Maria Teresa Colomina
Cholinesterases (ChE) are common targets of organophosphate (OP) pesticides and play a critical role in the pathology of some dementias. While chlorpyrifos (CPF) remains one of the most commonly used OPs in the world, numerous investigations have reported its neurotoxic potential and highlighted behavioral disturbances upon its administration. Rivastigmine currently serves to treat Alzheimer's disease, but it may induce cholinergic overstimulation in non-demented individuals. The present investigation aimed to compare the acute and delayed effects caused by both ChE inhibitors in adult C57BL/6 male mice...
October 11, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27721970/effectiveness-of-rivastigmine-on-positive-negative-and-cognitive-symptoms-of-schizophrenia-a-double-blind-clinical-trial
#12
Saeed Shoja Shafti, Abbas Azizi Khoei
BACKGROUND: Several lines of evidence suggest that the cholinergic system may be disrupted in schizophrenia and so this may contribute to the cognitive impairments of schizophrenic patients. Because such deficits do not respond to neuroleptic treatment, different approaches have been done by acetylcholinesterase inhibitors (AChEIs). The objective of the present assessment was to evaluate the safety and clinical effects of rivastigmine, as an adjunctive drug, on the clinical symptoms of schizophrenia...
October 2016: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/27697039/therapeutic-effects-of-rivastigmine-and-alfa-lipoic-acid-combination-in-the-charles-bonnet-syndrome-electroencephalography-correlates
#13
Lutfu Hanoglu, Sultan Yildiz, Burcu Polat, Sema Demirci, Ahmet Mithat Tavli, Nesrin Yilmaz, Burak Yulug
BACKGROUND: Charles Bonnet Syndrome (CBS) is a rare clinical condition which is characterized with complex hallucinations by visually impaired patients. The pathophysiology of this disorder remains largely unknown, and there is still no proven treatment for this disease. In our study, we aimed to investigate the neural activity through Electroencephalography (EEG) power and evaluate the effect of rivastigmine in combination with alpha-lipoic acid on hallucination in two CBS patients with diabetic retinopathy...
October 3, 2016: Current Clinical Pharmacology
https://www.readbyqxmd.com/read/27681702/effects-of-renal-impairment-on-steady-state-plasma-concentrations-of-rivastigmine-a-population-pharmacokinetic-analysis-of-capsule-and-patch-formulations-in-patients-with-alzheimer-s-disease
#14
Gilbert Lefèvre, Francesca Callegari, Sandro Gsteiger, Yuan Xiong
INTRODUCTION: The glomerular filtration rate (GFR), a measure of renal function, decreases by approximately 10 mL/min every 10 years after the age of 40 years, which could lead to the accumulation of drugs and/or renal toxicity. Pharmacokinetic studies of drugs excreted both renally and non-renally are desirable in patients with impaired renal function, defined by parameters including estimated GFR (eGFR) and creatinine clearance (CLCR). OBJECTIVE: We describe here a population pharmacokinetic analysis of the possible effects of renal impairment on steady-state plasma concentrations of rivastigmine and its metabolite NAP226-90 after rivastigmine patch (5 cm(2) [4...
September 28, 2016: Drugs & Aging
https://www.readbyqxmd.com/read/27660276/in-vitro-effects-of-cognitives-and-nootropics-on-mitochondrial-respiration-and-monoamine-oxidase-activity
#15
Namrata Singh, Jana Hroudová, Zdeněk Fišar
Impairment of mitochondrial metabolism, particularly the electron transport chain (ETC), as well as increased oxidative stress might play a significant role in pathogenesis of Alzheimer's disease (AD). Some effects of drugs used for symptomatic AD treatment may be related to their direct action on mitochondrial function. In vitro effects of pharmacologically different cognitives (galantamine, donepezil, rivastigmine, 7-MEOTA, memantine) and nootropic drugs (latrepirdine, piracetam) were investigated on selected mitochondrial parameters: activities of ETC complexes I, II + III, and IV, citrate synthase, monoamine oxidase (MAO), oxygen consumption rate, and hydrogen peroxide production of pig brain mitochondria...
September 23, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27639640/absolute-bioavailability-and-safety-of-a-novel-rivastigmine-nasal-spray-in-healthy-elderly-individuals
#16
Timothy M Morgan, Bob Soh
AIMS: To test the feasibility of a novel rivastigmine nasal spray as prospective treatment for dementia. METHODS: A single dose, crossover absolute bioavailability and safety study was conducted with rivastigmine intravenous solution (1 mg) and nasal spray (3.126 mg) in eight healthy elderly individuals, aged 58 to 75 years. RESULTS: The absolute bioavailability (F) of the nasal spray was significant at 0.62 (0.15) for F > 0 (p < 0...
September 18, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27627023/pharmacological-evidence-of-specific-acetylcholine-transport-in-rat-cerebral-cortex-and-other-brain-regions
#17
Ikunobu Muramatsu, Hatsumi Yoshiki, Junsuke Uwada, Takayoshi Masuoka, Kiyonao Sada, Takanobu Taniguchi, Matomo Nishio
Functional acetylcholine receptors (AChRs) were recently demonstrated to exist not only in the plasma membrane but also intracellularly in brain tissues. In order to activate intracellular AChRs, endogenous hydrophilic ACh must cross the plasma membrane. Here, we examined the pharmacological characteristics of this process, including whether it is mediated by active ACh uptake. When ACh esterase (AChE) was suppressed by diisopropylfluorophosphate, [(3) H]ACh was effectively taken up into segments of rat cerebral cortex and other brain regions, in contrast to peripheral tissues such as liver and kidney...
November 2016: Journal of Neurochemistry
https://www.readbyqxmd.com/read/27599816/-rivastigmine-and-parkinson-s-disease-without-dementia-impact-on-gait-stability-and-frequency-of-falling
#18
Kerstin Amadori
No abstract text is available yet for this article.
October 2016: Zeitschrift Für Gerontologie und Geriatrie
https://www.readbyqxmd.com/read/27597816/key-targets-for-multi-target-ligands-designed-to-combat-neurodegeneration
#19
REVIEW
Rona R Ramsay, Magdalena Majekova, Milagros Medina, Massimo Valoti
HIGHLIGHTS Compounds that interact with multiple targets but minimally with the cytochrome P450 system (CYP) address the many factors leading to neurodegeneration.Acetyl- and Butyryl-cholineEsterases (AChE, BChE) and Monoamine Oxidases A/B (MAO A, MAO B) are targets for Multi-Target Designed Ligands (MTDL).ASS234 is an irreversible inhibitor of MAO A >MAO B and has micromolar potency against the cholinesterases.ASS234 is a poor CYP substrate in human liver, yielding the depropargylated metabolite.SMe1EC2, a stobadine derivative, showed high radical scavenging property, in vitro and in vivo giving protection in head trauma and diabetic damage of endothelium...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27587069/the-citirivad-study-citicoline-plus-rivastigmine-in-elderly-patients-affected-with-dementia-study
#20
Alberto Castagna, Antonino Maria Cotroneo, Giovanni Ruotolo, Pietro Gareri
BACKGROUND: Acetylcholinesterase inhibitors (AchEIs), such as rivastigmine, coadministered with cholinergic precursors, such as citicoline, could be effective in Alzheimer's disease (AD) and in mixed dementia (MD), because they are able to increase the intrasynaptic levels of acetylcholine more than the single drugs given alone. OBJECTIVE: The aim of the present study was to show the effectiveness of oral citicoline plus rivastigmine in patients with AD and MD. METHODS: The CITIRIVAD study was a retrospective case-control study on 174 consecutive outpatients aged ≥65 years, affected with AD or MD, mean age 81...
September 1, 2016: Clinical Drug Investigation
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