keyword
MENU ▼
Read by QxMD icon Read
search

Donepezil

keyword
https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#1
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28205135/apium-graveolens-extract-influences-mood-and-cognition-in-healthy-mice
#2
Phetcharat Boonruamkaew, Wanida Sukketsiri, Pharkphoom Panichayupakaranant, Wijittra Kaewnam, Supita Tanasawet, Varomyalin Tipmanee, Pilaiwanwadee Hutamekalin, Pennapa Chonpathompikunlert
Apium graveolens is a food flavoring which possesses various health promoting effects. This study investigates the effect of a sub-acute administration of A. graveolens on cognition and anti-depression behaviors via antioxidant and related neurotransmitter systems in mice brains. Cognition and depression was assessed by various models of behavior. The antioxidant system of glutathione peroxidase (GPx), % inhibition of superoxide anion (O2(-)), and lipid peroxidation were studied. In addition, neurochemical parameters including acetylcholinesterase (AChE) and monoamine oxidase-type A (MAO-A) were also evaluated...
February 15, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28198801/inhibitory-effects-of-cholinesterase-inhibitor-donepezil-on-the-kv1-5-potassium-channel
#3
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
https://www.readbyqxmd.com/read/28188762/effects-of-the-5-ht6-receptor-antagonist-idalopirdine-on-extracellular-levels-of-monoamines-glutamate-and-acetylcholine-in-the-rat-medial-prefrontal-cortex
#4
Arne Mørk, Rasmus Vinther Russell, Inge E M de Jong, Gennady Smagin
Idalopirdine (Lu AE58054) is a high affinity and selective antagonist for the human serotonin 5-HT6 receptor (Ki 0.83nM) in phase III development for mild-to-moderate Alzheimer's disease as an adjunct therapy to acetylcholinesterase inhibitors (AChEIs). We have studied the effects of idalopirdine on extracellular levels of monoamines, glutamate and acetylcholine in the medial prefrontal cortex (mPFC) of freely-moving rats using microdialysis. Idalopirdine (10mg/kg p.o.) increased extracellular levels of dopamine, noradrenaline and glutamate in the mPFC and showed a trend to increase serotonin levels...
February 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28177980/alzheimer-s-disease-in-the-zebrafish-where-can-we-take-it
#5
Erika M Caramillo, David J Echevarria
With the ever-growing geriatric population, research on brain diseases such as dementia is more imperative now than ever. The most prevalent of all dementias is Alzheimer's disease, a progressive neurodegenerative disease that presents with deficits in memory, cognition, motor skills, and a general decline in the quality of life. The social and economic burden associated with Alzheimer's disease is tremendous and is projected to grow even greater over the coming years. There is a specific need to elucidate and improve the treatments available, not only to alleviate the symptoms related to dementias such as Alzheimer's but also to prevent the formation of the disease...
February 7, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28176625/protective-effects-of-huang-lian-jie-du-tang-on-a%C3%AE-25-35-induced-memory-deficits-and-oxidative-stress-in-male-rats
#6
Wenbin Wu, Shuling Xie, Bin Li, Kun Yang, Xuehui Liu, Baiyang Li
BACKGROUND: Alzheimer's disease is a neurodegenerative disorder characterized by progressive cognitive deterioration and is the most common cause of dementia. Extracellular β-amyloid deposit in senile plaques is the most characteristic pathological hallmark. β-amyloid (Aβ) accumulation is associated with neurodegeneration and involved in memory impairment associated with Alzheimer's disease. It can also induce intracellular reactive oxygen species (ROS) production, which results in neurodegeneration and immune response...
February 6, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/28174534/behavioral-changes-and-hippocampus-glucose-metabolism-in-app-ps1-transgenic-mice-via-electro-acupuncture-at-governor-vessel-acupoints
#7
Jin Cao, Yinshan Tang, Yujie Li, Kai Gao, Xudong Shi, Zhigang Li
Objective: Investigating the effects of electro-acupuncture (EA) treatment on mice with Alzheimer's disease (AD), using Morris water maze (MWM) for spatial learning and memory behavior tests combined with micro-positron emission tomography (micro-PET) imaging for glucose metabolism in hippocampus. Methods: Thirty seven-month-old APP/PS1 mice were randomly divided into AD Model group (AD group), medicine group (M group) and EA group, C57BL/6 mice were used for Normal control group (N group), n = 10 in each group...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28157100/efficacy-and-safety-of-donepezil-in-chinese-patients-with-severe-alzheimer-s-disease-a-randomized-controlled-trial
#8
Jianping Jia, Cuibai Wei, Longfei Jia, Yi Tang, Junhua Liang, Aihong Zhou, Fangyu Li, Lu Shi, Rachelle S Doody
BACKGROUND: Donepezil has been used worldwide for the treatment of severe Alzheimer's disease (AD). Whether it is also appropriate for severe AD in Chinese patients remains unknown. OBJECTIVE: To determine whether donepezil is effective and tolerable for Chinese patients with severe AD. METHODS: The present study was a 24-week, multicenter, double-blind, randomized, placebo-controlled, parallel-group study conducted at 38 investigational hospitals in China...
February 1, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28157092/multifunctional-compound-ad-35-improves-cognitive-impairment-and-attenuates-the-production-of-tnf-%C3%AE-and-il-1%C3%AE-in-an-a%C3%AE-25-35-induced-rat-model-of-alzheimer-s-disease
#9
Lin Li, Shaofeng Xu, Lifei Liu, Rentian Feng, Yongxiang Gong, Xuyang Zhao, Jiang Li, Jie Cai, Nan Feng, Ling Wang, Xiaoliang Wang, Ying Peng
The dyshomeostasis of transition metal ions, accumulation of amyloid-β (Aβ) senile plaques and neuroinflammatory response found in the brain of patients with Alzheimer's disease (AD) have been suggested to be involved in AD pathogenesis. Novel compounds capable of targeting metal-Aβ species and neuroinflammation would be valuable. AD-35 is such a patented small-molecule compound derived from innovative modification of the chemical structure of donepezil. This compound could moderately inhibit acetylcholinesterase and metal-induced Aβ aggregation in vitro and showed disassembly of Aβ aggregates...
February 1, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28154306/taste-masking-effect-of-chlorogenic-acid-cga-on-bitter-drugs-evaluated-by-taste-sensor-and-surface-plasmon-resonance-on-the-basis-of-cga-drug-interactions
#10
Sayuko Shiraishi, Tamami Haraguchi, Saki Nakamura, Dahong Li, Honami Kojima, Miyako Yoshida, Takahiro Uchida
The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RBM≈ETD...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28153340/microwave-assisted-synthesis-of-novel-hybrid-tacrine-sulfonamide-derivatives-and-investigation-of-their-antioxidant-and-anticholinesterase-activities
#11
Ramazan Ulus, Belma Zengin Kurt, Isil Gazioğlu, Muharrem Kaya
A novel series of tacrine derivatives containing sulfonamide group were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. The result showed that all the synthesized tacrine-sulfonamides (VIIIa-o) exhibited inhibitory activity on both cholinesterases. VIIIg showed the highest inhibitory activity on AChE IC50=0.009μM. This value is 220-fold greater than that of galantamine (IC50=2.054μM) and 6-fold greater than tacrine (IC50=0.055μM). VIIIf displayed the strongest inhibition of BuChE (IC50=2...
January 9, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28138912/tolerability-of-cholinesterase-inhibitors-a-population-based-study-of-persistence-adherence-and-switching
#12
Anat Fisher, Greg Carney, Ken Bassett, Colin R Dormuth
BACKGROUND: Cholinesterase inhibitors (ChEIs) are prescribed to dementia patients despite their poor tolerance. Low tolerability potentially reduces persistence and adherence, while inducing switching between medications. Comparisons of these utilization measures contribute to knowledge of the relative tolerability of these medications. AIM: The aim was to compare persistence, adherence, and switching between donepezil, galantamine, oral rivastigmine, and rivastigmine patch...
January 30, 2017: Drugs & Aging
https://www.readbyqxmd.com/read/28138837/donepezil-plus-solifenacin-cpc-201-treatment-for-alzheimer-s-disease
#13
Thomas N Chase, Martin R Farlow, Kathleen Clarence-Smith
Available cholinergic drugs for treating Alzheimer's disease (AD) provide modest symptomatic benefit. We hypothesized that co-administration of a peripheral anticholinergic to reduce dose-limiting adverse effects (AEs) would enable the safe/tolerable use of higher cholinesterase inhibitor doses and thus improve their antidementia efficacy. A modified single-blind, ascending-dose, phase IIa study of donepezil plus solifenacin (CPC-201) lasting 26 weeks was conducted in 41 patients with probable AD of moderate severity...
January 30, 2017: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/28133526/2-2-4-benzoylpiperazin-1-yl-ethyl-isoindoline-1-3-dione-derivatives-synthesis-docking-and-acetylcholinesterase-inhibitory-evaluation-as-anti-alzheimer-agents
#14
Ahmad Mohammadi-Farani, Nasibeh Abdi, Alireza Moradi, Alireza Aliabadi
OBJECTIVES: Alzheimer's disease (AD) as progressive cognitive decline and the most common form of dementia is due to degeneration of the cholinergic neurons in the brain. Therefore, administration of the acetylcholinesterase (AChE) inhibitors such as donepezil is the first choice for treatment of the AD. In the present study, we focused on the synthesis and anti-cholinesterase evaluation of new donepezil like analogs. MATERIALS AND METHODS: A new series of phthalimide derivatives (compounds 4a-4j) were synthesized via Gabriel protocol and subsequently amidation reaction was performed using various benzoic acid derivatives...
January 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28126439/design-synthesis-and-evaluation-of-some-n-methylenebenzenamine-derivatives-as-selective-acetylcholinesterase-ache-inhibitor-and-antioxidant-to-enhance-learning-and-memory
#15
Sushant K Shrivastava, Pavan Srivastava, T V R Upendra, Prabhash Nath Tripathi, Saurabh K Sinha
Series of some 3,5-dimethoxy-N-methylenebenzenamine and 4-(methyleneamino)benzoic acid derivatives comprising of N-methylenebenzenamine nucleus were designed, synthesized, characterized, and assessed for their acetylcholinesterase (AChE), butyrylcholinesterase (BChE) inhibitory, and antioxidant activity thereby improving learning and memory in rats. The IC50 values of all the compound along with standard were determined on AChE and BChE enzyme. The free radical scavenging activity was also assessed by in vitro DPPH (2,2-diphenyl-1-picryl-hydrazyl) and hydrogen peroxide radical scavenging assay...
January 11, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28125507/behavioural-effects-of-novel-multitarget-anticholinesterasic-derivatives-in-alzheimer-s-disease
#16
Lydia Giménez-Llort, Miriam Ratia, Belén Pérez, Pelayo Camps, Diego Muñoz-Torrero, Albert Badia, Maria V Clos
The current pharmacological approach to Alzheimer's disease (AD) treatment, mostly based on acetylcholinesterase inhibitors (AChEIs), is being revisited, especially in terms of the temporal frames and the potential benefits of their noncanonic actions, raising the question of whether inhibitors of AChE might also act in a disease-modifying manner. Besides, in the last decades, the pharmacophoric moieties of known AChEIs have been covalently linked to other pharmacophores in the pursuit of multitarget hybrid molecules that are expected to induce long-lasting amelioration of impaired neurotransmission and clinical symptoms but also to exert disease-modifying effects...
January 25, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28123400/six-psychotropics-for-pre-symptomatic-early-alzheimer-s-mci-parkinson-s-and-huntington-s-disease-modification
#17
REVIEW
Edward C Lauterbach
The quest for neuroprotective drugs to slow the progression of neurodegenerative diseases (NDDs), including Alzheimer's disease (AD), Parkinson's disease (PD), and Huntington's disease (HD), has been largely unrewarding. Preclinical evidence suggests that repurposing quetiapine, lithium, valproate, fluoxetine, donepezil, and memantine for early and pre-symptomatic disease-modification in NDDs may be promising and can spare regulatory barriers. The literature of these psychotropics in early stage and pre-symptomatic AD, PD, and HD is reviewed and propitious findings follow...
November 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/28123152/the-anti-dementia-effects-of-donepezil-involve-mir-206-3p-in-the-hippocampus-and-cortex
#18
Cheng-Niu Wang, Ying-Jie Wang, Hao Wang, Lu Song, Yu Chen, Jin-Liang Wang, Ying Ye, Bo Jiang
Alzheimer's disease (AD) is a most serious age-related neurodegenerative disorder accompanied with significant memory impairments in this world. Recently, microRNAs have been reported to be invlolved in the pathophysiology of AD. Previous studies have shown that miR-206 is implicated in the pathogenesis of AD via suppressing the expression of BDNF in the brain. Here, we examined the miR-206-3p and miR-206-5p expression in the hippocampus and cortex of APP/PS1 transgenic mice treated with donepezil, a drug approved for treating AD in clinic...
January 25, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28120208/huannao-yicong-formula-regulates-%C3%AE-secretase-activity-through-aph-1-and-pen-2-gene-ragulation-pathways-in-hippocampus-of-app-ps1-double-transgenic-mice
#19
Zhi-Yong Wang, Jian-Gang Liu, Yun Wei, Mei-Xia Liu, Qi Wang, Lin Liang, Hui-Min Yang, Hao Li
OBJECTIVE: To observe the effects of Huannao Yicong Formula (, HYF) on learning and memory and it's regulating effect on γ-secretase related anterior pharynx defective 1 (APH-1), presenilin enhancer-2 (PEN-2) signaling pathway, so as to discuss and further clarify the mechanism of HYF on Alzheimer's disease. METHODS: Sixty APP/PS1 transgenic mice, randomly allocated into 4 groups, the model group, the donepezil group (0.65 mg/kg), HYF low-dose group (HYF-L, 5.46 g/kg) and HYF high-dose group (HYF-H, 10...
January 24, 2017: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/28104598/pisa-syndrome-due-to-donepezil-pharmacokinetic-interactions-to-blame
#20
David Pollock, Emma Cunningham, Bernadette McGuinness, Anthony Peter Passmore
We report a case of Pisa syndrome (PS) due to the acetylcholinesterase inhibitor donepezil which may have been precipitated by pharmacokinetic interactions with commonly used medications. PS is defined as a reversible lateral bending of the trunk with a tendency to lean to one side. This is a rare but very distressing complication with this commonly used medication which was not initially recognised, leading to increasing disability for the patient and significant carer stress. Cessation of donepezil and modulation of potential interacting medications resulted in complete resolution...
January 18, 2017: Age and Ageing
keyword
keyword
17107
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"