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https://www.readbyqxmd.com/read/28315270/sigma-1-receptor-agonists-and-their-clinical-implications-in-neuropsychiatric-disorders
#1
Yakup Albayrak, Kenji Hashimoto
Accumulating evidence suggests that sigma-1 receptors play a role in the pathophysiology of neuropsychiatric diseases, as well as in the mechanisms of some selective serotonin reuptake inhibitors (SSRIs). Among the SSRIs, the order of affinity for sigma-1 receptors is as follows: fluvoxamine > sertraline > fluoxetine > escitalopram > citalopram > paroxetine. Some SSRIs (e.g., fluvoxamine, fluoxetine and escitalopram) and other drugs (donepezil , ifenprodil , dehydroepiandeterone (DHEA)) potentiate nerve-growth factor (NGF)-induced neurite outgrowth in PC12 cells, and these effects could be antagonized by the selective sigma-1 receptor antagonist NE-100...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28295141/adherence-and-tolerability-of-alzheimer-s-disease-medications-a-pragmatic-randomized-trial
#2
Noll L Campbell, Anthony J Perkins, Sujuan Gao, Todd C Skaar, Lang Li, Hugh C Hendrie, Nicole Fowler, Christopher M Callahan, Malaz A Boustani
BACKGROUND/OBJECTIVES: Post-marketing comparative trials describe medication use patterns in diverse, real-world populations. Our objective was to determine if differences in rates of adherence and tolerability exist among new users to acetylcholinesterase inhibitors (AChEI's). DESIGN: Pragmatic randomized, open label comparative trial of AChEI's currently available in the United States. SETTING: Four memory care practices within four healthcare systems in the greater Indianapolis area...
March 14, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28287355/donepezil-an-acetylcholinesterase-inhibitor-can-attenuate-gabapentinoid-induced-somnolence-in-patients-with-neuropathic-pain-a-retrospective-chart-review
#3
Takamichi Kogure, Masahiko Sumitani, Kiyoshi Ikegami, Hiroaki Abe, Jun Hozumi, Reo Inoue, Kazuo Kawahara, Yoshitsugu Yamada
Donepezil, an oral acetylcholinesterase inhibitor, is used to treat Alzheimer's disease and reportedly attenuates opioid-induced sedation in patients with cancer pain. Neuropathic pain is often treated with gabapentinoids (pregabalin, gabapentin), but gabapentinoid-induced somnolence sometimes prevents patients from using these agents. We conducted a retrospective chart review of patients with neuropathic pain to examine whether donepezil is useful for gabapentinoid-induced somnolence. We investigated pain severity in 13 patients before and after taking gabapentinoids and donepezil, the degree of gabapentinoid-induced somnolence before and after starting donepezil, and gabapentinoid dose escalation after taking donepezil...
March 2017: Journal of Pain & Palliative Care Pharmacotherapy
https://www.readbyqxmd.com/read/28286520/acetylcholinesterase-inhibitors-assay-using-colorimetric-ph-sensitive-strips-and-image-analysis-by-a-smartphone
#4
Adam Kostelnik, Alexander Cegan, Miroslav Pohanka
Smartphones are widely spread and their usage does not require any trained personnel. Recently, smartphones were successfully used in analytical chemistry as a simple detection tool in some applications. This paper focuses on immobilization of acetylcholinesterase (AChE) onto commercially available pH strips with stabilization in the gelatin membrane. AChE degrades acetylcholine into choline and acetic acid which causes color change of acid-base indicator. Smartphone served as a tool for measurement of indicator color change from red to orange while inhibitors blocked this process...
2017: International Journal of Analytical Chemistry
https://www.readbyqxmd.com/read/28282613/design-synthesis-and-evaluation-of-novel-feruloyl-donepezil-hybrids-as-potential-multitarget-drugs-for-the-treatment-of-alzheimer-s-disease
#5
Kris Simone T Dias, Cynthia T de Paula, Thiago Dos Santos, Isis N O Souza, Marina S Boni, Marcos J R Guimarães, Fernanda M R da Silva, Newton G Castro, Gilda A Neves, Clarice C Veloso, Márcio M Coelho, Ivo Souza F de Melo, Fabiana C V Giusti, Alexandre Giusti-Paiva, Marcelo L da Silva, Laurent E Dardenne, Isabella A Guedes, Letizia Pruccoli, Fabiana Morroni, Andrea Tarozzi, Claudio Viegas
A novel series of feruloyl-donepezil hybrid compounds were designed, synthesized and evaluated as multitarget drug candidates for the treatment of Alzheimer's Disease (AD). In vitro results revealed potent acetylcholinesterase (AChE) inhibitory activity for some of these compounds and all of them showed moderate antioxidant properties. Compounds 12a, 12b and 12c were the most potent AChE inhibitors, highlighting 12a with IC50 = 0.46 μM. In addition, these three most promising compounds exhibited significant in vivo anti-inflammatory activity in the mice paw edema, pleurisy and formalin-induced hyperalgesy models, in vitro metal chelator activity for Cu(2+) and Fe(2+), and neuroprotection of human neuronal cells against oxidative damage...
February 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28276131/different-clinical-effect-of-four-antidementia-drugs-for-alzheimer-s-disease-patients-depending-on-white-matter-severity
#6
Yusuke Fukui, Nozomi Hishikawa, Jin Ichinose, Kota Sato, Yumiko Nakano, Ryuta Morihara, Yasuyuki Ohta, Toru Yamashita, Koji Abe
AIM: To examine the clinical effect of four antidementia drugs (donepezil, galantamine, rivastigmine and memantine) in Alzheimer's disease patients who were divided into subgroups based on their periventricular hyperintensity (PVH) severity. METHODS: A total of 551 Alzheimer's disease patients (201 men and 350 women) were divided into four subgroups based on their PVH severity (0-III). They received monotherapy for 12 months. We compared the clinical effects at the baseline, and at 3, 6 and 12 months after initiation...
March 9, 2017: Geriatrics & Gerontology International
https://www.readbyqxmd.com/read/28275781/aqueous-extracts-from-asparagus-stems-prevent-memory-impairments-in-scopolamine-treated-mice
#7
Zifang Sui, Ce Qi, Yunxiang Huang, Shufeng Ma, Xinguo Wang, Guowei Le, Jin Sun
Aqueous extracts from Asparagus officinalis L. stems (AEAS) are rich in polysaccharides, gamma-amino butyric acid (GABA), and steroidal saponin. This study was designed to investigate the effects of AEAS on learning, memory, and acetylcholinesterase-related activity in a scopolamine-induced model of amnesia. Sixty ICR mice were randomly divided into 6 groups (n = 10) including the control group (CT), scopolamine group (SC), donepezil group (DON), low, medium, and high dose groups of AEAS (LS, MS, HS; 1.6 mL kg(-1), 8 mL kg(-1), 16 mL kg(-1))...
March 9, 2017: Food & Function
https://www.readbyqxmd.com/read/28272324/dl0410-ameliorates-memory-and-cognitive-impairments-induced-by-scopolamine-via-increasing-cholinergic-neurotransmission-in-mice
#8
Wenwen Lian, Jiansong Fang, Lvjie Xu, Wei Zhou, De Kang, Wandi Xiong, Hao Jia, Ai-Lin Liu, Guan-Hua Du
Deficiency of the cholinergic system is thought to play a vital role in cognitive impairment of dementia. DL0410 was discovered as a dual inhibitor of acetylcholinesterase (AChE) and butyrylcholinestease (BuChE), with potent efficiency in in-vitro experiments, but its in vivo effect on the cholinergic model has not been evaluated, and its action mechanism has also not been illustrated. In the present study, the capability of DL0410 in ameliorating the amnesia induced by scopolamine was investigated, and its effect on the cholinergic system in the hippocampus and its binding mode in the active site of AChE was also explored...
March 6, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28270636/-adult-onset-neuronal-intranuclear-inclusion-disease-in-two-female-siblings
#9
Takeshi Yoshimoto, Kazuhiro Takamatsu, Takashi Kurashige, Jun Sone, Gen Sobue, Masaru Kuriyama
Neuronal intranuclear inclusion disease (NIID) in two adult siblings (both women, aged 76 and 68 years) is reported on here. The elder sister had a resting tremor and bradykinesia at age 66 years, and treatment with L-DOPA was initiated(L-3, 4-dihydroxyphenylalanine). Three years later, she showed a frozen gait that was associated with the medication wearing off. The clinical manifestations did not improve with the administration of antiparkinson drugs. Six years later, she showed impaired cognitive functions, which had occured gradually, and she began to take donepezil...
March 2017: Brain and Nerve, Shinkei Kenkyū No Shinpo
https://www.readbyqxmd.com/read/28260511/clinically-relevant-drug-interactions-with-anti-alzheimer-s-drugs
#10
Filippo Caraci, Janet Sultana, Filippo Drago, Edoardo Spina
The aging world population had led to an increase in the prevalence of Alzheimer's disease (AD). The drugs used to slow down the onset of AD, galantamine, donepezil, rivastigmine and memantine, are generally well-tolerated. However, drug interactions between these drugs and other drugs are an important aspect of patient safety that should be borne in mind, particularly given the high burden of polypharmacy in the elderly. The aim of this review is to provide an updated review of clinically significant drug-drug interactions concerning drugs approved for AD...
March 3, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28259857/auditory-training-changes-temporal-lobe-connectivity-in-wernicke-s-aphasia-a-randomised-trial
#11
Zoe Vj Woodhead, Jennifer Crinion, Sundeep Teki, Will Penny, Cathy J Price, Alexander P Leff
INTRODUCTION: Aphasia is one of the most disabling sequelae after stroke, occurring in 25%-40% of stroke survivors. However, there remains a lack of good evidence for the efficacy or mechanisms of speech comprehension rehabilitation. TRIAL DESIGN: This within-subjects trial tested two concurrent interventions in 20 patients with chronic aphasia with speech comprehension impairment following left hemisphere stroke: (1) phonological training using 'Earobics' software and (2) a pharmacological intervention using donepezil, an acetylcholinesterase inhibitor...
March 4, 2017: Journal of Neurology, Neurosurgery, and Psychiatry
https://www.readbyqxmd.com/read/28259598/tropisetron-sensitizes-%C3%AE-7-containing-nicotinic-receptors-to-low-levels-of-acetylcholine-in%C3%A2-vitro-and-improves-memory-related-task-performance-in-young-and-aged-animals
#12
Patrick M Callahan, Daniel Bertrand, Sonia Bertrand, Marc R Plagenhoef, Alvin V Terry
Tropisetron, a 5-HT3 receptor antagonist commonly prescribed for chemotherapy-induced nausea and vomiting also exhibits high affinity, partial agonist activity at α7 nicotinic acetylcholine receptors (α7 nAChRs). α7 nAChRs are considered viable therapeutic targets for neuropsychiatric disorders such as Alzheimer's disease (AD). Here we further explored the nAChR pharmacology of tropisetron to include the homomeric α7 nAChR and recently characterized heteromeric α7β2 nAChR (1:10 ratio) and we evaluated its cognitive effects in young and aged animals...
March 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28245707/standardized-extract-of-lactuca-sativa-linn-and-its-fractions-abrogates-scopolamine-induced-amnesia-in-mice-a-possible-cholinergic-and-antioxidant-mechanism
#13
Jai Malik, Jagpreet Kaur, Sunayna Choudhary
OBJECTIVES: The present study was designed to evaluate the efficacy of Lactuca sativa (LS) Linn. (Asteraceae) against scopolamine- induced amnesia and to validate its traditional claim as memory enhancer. METHODS: Ethanol extract of fresh LS leaves (LSEE), standardized on the basis of quercetin content, was successively partitioned using various solvents viz., hexane, ethyl acetate, and n-butanol in increasing order of polarity. LSEE (50, 100, and 200 mg/kg) and its various fractions (at a dose equivalent to dose of LSEE exhibiting maximum activity), administered orally for 14 days, were evaluated for their memory enhancing effect against scopolamine-induced (1 mg/kg, i...
February 28, 2017: Nutritional Neuroscience
https://www.readbyqxmd.com/read/28243607/treatment-with-sildenafil-and-donepezil-improves-angiogenesis-in-experimentally-induced-critical-limb-ischemia
#14
Ioana M Constantinescu, Pompei Bolfa, Dan Constantinescu, Aurel I Mironiuc, Claudia D Gherman
Objectives. In this study, we aimed to demonstrate the role of sildenafil (an antagonist of phosphodiesterase type 5 (PDE-5)) and donepezil (a specific and reversible inhibitor of acetylcholinesterase (Ach)) in increasing ischemia-induced angiogenesis. Method. Critical limb ischemia was induced by ligation of the common femoral artery followed by ligation of the common iliac artery. The operated animals were divided into 3 groups: receiving sildenafil, receiving donepezil, and surgery alone; the contralateral lower limb was used as a negative control...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28242552/enzymatic-and-solid-phase-synthesis-of-new-donepezil-based-l-and-d-glutamic-acid-derivatives-and-their-pharmacological-evaluation-in-models-related-to-alzheimer-s-disease-and-cerebral-ischemia
#15
Leticia Monjas, Mariana P Arce, Rafael León, Javier Egea, Concepción Pérez, Mercedes Villarroya, Manuela G López, Carmen Gil, Santiago Conde, María Isabel Rodríguez-Franco
Previously, we have described N-Bz-L-Glu[NH-2-(1-benzylpiperidin-4-yl)ethyl]-O-nHex (IQM9.21, L-1) as an interesting multifunctional neuroprotective compound for the potential treatment of neurodegenerative diseases. Here, we describe new derivatives and different synthetic routes, such as chemoenzymatic and solid-phase synthesis, aiming to improve the previously described route in solution. The lipase-catalysed amidation of L- and D-Glu diesters with N-benzyl-4-(2-aminoethyl)piperidine has been studied, using Candida antarctica and Mucor miehei lipases...
April 21, 2017: European Journal of Medicinal Chemistry
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
#16
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/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
#17
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
#18
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
#19
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
#20
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 8, 2017: European Journal of Pharmacology
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