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https://www.readbyqxmd.com/read/28922500/total-synthesis-of-the-diglycosidic-tetramic-acid-ancorinoside-a
#1
Markus Petermichl, Rainer Schobert
Ancorinoside A, a metabolite of a sponge Ancorina sp., was prepared in 18 steps as the first derivative of this class of glycosylated 3-acyltetramic acids. It features a β-D-glucopyranosyl-(1→4)-β-D-galacturonic acid linked to a D-aspartic acid derived tetramic acid via a 3-docosanoyl spacer. The diglycoside was built up by connecting the protected monosaccharides D-galactose and D-glucose via a thioglycoside glycosylation. Attachment of the spacer by a subsequent Schmidt glycosylation of this diglycoside, TEMPO oxidation to the uronic acid, functionalisation of the spacer terminus with an N-(β-ketoacyl)aspartate, and a final Dieckmann cyclisation of the latter were the key steps leading to ancorinoside A...
September 18, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28922421/effects-of-acute-administration-of-donepezil-or-memantine-on-sleep-deprivation-induced-spatial-memory-deficit-in-young-and-aged-non-human-primate-grey-mouse-lemurs-microcebus-murinus
#2
Anisur Rahman, Yves Lamberty, Esther Schenker, Massimo Cella, Solène Languille, Régis Bordet, Jill Richardson, Fabien Pifferi, Fabienne Aujard
The development of novel therapeutics to prevent cognitive decline of Alzheimer's disease (AD) is facing paramount difficulties since the translational efficacy of rodent models did not resulted in better clinical results. Currently approved treatments, including the acetylcholinesterase inhibitor donepezil (DON) and the N-methyl-D-aspartate antagonist memantine (MEM) provide marginal therapeutic benefits to AD patients. There is an urgent need to develop a predictive animal model that is phylogenetically proximal to humans to achieve better translation...
2017: PloS One
https://www.readbyqxmd.com/read/28921744/cholinergic-basal-forebrain-structures-are-not-essential-for-mediation-of-the-arousing-action-of-glutamate
#3
Zoltán Lelkes, Shamsiiat Abdurakhmanova, Tarja Porkka-Heiskanen
The cholinergic basal forebrain contributes to cortical activation and receives rich innervations from the ascending activating system. It is involved in the mediation of the arousing actions of noradrenaline and histamine. Glutamatergic stimulation in the basal forebrain results in cortical acetylcholine release and suppression of sleep. However, it is not known to what extent the cholinergic versus non-cholinergic basal forebrain projection neurones contribute to the arousing action of glutamate. To clarify this question, we administered N-methyl-D-aspartate (NMDA), a glutamate agonist, into the basal forebrain in intact rats and after destruction of the cholinergic cells in the basal forebrain with 192 immunoglobulin (Ig)G-saporin...
September 18, 2017: Journal of Sleep Research
https://www.readbyqxmd.com/read/28920570/brain-relevant-antibodies-in-first-episode-psychosis-a-matched-case-control-study
#4
Fiona Gaughran, John Lally, Katherine Beck, Ruaidhri McCormack, Poonam Gardner-Sood, Ester Coutinho, Leslie Jacobson, Bethan Lang, Ricardo Sainz-Fuertes, Evangelos Papanastasiou, Marta Di Forti, Tim Nicholson, Angela Vincent, Robin M Murray
BACKGROUND: There has been much recent excitement about the possibility that some cases of psychosis may be wholly due to brain-reactive antibodies, with antibodies to N-methyl-D-aspartate receptor (NMDAR) and the voltage-gated potassium channel (VGKC)-complex reported in a few patients with first-episode psychosis (FEP). METHODS: Participants were recruited from psychiatric services in South London, UK, from 2009 to 2011 as part of the Genetics and Psychosis study...
September 18, 2017: Psychological Medicine
https://www.readbyqxmd.com/read/28919538/roles-of-n-methyl-d-aspartate-receptors-during-the-sensory-stimulation-evoked-field-potential-responses-in-mouse-cerebellar-cortical-molecular-layer
#5
Yin-Hua Xu, Guang-Jian Zhang, Jing-Tong Zhao, Chun-Ping Chu, Yu-Zi Li, De-Lai Qiu
The functions of N-methyl-d-aspartate receptors (NMDARs) in cerebellar cortex have been widely studied under in vitro condition, but their roles during the sensory stimulation-evoked responses in the cerebellar cortical molecular layer in living animals are currently unclear. We here investigated the roles of NMDARs during the air-puff stimulation on ipsilateral whisker pad-evoked field potential responses in cerebellar cortical molecular layer in urethane-anesthetized mice by electrophysiological recording and pharmacological methods...
September 14, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28918258/olfactory-function-in-an-excitotoxic-model-for-secondary-neuronal-degeneration-role-of-dopaminergic-interneurons
#6
Concepció Marin, Sara Laxe, Cristobal Langdon, Joan Berenguer, Eduardo Lehrer, Franklin Mariño-Sánchez, Isam Alobid, Montserrat Bernabeu, Joaquim Mullol
Secondary neuronal degeneration (SND) occurring in Traumatic brain injury (TBI) consists in downstream destructive events affecting cells that were not or only marginally affected by the initial wound, further increasing the effects of the primary injury. Glutamate excitotoxicity is hypothesized to play an important role in SND. TBI is a common cause of olfactory dysfunction that may be spontaneous and partially recovered. The role of the glutamate excitotoxicity in the TBI-induced olfactory dysfunction is still unknown...
September 13, 2017: Neuroscience
https://www.readbyqxmd.com/read/28917837/memantine-inhibits-%C3%AE-amyloid-aggregation-and-disassembles-preformed-%C3%AE-amyloid-aggregates
#7
Kaori Ito, Mitsuhiro Makino, Keiko Okado, Taisuke Tomita
Memantine, an uncompetitive glutamatergic N-methyl-d-aspartate (NMDA) receptor antagonist, is widely used as a medication for the treatment of Alzheimer's disease (AD). We previously reported that chronic treatment of AD with memantine reduces the amount of insoluble β-amyloid (Aβ) and soluble Aβ oligomers in animal models of AD. The mechanisms by which memantine reduces Aβ levels in the brain were evaluated by determining the effect of memantine on Aβ aggregation using thioflavin T and transmission electron microscopy...
September 13, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28917389/alternative-treatment-strategies-for-catatonia-a-systematic-review
#8
REVIEW
Scott R Beach, Federico Gomez-Bernal, Jeff C Huffman, Gregory L Fricchione
BACKGROUND: Catatonia is a commonly encountered syndrome, affecting 10-20% of various psychiatric populations and carrying significant medical co-morbidities. However, there are few established alternative treatment strategies when benzodiazepines are ineffective and electroconvulsive therapy is unavailable. OBJECTIVE: The authors systematically review evidence for alternative treatment strategies for catatonia using Preferred Reporting Items for Systematic reviews and Meta-Analyses (PRISMA) guidelines...
September 2017: General Hospital Psychiatry
https://www.readbyqxmd.com/read/28916251/mk-801-but-not-naloxone-attenuates-high-dose-dextromethorphan-induced-convulsive-behavior-possible-involvement-of-the-glun2b-receptor
#9
Hai-Quyen Tran, Yoon Hee Chung, Eun-Joo Shin, The-Vinh Tran, Ji Hoon Jeong, Choon-Gon Jang, Seung-Yeol Nah, Kiyofumi Yamada, Toshitaka Nabeshima, Hyoung-Chun Kim
Dextromethorphan (DM) is a dextrorotatory isomer of levorphanol, a typical morphine-like opioid. When administered at supra-antitussive doses, DM produces psychotoxic and neurotoxic effects in humans. Although DM abuse has been well-documented, few studies have examined the effects of high-dose DM. The present study aimed to explore the effects of a single high dose of DM on mortality and seizure occurrence. After intraperitoneal administration with a high dose of DM (80mg/kg), Sprague-Dawley rats showed increased seizure occurrence and intensity...
September 13, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28916137/oxytocin-induces-penile-erection-and-yawning-when-injected-into-the-bed-nucleus-of-the-stria-terminalis-involvement-of-glutamic-acid-dopamine-and-nitric-oxide
#10
Fabrizio Sanna, Jessica Bratzu, Antonio Argiolas, Maria Rosaria Melis
Oxytocin (5-100ng), but not Arg(8)-vasopressin (100ng), injected unilaterally into the bed nucleus of the stria terminalis (BNST) induces penile erection and yawning in a dose-dependent manner in male rats. The minimal effective dose was 20ng for penile erection and 5ng for yawning. Oxytocin responses were abolished not only by the oxytocin receptor antagonist d(CH2)5Tyr(Me)(2)-Orn(8)-vasotocin (1μg), but also by (+) MK-801 (1μg), an excitatory amino acid receptor antagonist of the N-methyl-d-aspartic acid (NMDA) subtype, SCH 23390 (1μg), a D1 receptor antagonist, but not haloperidol (1μg), a D2 receptor antagonist, and SMTC (40μg), an inhibitor of neuronal nitric oxide synthase, injected into the BNST 15min before oxytocin...
September 12, 2017: Hormones and Behavior
https://www.readbyqxmd.com/read/28913780/anxiolytic-like-effects-of-%C3%AE-asarone-in-a-mouse-model-of-chronic-pain
#11
Jiao Tian, Zhen Tian, Shu-Li Qin, Pu-Yu Zhao, Xun Jiang, Zhen Tian
α-asarone (ASR) is a major bioactive compound isolated from the rhizome of Acorus tatarinowii Schott and it has extensive biological effects. Clinically, anxiety disorder is a common comorbidity of chronic pain. However, limited information is available regarding the effects of ASR on chronic pain-related anxiety. This study aims to evaluate the anxiolytic effects of ASR in chronic pain mice. Chronic inflammatory pain was induced by hind-paw injection of complete Freund's adjuvant (CFA). Behavioral tests, western-blot analysis and whole-cell patch recordings were performed to evaluate the subsequent events...
September 15, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28912687/alterations-in-properties-of-glutamatergic-transmission-in-the-temporal-cortex-and-hippocampus-following-pilocarpine-induced-acute-seizures-in-wistar-rats
#12
Dmitry V Amakhin, Sergey L Malkin, Julia L Ergina, Kirill A Kryukov, Ekaterina A Veniaminova, Olga E Zubareva, Aleksey V Zaitsev
Temporal lobe epilepsy (TLE) is the most common type of focal epilepsy in humans, and is often developed after an initial precipitating brain injury. This form of epilepsy is frequently resistant to pharmacological treatment; therefore, the prevention of TLE is the prospective approach to TLE therapy. The lithium-pilocarpine model in rats replicates some of the main features of TLE in human, including the pathogenic mechanisms of cell damage and epileptogenesis after a primary brain injury. In the present study, we investigated changes in the properties of glutamatergic transmission during the first 3 days after pilocarpine-induced acute seizures in Wistar rats (PILO-rats)...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28912557/a-nmda-receptor-calcium-influx-assay-sensitive-to-stimulation-by-glutamate-and-glycine-d-serine
#13
Hongqiu Guo, L Miguel Camargo, Fred Yeboah, Mary Ellen Digan, Honglin Niu, Yue Pan, Stephan Reiling, Gilberto Soler-Llavina, Wilhelm A Weihofen, Hao-Ran Wang, Y Gopi Shanker, Travis Stams, Anke Bill
N-methyl-D-aspartate-receptors (NMDARs) are ionotropic glutamate receptors that function in synaptic transmission, plasticity and cognition. Malfunction of NMDARs has been implicated in a variety of nervous system disorders, making them attractive therapeutic targets. Overexpression of functional NMDAR in non-neuronal cells results in cell death by excitotoxicity, hindering the development of cell-based assays for NMDAR drug discovery. Here we report a plate-based, high-throughput approach to study NMDAR function...
September 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28911655/therapeutic-effects-of-d-aspartate-in-a-mouse-model-of-multiple-sclerosis
#14
Sanaz Afraei, Antimo D'Aniello, Reza Sedaghat, Parvin Ekhtiari, Gholamreza Azizi, Nakisa Tabrizian, Laura Magliozzi, Zahra Aghazadeh, Abbas Mirshafiey
Experimental autoimmune encephalomyelitis (EAE) is an animal model of multiple sclerosis. EAE is mainly mediated by adaptive and innate immune responses that leads to an inflammatory demyelization and axonal damage. The aim of the present research was to examine the therapeutic efficacy of D-aspartic acid (D-Asp) on a mouse EAE model. EAE induction was performed in female C57BL/6 mice by myelin 40 oligodendrocyte glycoprotein (35-55) in a complete Freund's adjuvant emulsion, and D-Asp was used to test its efficiency in the reduction of EAE...
July 2017: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28910980/neuroprotective-effect-of-deferoxamine-on-n-methyl-d-aspartate-induced-excitotoxicity-in-rgc-5-cells
#15
Ying Tian, Ye He, Weitao Song, Endong Zhang, Xiaobo Xia
Many N-methyl-d-aspartate (NMDA) receptor antagonists have been used to treat neurodegenerative diseases induced by glutamate excitotoxicity in clinics. However, the universality of the glutamic acid neurotransmitter system makes the glutamic acid receptor blockers inefficient and unsafe. Thus, regulating the downstream signaling pathway in the excitotoxicity of glutamic acid may be a more effective and safer way to antagonize the glutamic acid receptor. In this study, we investigated the effect of deferoxamine (DFO), an iron chelator, on the NMDA-induced excitotoxicity...
September 1, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/28905135/a-case-of-reversible-anti-nmda-receptor-encephalitis-neuropsychological-and-neuroradiological-features
#16
Carlotta Mutti, Federica Barocco, Lucia Zinno, Anna Negrotti, Marco Spallazzi, Giovanni Pavesi, Simona Gardini, Paolo Caffarra
Anti-N-methyl-D-aspartate receptor (anti-NMDAR) encephalitis is an autoimmune encephalitis mainly affecting young women. We report a case of a mild paraneoplastic anti-NMDAR encephalitis in a 31-year-old female with an ovarian immature teratoma. The patient exhibited a severe short-term episodic memory impairment and psychiatric symptoms. A detailed diagnostic work-up including complete clinical and laboratory examinations, neuropsychological assessments, and neuroradiological investigations has been done at the onset and during follow-up...
September 13, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28902622/functional-interaction-between-n-methyl-d-aspartate-receptor-and-ascorbic-acid-during-neuropathic-pain-induced-by-chronic-constriction-injury-of-the-sciatic-nerve
#17
Sepideh Saffarpour, Farinaz Nasirinezhad
BACKGROUND: Neuropathic pain is a chronic pain condition, which is resistant to therapy. Ascorbate was released because of the activation of glutaminergic neurons. Due to the important role of N-methyl-D-aspartate (NMDA) receptors in the pathophysiology of neuropathic pain, this study investigated the analgesic efficacy of ascorbic acid (AA) in neuropathic pain condition and the role of NMDA receptors in this effect. METHODS: For this purpose, adult male rats were randomly allocated to experimental groups (n=8 in each group)...
September 13, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28902183/patient-characteristics-affect-the-response-to-ketamine-and-opioids-during-the-treatment-of-vaso-occlusive-episode-related-pain-in-sickle-cell-disease
#18
Raissa Nobrega, Kathy A Sheehy, Caroline Lippold, Amy L Rice, Julia C Finkel, Zenaide M N Quezado
BackgroundN-methyl-D-aspartate receptor activation has been implicated in the pathobiology of inflammatory, nociceptive and neuropathic pain, opioid tolerance, opioid-induced hyperalgesia, and central sensitization. Some of those mechanisms underlie sickle cell disease(SCD)-associated pain.MethodsWe conducted an exploratory cohort study of SCD patients who during vaso-occlusive episodes (VOEs) received subanesthetic doses of the N-methyl-D-aspartate receptor antagonist, ketamine, as an adjunct to opioids. We sought to identify predictors of changes in pain scores and of the percentage of ketamine infusions associated with meaningful changes (≥20% reduction) in pain and opioid consumption...
September 13, 2017: Pediatric Research
https://www.readbyqxmd.com/read/28901528/beyond-symptomatic-effects-donepezil-s-potential-for-neuroprotection-and-disease-modification-in-alzheimer-s-disease
#19
REVIEW
Seung Hyun Kim, Nagaendran Kandiah, Jung-Lung Hsu, Chuthamanee Suthisisang, Chesda Udommongkol, Amitabh Dash
Alzheimer's disease (AD) is associated with neurodegenerative changes resulting clinically in progressive cognitive and functional deficits. The only therapies are the cholinesterase inhibitors (ChEIs) donepezil, galantamine, and rivastigmine and the N-methyl-D-aspartate-receptor antagonist memantine. Donepezil acts primarily on the cholinergic system as symptomatic treatment, but it also has potential for disease modification and may reduce the rate of progression of AD. This review explores the potential for a disease modifying effect of donepezil...
September 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28900826/comparative-examination-of-temporal-glyoxalase-1-variations-following-perforant-pathway-transection-excitotoxicity-and-controlled-cortical-impact-injury
#20
Philipp Pieroh, Daniel-Christoph Wagner, Beat Alessandri, Mojgan Dabbagh Nazari, Angela Ehrlich, Chalid Ghadban, Constance Hobusch, Gerd Birkenmeier, Faramarz Dehghani
Following acute neuronal lesions, metabolic imbalance occurs, the rate of glycolysis increases, and methylglyoxal (MGO) forms, finally leading to metabolic dysfunction and inflammation. The glyoxalase system is the main detoxification system for MGO and is impaired following excitotoxicity and stroke. However, it is not known yet whether alterations of the glyoxalase system are also characteristic for other neuronal damage models. Neuronal damage was induced in organotypic hippocampal slice cultures by transection of perforant pathway (PPT; 5 min to 72 h) and N-methyl-D-aspartate (NMDA; 50 μM for 4 h) or in vivo after controlled cortical impact (CCI) injury (2 h to 14 days)...
September 12, 2017: Neurotoxicity Research
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