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ACS Chemical Neuroscience

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https://www.readbyqxmd.com/read/29115830/gastrodin-and-isorhynchophylline-synergistically-inhibit-mpp-induced-oxidative-stress-in-sh-sy5y-cells-by-targeting-erk1-2-and-gsk-3%C3%AE-pathways-involvement-of-nrf2-nuclear-translocation
#1
Qiang Li, Chengu Niu, Xiaojie Zhang, Miaoxian Dong
The pathogenesis of Parkinson's disease (PD) is multifactorial event. Combination therapies might be more effective in controlling the disease. Thus, the studies reported were designed to test the hypothesis that gastrodin (GAS)-induced de novo synthesis of nuclear factor E2-related factor 2 (Nrf2) and isorhynchophylline (IRN) inhibition of Nrf2 nuclear export contribute to their additive or synergistic neuroprotective effect. Here, we have demonstrated that the combination of GAS and IRN (GAS/IRN) protects SH-SY5Y cells against 1-methyl-4-phenylpyridinium (MPP(+)) toxicity in a synergistic manner...
November 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29144727/ex-vivo-measurement-of-electrically-evoked-dopamine-release-in-zebrafish-whole-brain
#2
Mimi Shin, Thomas M Field, Chase S Stucky, Mia N Furgurson, Michael A Johnson
No abstract text is available yet for this article.
November 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29078045/higher-aminopeptidase-activity-determined-by-electroosmotic-push-pull-perfusion-contributes-to-selective-vulnerability-of-the-hippocampal-ca1-region-to-oxygen-glucose-deprivation
#3
Yangguang Ou, Stephen G Weber
It has been known for over a century that the hippocampus, the center for learning and memory in the brain, is selectively vulnerable to ischemic damage, with the CA1 being more vulnerable than the CA3. It is also known that leucine enkephalin, or YGGFL, is neuroprotective. We hypothesized that the extracellular hydrolysis of YGGFL may be greater in the CA1 than the CA3, which would lead to the observed difference in susceptibility to ischemia. In rat organotypic hippocampal slice cultures, we estimated the Michaelis constant and the maximum velocity for membrane-bound aminopeptidase activity in the CA1 and CA3 regions...
November 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29140675/identification-of-novel-allosteric-modulators-of-glutamate-transporter-eaat2
#4
Sandhya Kortagere, Ole Valente Mortensen, Jingsheng Xia, William Lester, Yuhong Fang, Yellamelli V V Srikanth, Joseph M Salvino, Andreia Cristina Karklin Fontana
Dysfunction of excitatory amino acid transporters (EAATs) has been implicated in the pathogenesis of various neurological disorders, such as stroke, brain trauma, epilepsyand neurodegenerative diseases among others. EAAT2 is the main subtype responsible for glutamate clearance in the brain, having a key role in regulating transmission and preventing excitotoxicity. Therefore, compounds that increase the expression or activity of EAAT2 have therapeutic potential for neuroprotection. Previous studies identified molecular determinants for EAAT2 transport stimulation in a structural domain that lies at the interface of the rigid trimerization domain and the central substrate binding transport domain...
November 15, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29135225/regional-variations-of-spontaneous-transient-adenosine-release-in-brain-slices
#5
Scott T Lee, B Jill Venton
Transient adenosine signaling has been recently discovered in vivo, where the concentration is on average 180 nM and the duration only 3-4 seconds. Characterizing transient adenosine release in brain slices would facilitate pharmacological experiments testing formation and function of adenosine. Here, the goal was to compare the frequency, concentration, and duration of transient events in rat brain slices from the pre-frontal cortex (PFC), hippocampus (CA1), and thalamus using fast-scan cyclic voltammetry...
November 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29050469/in-vivo-18-f-ge-179-brain-signal-does-not-show-nmda-specific-modulation-with-drug-challenges-in-rodents-and-nonhuman-primates
#6
Matthias Schoenberger, Frederick A Schroeder, Michael S Placzek, Randall L Carter, Bruce R Rosen, Jacob M Hooker, Christin Y Sander
As one of the major excitatory ion channels in the brain, NMDA receptors have been a leading research target for neuroscientists, physicians, medicinal chemists, and pharmaceutical companies for decades. Molecular imaging of NMDA receptors by means of positron emission tomography (PET) with [(18)F]GE-179 quickly progressed to clinical PET studies, but a thorough understanding of its binding specificity has been missing and has thus limited signal interpretation. Here a preclinical study with [(18)F]GE-179 in rodents and nonhuman primates (NHPs) is presented in an attempt to characterize [(18)F]GE-179 signal specificity...
November 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29131938/a-crash-course-in-calcium-channels
#7
Gerald W Zamponi
Much progress has been made in understanding the molecular physiology and pharmacology of calcium channels. Recently, there have been tremendous advances in learning about calcium channel structure and function through crystallography and cryo-electron microscopy studies. Here, I will give an overview of our knowledge about calcium channels, and highlight two recent studies that give important insights into calcium channel structure.
November 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29131576/pharmacological-characterization-of-3h-atpca-as-a-substrate-for-studying-the-functional-role-of-the-betaine-gaba-transporter-1-and-the-creatine-transporter
#8
Anas Al-Khawaja, Anne S Haugaard, Ales Marek, Rebekka Löffler, Louise Thiesen, Monica Santiveri, Maria Damgaard, Christoffer Bundgaard, Bente Frølund, Petrine Wellendorph
The betaine/γ-aminobutyric acid (GABA) transporter 1 (BGT1) is one of the four GABA transporters (GATs) involved in the termination of GABAergic neurotransmission. Although suggested to be implicated in seizure management, the exact functional importance of BGT1 in the brain is still elusive. This is partly owing to the lack of potent and selective pharmacological tool compounds that can be used to probe its function. We previously reported the identification of 2-amino-1,4,5,6-tetrahydropyrimidine-5-carboxylic acid (ATPCA), a selective substrate for BGT1 over GAT1/GAT3, but also an agonist for GABAA receptors...
November 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29094921/endosulfan-and-cypermethrin-pesticide-mixture-induces-synergistic-or-antagonistic-effects-on-developmental-exposed-rats-depending-on-the-analyzed-behavioral-or-neurochemical-end-points
#9
Belén Gómez-Giménez, Marta Llansola, Andrea Cabrera-Pastor, Vicente Hernández-Rabaza, Ana Agustí, Vicente Felipo
Exposure to pesticides has been associated with neurodevelopmental toxicity. Usually people are exposed to mixtures of pesticides. However, most studies analyze the effects of individual pesticides. Developmental exposure to mixtures of pesticides may result in additive effects or in antagonistic or synergistic effects. The aim of this work was to compare the effects of developmental exposure of rats to cypermethrin or endosulfan with the effects of its mixture on cognitive and motor function and on some underlying mechanisms...
November 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29072902/discovery-of-a-novel-muscarinic-receptor-pet-radioligand-with-rapid-kinetics-in-the-monkey-brain
#10
Jonas Malmquist, Katarina Varnäs, Marie Svedberg, Frédéric Vallée, Jeffrey S Albert, Sjoerd J Finnema, Magnus Schou
Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic neurotransmitter concentrations in vivo. The radioligand of choice for such measurements on the cholinergic system is the muscarinic receptor antagonist N-[1-(11)C]propyl-3-piperidyl benzilate (PPB). In an effort to overcome the shortcomings with the technically cumbersome synthesis of [(11)C]PPB, we designed and synthesized four structurally related analogues of PPB, of which (S,R)-1-methylpiperidin-3-yl)2-cyclopentyl-2-hydroxy-2-phenylacetate (1) was found to bind muscarinic receptors with similar affinity as PPB (3...
November 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29058403/traced-on-the-timeline-discovery-of-acetylcholine-and-the-components-of-the-human-cholinergic-system-in-a-primitive-unicellular-eukaryote-acanthamoeba-spp
#11
Abdul Mannan Baig, Zohaib Rana, Sumayya Tariq, Salima Lalani, H R Ahmad
Acetylcholine (ACh) is the neurotransmitter of cholinergic signal transduction that affects the target cells via muscarinic (mAChR) and nicotinic (nAChR) cholinergic receptors embedded in the cell membrane. Of the cholinergic receptors that bind to ACh, the mAChRs execute several cognitive and metabolic functions in the human central nervous system (CNS). Very little is known about the origins and autocrine/paracrine roles of the ACh in primitive life forms. With the recent report of the evidence of an ACh binding mAChR1 like receptor in Acanthamoeba spp...
November 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29129052/synthesis-and-evaluation-of-orexin-1-receptor-antagonists-with-improved-solubility-and-cns-permeability
#12
David A Perrey, Ann M Decker, Yanan Zhang
Orexins are hypothalamic neuropeptides playing important roles in many functions including the motivation of addictive behaviors. Blockade of the orexin-1 receptor has been suggested as a potential strategy for the treatment of drug addiction. We have previously reported OX1 receptor antagonists based on the tetrahydroisoquinoline scaffold with excellent OX1 potency and selectivity; however, these compounds had high lipophilicity (clogP > 5) and low to moderate solubility. In an effort to improve their properties, we have designed and synthesized a series of analogs where the 7-position substituents known to favor OX1 potency and selectivity were retained, and groups of different nature were introduced at the 1-position where substitution was generally tolerated as demonstrated in previous studies...
November 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29120605/targeting-heat-shock-protein-70-to-ameliorate-c-jun-expression-and-improve-demyelinating-neuropathy
#13
Xinyue Zhang, Chengyuan Li, Stephen C Fowler, Zheng Zhang, Brian S J Blagg, Rick T Dobrowsky
Increased expression of the c-jun transcription factor occurs in a variety of human neuropathies and is critical in promoting Schwann cell (SC) dedifferentiation and loss of the myelinated phenotype. Using cell culture models, we previously identified KU-32 as a novobiocin-based C-terminal heat shock protein 90 (Hsp90) inhibitor that decreased c-jun expression and the extent of demyelination. Additional chemical optimization has yielded KU-596 as a neuroprotective novologue whose mechanistic efficacy to improve a metabolic neuropathy requires the expression of Hsp70...
November 9, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29120604/molecular-determinants-for-substrate-interactions-with-the-glycine-transporter-glyt2
#14
Jane E Carland, Michael Thomas, Shannon N Mostyn, Nandhitha Subramanian, Megan Louise O'Mara, Renae M Ryan, Robert J Vandenberg
Transporters in the SLC6 family play key roles in regulating neurotransmission and are the targets for a wide range of therapeutics. Important insights into the transport mechanisms and the specificity of drug interactions of SLC6 transporters have been obtained from the crystal structures of a bacterial homolog of the family, LeuTAa, and more recently the Drosophila dopamine transporter and the human serotonin transporter. However, there is disputed evidence that the bacterial leucine transporter, LeuTAa, contains two substrate binding sites that work cooperatively in the mechanism of transport, with the binding of a second substrate being required for the release of the substrate from the primary site...
November 9, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29120167/understanding-the-inflammatory-tissue-reaction-to-brain-implants-to-improve-neurochemical-sensing-performance
#15
Steven M Wellman, Takashi D Y Kozai
Neurochemical sensing probes are a valuable diagnostic and therapeutic tool that can be used to study neurodegenerative diseases involving deficiencies in neurotransmitter signaling. However, implantation of these biosensors can elicit a harmful tissue response that alters the neurochemical environment within the brain. Transmission of chemical messengers via neurons is impeded by a barrier-forming glial scar that occurs within weeks after insertion followed by progressive neurodegeneration, attenuating signal sensitivity...
November 9, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29120166/aromatic-residues-in-the-fourth-transmembrane-spanning-helix-m4-are-important-for-gaba%C3%AF-receptor-function
#16
James Cory-Wright, Mona Alqazzaz, Francesca Wroe, Jenny Jeffreys, Lu Zhou, Sarah C R Lummis
GABAρ receptors are a subfamily of the GABAA receptor family of pentameric ligand-gated ion channels (pLGICs). Each of the five subunits has four transmembrane α-helices (M1-M4), with M4 most distant from the central pore. Aromatic residues in this M4 helix are important for receptor assembly in pLGICs and also may interact with adjacent lipids and/or residues in neighboring α-helices and the extracellular domain to modify or enable channel gating. This study examines the role of M4 receptor aromatic residues in the GABAρ receptor transmembrane domain using site-directed mutagenesis and subsequent expression in HEK293 cells, probing functional parameters using a fluorescent membrane-potential-sensitive dye...
November 9, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29115823/an-overview-of-the-clinical-uses-pharmacology-and-safety-of-modafinil
#17
Eric Murillo-Rodriguez, André Barciela Veras, Nuno Barbosa Rocha, Henning Budde, Sérgio Machado
Modafinil (MOD) is a drug used for the management of excessive daytime sleepiness observed in several sleep disturbances such as shift work sleep disorder, obstructive sleep apnea, restless leg syndrome and narcolepsy. Additionally, a wide scope of medical uses of MOD have been described such as fatigue in subjects with depression as well as patients under chemotherapy. Moreover, there also appear to be a cognitive enhancer drug. In contrast, recent reports have indicated the risk of developing addiction to MOD...
November 8, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29111677/novel-bivalent-5-ht2a-receptor-antagonists-exhibit-high-affinity-and-potency-in-vitro-and-efficacy-in-vivo
#18
Claudia A Soto, Matthew J Shashack, Robert G Fox, Marcy J Bubar, Kenner C Rice, Cheryl S Watson, Kathryn A Cunningham, Scott R Gilbertson, Noelle C Anastasio
The 5-HT2AR plays an important role in various neuropsychiatric disorders including cocaine use disorder and schizophrenia. Homodimerization of this receptor has been suggested but tools that allow direct assessment of 5-HT2AR:5-HT2AR homodimer relevance in these disorders are necessary. We chemically modified the selective 5-HT2AR antagonist M100907 to synthesize a series of homobivalent ligands connected by ethylene glycol linkers of varying lengths that may be useful tools to probe 5-HT2AR:5-HT2AR homodimer function...
November 7, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29110463/8-nitro-cgmp-attenuates-the-interaction-between-snare-complex-and-complexin-through-s-guanylation-of-snap-25
#19
Yusuke Kishimoto, Kohei Kunieda, Atsushi Kitamura, Yuki Kakihana, Takaaki Akaike, Hideshi Ihara
8-Nitroguanosine 3',5'-cyclic monophosphate (8-nitro-cGMP) is the second messenger in nitric oxide/reactive oxygen species redox signaling. This molecule covalently binds to protein thiol groups, called S-guanylation, and exerts various biological functions. Recently, we have identified synaptosomal-associated protein 25 (SNAP-25) as a target of S-guanylation, and demonstrated that S-guanylation of SNAP25 enhanced SNARE complex formation. In this study, we have examined the effects of S-guanylation of SNAP-25 on the interaction between the soluble SNARE complex and complexin (cplx), which binds to the SNARE complex with a high affinity...
November 7, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29077387/anti-nmda-receptor-encephalitis-from-bench-to-clinic
#20
Arun Venkatesan, Krishma Adatia
NMDAR encephalitis is a common cause of autoimmune encephalitis, predominantly affecting young adults. Current data supports the idea that autoantibodies targeting NMDARs are responsible for disease pathogenesis. While these autoantibodies occur in the setting of underlying malignancy in approximately half of all patients, initiating factors for the autoimmune response in the remainder of patients are unclear. While there is increasing evidence supporting viral triggers such as herpes simplex encephalitis, this association and the mechanism of action have not yet been fully described...
November 7, 2017: ACS Chemical Neuroscience
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