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ACS Chemical Neuroscience

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https://www.readbyqxmd.com/read/28532151/a-biotinylated-bioluminescent-probe-for-long-lasting-targeted-in-vivo-imaging-of-xenografted-brain-tumors-in-mice
#1
Yu Lin Jiang, Yun Zhu, Alfred B Moore, Kayla Miller, Ann-Marie Broome
Bioluminescence is a useful tool for imaging of cancer in in vivo animal models that endogenously express luciferase, an enzyme that requires a substrate for visual readout. Current bioluminescence imaging, using commonly available luciferin substrates, only lasts a short time (15-20 min). To avoid repeated administration of luciferase substrate during cancer detection and surgery, a long lasting bioluminescence imaging substrate or system is needed. A novel water-soluble biotinylated luciferase probe, B-YL (1), was synthesized...
May 22, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28520395/tricyclic-spirolactones-as-modular-trpv1-synthetic-agonists
#2
Yelena Mostinski, Gilad Noy, Rakesh Kumar, Dmitry Tsvelikhovsky, Avi Priel
TRPV1 is a prominent signal integrator of the pain system, known to be activated by vanilloids, a family of endogenous and exogenous pain-evoking molecules, through the vanilloid-binding site (VBS). The extensive preclinical profiling of small molecule inhibitors provides intriguing evidence that TRPV1 inhibition can be a useful therapeutic approach. However, the dissimilarity of chemical species that activate TRPV1 creates a major obstacle to understanding the molecular mechanism of pain induction, which is viewed as a pivotal trait of the somatosensory system...
May 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28514141/subtype-specific-agonists-for-nmda-receptor-glycine-binding-sites
#3
Alex Maolanon, Rune Risgaard, Shuang-Yan Wang, Yoran Snoep, Athanasios Papangelis, Feng Yi, David Holley, Anne F Barslund, Niels Svenstrup, Kasper B Hansen, Rasmus Prætorius Clausen
A series of analogues based on serine as lead structure were designed and their agonist activities were evaluated at recombinant NMDA receptor subtypes (GluN1/2A-D) using two-electrode voltage-clamp (TEVC) electrophysiology. Pronounced variation in subunit-selectivity, potency, and agonist efficacy was observed in a manner that was dependent on the GluN2 subunit in the NMDA receptor. In particular, compounds 15a and 16a are potent GluN2C-specific superagonists at the GluN1 subunit with agonist efficacies of 398% and 308% compared to glycine...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28485573/radiosynthesis-and-in-vivo-evaluation-of-11-c-a1070722-a-high-affinity-gsk-3-pet-tracer-in-primate-brain
#4
Jaya Prabhakaran, Francesca Zanderigo, Kiran Kumar Solingapuram Sai, Harry Rubin-Falcone, Matthew J Jorgensen, Jay R Kaplan, Akiva Mintz, J John Mann, J S Dileep Kumar
Dysfunction of glycogen synthase kinase 3 (GSK-3) is implicated in the etiology of Alzheimer's disease, Parkinson's disease, diabetes, pain, and cancer. A radiotracer for functional positron emission tomography (PET) imaging could be used to study the kinase in brain disorders and to facilitate the development of small molecule inhibitors of GSK-3 for treatment. At present, there is no target-specific or validated PET tracer available for the in vivo monitoring of GSK-3. We radiolabeled the small molecule inhibitor [(11)C]1-(7-methoxy- quinolin-4-yl)-3-(6-(trifluoromethyl)pyridin-2-yl)urea ([(11)C]A1070722) with high affinity to GSK-3 (Ki = 0...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28511005/characterization-of-l-theanine-excitatory-actions-on-hippocampal-neurons-towards-the-generation-of-novel-n-methyl-d-aspartate-receptor-modulators-based-on-its-backbone
#5
Fatiha Sebih, Matthieu Rousset, Salima Bellahouel, Marc Rolland, Marie Celeste de Jesus Ferreira, Janique Guiramand, Catherine Cohen-Solal, Gérard Barbanel, Thierry Cens, Mohammed Abouazza, Adrien Tassou, Maud Gratuze, Céline Meunier, Pierre Charnet, Michel Vignes, Valérie Rolland
L-Theanine (or L-γ-N-ethyl-glutamine) is the major amino acid found in Camellia sinensis. It has received much attention because of its pleiotropic physiological and pharmacological activities leading to health benefits in humans, especially. We describe here a new, easy, efficient and environmentally-friendly chemical synthesis of L-Theanine and L-γ-N-propyl-Gln and their corresponding D isomers. L-Theanine, and its derivatives obtained so far, exhibited partial co-agonistic action at N-methyl-D-aspartate (NMDA) receptors, with no detectable agonist effect at other glutamate receptors, on cultured hippocampal neurons...
May 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28510417/correction-to-classics-in-chemical-neuroscience-haloperidol
#6
Marshall W Tyler, Josefa Zaldivar-Diez, Stephen J Haggarty
No abstract text is available yet for this article.
May 16, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28471166/crocus-sativus-extract-tightens-the-blood-brain-barrier-reduces-amyloid-%C3%AE-load-and-related-toxicity-in-5xfad-mice
#7
Yazan S Batarseh, Sonali S Bharate, Vikas Kumar, Ajay Kumar, Ram A Vishwakarma, Sandip B Bharate, Amal Kaddoumi
Crocus sativus, commonly known as saffron or Kesar, is used in Ayurveda and other folk medicines for various purposes as an aphrodisiac, antispasmodic, and expectorant. Previous evidence suggested that Crocus sativus is linked to improving cognitive function in Alzheimer's disease (AD) patients. The aim of this study was to in vitro and in vivo investigate the mechanism(s) by which Crocus sativus exerts its positive effect against AD. The effect of Crocus sativus extract on Aβ load and related toxicity was evaluated...
May 15, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28472878/neuropeptide-kyotorphin-impacts-on-lipopolysaccharide-induced-glucocorticoid-mediated-inflammatory-response-a-molecular-link-to-nociception-neuroprotection-and-anti-inflammatory-action
#8
Juliana Perazzo, Carla Lima, Montserrat Heras, Eduard Bardají, Mônica Lopes-Ferreira, Miguel Castanho
Neuropeptide kyotorphin (KTP) is a potent analgesic if administered directly into the brain. In contrast, KTP-amide (KTP-NH2) is analgesic, neuroprotective, and anti-inflammatory following systemic administration, albeit its mechanism of action is unknown. The aim of this study was to shed light on the mechanism of action of KTP-NH2 at the molecular level. KTP-NH2 does not inhibit the enkephalinases angiotensin-converting-enzyme and dipeptidyl-peptidase 3. Intravital microscopy showed that KTP-NH2 decreased the number of rolling leukocytes in a mouse model of inflammation induced by lipopolysaccharide (LPS)...
May 9, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28482157/enhancing-continuous-online-microdialysis-using-dexamethasone-measurement-of-dynamic-neurometabolic-changes-during-spreading-depolarization
#9
Erika L Varner, Chi Leng Leong, Andrea Jaquins-Gerstl, Kathryn M Nesbitt, Martyn G Boutelle, Adrian Charles Michael
Microdialysis is well established in chemical neuroscience as a mainstay technology for real time intracranial chemical monitoring in both animal models and human patients. Evidence shows that microdialysis can be enhanced by mitigating the penetration injury caused during the insertion of microdialysis probes into brain tissue. Herein, we show that retrodialysis of dexamethasone in the rat cortex enhances the microdialysis detection of K+ and glucose transients induced by spreading depolarization. Without dexamethasone, quantification of glucose transients was unreliable by 5 days after probe insertion...
May 8, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28460160/serotonergic-approaches-in-parkinson-s-disease-translational-perspectives-an-update
#10
Philippe Huot, Véronique Sgambato-Faure, Susan H Fox, Andrew C McCreary
Parkinson's disease (PD) has long been seen as a disorder caused by degeneration of the dopaminergic system, leading to the classic motor manifestations of the disease. However, there is now overwhelming evidence that PD is more than a disease merely caused by dopamine depletion. It is well-known that a myriad of other neurotransmitters are affected by the disease process. One such neurotransmitter is serotonin (5-HT). 5-HT has been shown to play a role in several motor and nonmotor manifestations of PD, including tremor, cognition, depression and psychosis...
May 5, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28460173/a-visible-light-sensitive-caged-serotonin
#11
Ricardo Cabrera, Oscar Filevich, Beatriz García-Acosta, Jegath Athilingam, Kevin J Bender, Kira E Poskanzer, Roberto Etchenique
Serotonin, or 5-hydroxytryptamine (5HT), is an important neurotransmitter in the nervous system of both vertebrates and invertebrates. Deficits in 5HT signaling are responsible for many disabling psychiatric conditions, and its molecular machinery is the target of many pharmaceuticals. We present a new 5HT phototrigger, the compound [Ru(bpy)2(PMe3)(5HT)](2+), where PMe3 is trimethylphosphine. As with other ruthenium-bipyridyl based caged compounds, [Ru(bpy)2(PMe3)(5HT)](2+) presents activity in the visible region of the spectrum...
May 4, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28441487/the-isomeric-preference-of-an-atypical-dopamine-transporter-inhibitor-contributes-to-its-selection-of-the-transporter-conformation
#12
Ara M Abramyan, Sebastian Stolzenberg, Zheng Li, Claus J Loland, Frank Noé, Lei Shi
Cocaine, a widely abused psychostimulant, inhibits the dopamine transporter (DAT) by trapping the protein in an outward-open conformation, whereas atypical DAT inhibitors such as benztropine have low abuse liability and prefer less outward-open conformations. Here, we use a spectrum of computational modeling and simulation approaches to obtain the underlying molecular mechanism in atomistic detail. Interestingly, our quantum mechanical calculations and molecular dynamics (MD) simulations suggest that a benztropine derivative JHW007 prefers a different stereoisomeric conformation of tropane in binding to DAT compared to that of a cocaine derivative, CFT...
May 4, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28425704/an-ortho-iminoquinone-compound-reacts-with-lysine-inhibiting-aggregation-while-remodeling-mature-amyloid-fibrils
#13
Luiza Fernandes, Nathalia Moraes, Fernanda S Sagrillo, Augusto V Magalhães, Marcela C de Moraes, Luciana Romão, Jeffery W Kelly, Debora Foguel, Neil P Grimster, Fernando L Palhano
Protein aggregation is a hallmark of several neurodegenerative diseases, including Alzheimer's and Parkinson's diseases. It has been shown that lysine residues play a key role in the formation of these aggregates. Thus, the ability to disrupt aggregate formation by covalently modifying lysine residues could lead to the discovery of therapeutically relevant antiamyloidogenesis compounds. Herein, we demonstrate that an ortho-iminoquinone (IQ) can be utilized to inhibit amyloid aggregation. Using alpha-synuclein and Aβ1-40 as model amyloidogenic proteins, we observed that IQ was able to react with lysine residues and reduce amyloid aggregation...
May 4, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28467708/novel-benzothiazole-derivatives-as-fluorescent-probes-for-detection-of-%C3%AE-amyloid-and-%C3%AE-synuclein-aggregates
#14
Hiroyuki Watanabe, Masahiro Ono, Taisuke Ariyoshi, Rikako Katayanagi, Hideo Saji
Deposits of β-amyloid (Aβ) and α-synuclein (α-syn) are the hallmark of Alzheimer's disease (AD) and Parkinson's disease (PD), respectively. The detection of these protein aggregates with fluorescent probes is particularly of interest for preclinical studies using fluorescence microscopy on human brain tissue. In this study, we newly designed and synthesized three push-pull benzothiazole (PP-BTA) derivatives as fluorescent probes for detection of Aβ and α-syn aggregates. Fluorescence intensity of all PP-BTA derivatives significantly increased upon binding to Aβ(1-42) and α-syn aggregates in solution...
May 3, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28453930/the-apoe-%C3%AE%C2%B54-allele-is-associated-with-lower-selenium-levels-in-the-brain-implications-for-alzheimer-s-disease
#15
Bárbara R Cardoso, Dominic J Hare, Monica Lind, Catriona A McLean, Irene Volitakis, Simon M Laws, Colin L Masters, Ashley I Bush, Blaine R Roberts
The antioxidant activity of selenium, which is mainly conferred by its incorporation into dedicated selenoproteins, has been suggested as a possible neuroprotective approach for mitigating neuronal loss in Alzheimer's disease. However, there is inconsistent information with respect to selenium levels in the Alzheimer's disease brain. We examined the concentration and cellular compartmentalization of selenium in the temporal cortex of Alzheimer's disease and control brain tissue. We found that Alzheimer's disease was associated with decreased selenium concentration in both soluble (i...
May 3, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28425701/effects-of-glutamate-receptor-activation-on-local-oxygen-changes
#16
Lindsay R Walton, Nick G Boustead, Susan Carroll, R Mark Wightman
Glutamate is ubiquitous throughout the brain and serves as the primary excitatory neurotransmitter. Neurons require energy to fire, and energetic substrates (i.e., O2, glucose) are renewed via cerebral blood flow (CBF) to maintain metabolic homeostasis. Magnetic resonance brain functionality studies rely on the assumption that CBF and neuronal activity are coupled consistently throughout the brain; however, the origin of neuronal activity does not always coincide with signals indicative of energy consumption (e...
May 3, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28452458/chiro-optical-modulation-for-nurr1-production-from-stem-cells
#17
Madhumita Patel, Hyo Jung Moon, Ja Hye Hong, Byeongmoon Jeong
Nuclear receptor related 1 (NURR1) is an essential protein for maintenance of dopaminergic neurons in adult midbrain of which deficiency leads to Parkinson's disease. To enhance the NURR1 production of neural cells, various approaches are under investigation. Here we report that NURR1 is highly expressed in stem cells by exposure to an L-polarized blue light emitting diode (LED). Compared to stem cells cultured in the absence of a LED, under polarized green and red LEDs, the stem cells exposed to a polarized blue LED significantly enhanced neuronal biomarkers such as neurofilament M (NFM) and neuron specific enolase (NSE) at both mRNA and protein levels...
May 2, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28459529/-18-f-fpp-a-pet-ligand-for-the-5-ht2c-receptor
#18
Guy A Higgins
In the current issue of ACS Chemical Neuroscience, Kim et al. report on the early characterization of 4-(3-[(18)F] fluorophenethoxy)pyrimidine ((18)F-FPP) as a new positron emission tomography radiotracer for imaging brain 5-HT2C receptors ( Kim, J., et al. ( 2017 ) A potential PET radiotracer for the 5-HT2c receptor: Synthesis and in vivo evaluation of 4-(3-[(18)F]Fluorophenethoxy)pyrimidine. ACS Chem. Neurosci. , DOI: 10.1021/acschemneuro.6b00445 ). At the present time, the tracer properties of (18)F-FPP have only been reported in rats...
May 1, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28375615/specific-connectivity-and-unique-molecular-identity-of-met-receptor-tyrosine-kinase-expressing-serotonergic-neurons-in-the-caudal-dorsal-raphe-nuclei
#19
Ryan J Kast, Hsiao-Huei Wu, Piper Williams, Patricia Gaspar, Pat Levitt
Molecular characterization of neurons across brain regions has revealed new taxonomies for understanding functional diversity even among classically defined neuronal populations. Neuronal diversity has become evident within the brain serotonin (5-HT) system, which is far more complex than previously appreciated. However, until now it has been difficult to define subpopulations of 5-HT neurons based on molecular phenotypes. We demonstrate that the MET receptor tyrosine kinase (MET) is specifically expressed in a subset of 5-HT neurons within the caudal part of the dorsal raphe nuclei (DRC) that is encompassed by the classic B6 serotonin cell group...
May 1, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28447781/artemisinin-protectes-retinal-neuronal-cells-against-oxidative-stress-and-restores-rat-retinal-physiological-function-from-light-exposed-damage
#20
Fengxia Yan, Hai-Tao Wang, Yang Gao, Jiang-Ping Xu, Wenhua Zheng
Oxidative stress plays a key role in the pathogenesis of age-related macular degeneration (AMD), a leading cause of severe visual loss and blindness in the aging population which lacks any effective treatments currently. In this study, artemisinin, a well-known anti-malarial drug was found to suppress hydrogen peroxide (H2O2)-induced cell death in retinal neuronal RGC-5 cells. Artemisinin, in the therapeutically relevant dosage, concentration-dependently attenuated the accumulation of intracellular reactive oxygen species (ROS), increased mitochondrial mitochondrial membrane potential and decreased cell apoptosis in RGC-5 cells induced by H2O2...
April 27, 2017: ACS Chemical Neuroscience
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