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ACS Chemical Neuroscience

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https://www.readbyqxmd.com/read/28418641/classics-in-chemical-neuroscience-ketamine
#1
Marshall W Tyler, Harmony B Yourish, Dawn F Ionescu, Stephen J Haggarty
Ketamine, a molecule of many faces, has contributed immeasurably to numerous realms of clinical practice and scientific inquiry. From anesthesia and analgesia to depression and schizophrenia, it continues to shed light on the molecular underpinnings of pain, consciousness, and the pathophysiology of neuropsychiatric disorders. In particular, research on ketamine's mechanism of action is providing new hope in the search for therapies for treatment-resistant depression and affords insights into disorders of glutamatergic dysfunction...
April 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28362488/serotonin-transporter-associated-protein-complexes-are-enriched-in-synaptic-vesicle-proteins-and-proteins-involved-in-energy-metabolism-and-ion-homeostasis
#2
Jana Haase, Joanna Grudzinska-Goebel, Heidi Kaastrup Müller, Agnieszka Münster-Wandowski, Elysian Chow, Kieran Wynne, Zohreh Farsi, Johannes-Friedrich Zander, Gudrun Ahnert-Hilger
The serotonin transporter (SERT) mediates Na(+)-dependent high-affinity serotonin uptake and plays a key role in regulating extracellular serotonin concentration in the brain and periphery. To gain novel insight into SERT regulation, we conducted a comprehensive proteomics screen to identify components of SERT-associated protein complexes in the brain by employing three independent approaches. In vivo SERT complexes were purified from rat brain using an immobilized high-affinity SERT ligand, amino-methyl citalopram...
April 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28425704/an-ortho-iminoquinone-compound-reacts-with-lysine-inhibiting-aggregation-while-remodeling-mature-amyloid-fibrils
#3
Luiza Fernandes, Nathália Moraes, Fernanda Savacini Sagrillo, Augusto V Magalhães, Marcela Cristina 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 anti-amyloidogenesis compounds. Herein, we demonstrate that an ortho-iminoquinone (IQ) can be utilized to inhibit amyloid aggregation. Using alpha-synuclein and Aβ1-40 as model systems, we observed that IQ was able to react with lysine residues and reduce amyloid aggregation...
April 20, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28425701/the-effects-of-glutamate-receptor-activation-on-local-oxygen-changes
#4
Lindsay 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...
April 20, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28421738/targeting-the-nrf2-amyloid-beta-liaison-in-alzheimer-s-disease-a-rational-approach
#5
Elena Simoni, Melania M Serafini, Roberta Caporaso, Chiara Marchetti, Marco Racchi, Anna Minarini, Manuela Bartolini, Cristina Lanni, Michela Rosini
Amyloid is a prominent feature of Alzheimer's disease (AD). Yet, a linear linkage between amyloid-β peptide (Aβ) and the disease onset and progression has recently been questioned. In this context, the crucial partnership between Aβ and Nrf2 pathways is acquiring paramount importance, offering prospects for deciphering the Aβ-centered disease network. Here, we report on a new class of anti-aggregating agents rationally designed to simultaneously activate transcription-based antioxidant responses, whose lead 1 showed interesting properties in a preliminary investigation...
April 19, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28414422/synthesis-and-structure-activity-relationships-of-tool-compounds-based-on-way163909-a-5-ht2c-receptor-agonist
#6
Ying-Chu Chen, Rachel M Hartley, Noelle C Anastasio, Kathryn A Cunningham, Scott R Gilbertson
The development of probe molecules that can be used to investigate G protein-coupled receptor (GPCR) pharmacology, trafficking, and relationship with other GPCRs is an important and growing area of research. Here, we report the synthesis of analogues of the known selective serotonin (5-HT) 5-HT2C receptor (5-HT2CR) agonist WAY163909 which were designed to allow for the attachment of a second ligand, signaling or reporter molecules, as well as immobilization agents to the parent molecule with the maintenance of agonist activity...
April 19, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28418645/brain-region-and-isoform-specific-phosphorylation-alters-kalirin-sh2-domain-interaction-sites-and-calpain-sensitivity
#7
Megan B Miller, Yan Yan, Kazuya Machida, Drew D Kiraly, Aaron D Levy, Yi I Wu, TuKiet Tan Lam, Thomas Abbott, Anthony John Koleske, Betty A Eipper, Richard E Mains
Kalirin7 (Kal7), a postsynaptic Rho GDP/GTP exchange factor (RhoGEF), plays a crucial role in long term potentiation and in the effects of cocaine on behavior and spine morphology. The KALRN gene has been linked to schizophrenia and other disorders of synaptic function. Mass spectrometry was used to quantify phosphorylation at 26 sites in Kal7 from individual adult rat nucleus accumbens and prefrontal cortex before and after exposure to acute or chronic cocaine. Region- and isoform-specific phosphorylation was observed along with region-specific effects of cocaine on Kal7 phosphorylation...
April 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28418237/what-gene-mutations-affect-serotonin-in-mice
#8
Richard C Tenpenny, Kathryn G Commons
Although serotonin neurotransmission has been implicated in several neurodevelopmental and psychological disorders, the factors that drive dysfunction of the serotonin system are poorly understood. Current research regarding the serotonin system revolves around its dysfunction in neuropsychiatric disorders, but there is no database collating genetic mutations that result in serotonin abnormalities. To bridge this gap, we developed a list of genes in mice that, when perturbed, result in altered levels of serotonin either in brain or blood...
April 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28414419/a-photoswitchable-inhibitor-of-a-glutamate-transporter
#9
Bichu Cheng, Dirk Trauner, Dennis Shchepakin, Michael P Kavanaugh
Excitatory amino acid transporters clear glutamate from the synaptic cleft and play a critical role in glutamatergic neurotransmission. Their differential roles in astrocytes, microglia, and neurons are poorly understood due in part to a lack of pharmacological tools that can be targeted to specific cells and tissues. We now describe a photoswitchable inhibitor, termed ATT, that interacts with the major mammalian forebrain transporters EAAT1-3 in a manner that can be reversibly switched between trans (high-affinity) and cis (low-affinity) configurations using light of different colors...
April 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28406293/n-terminus-binding-preference-for-either-tanshinone-or-analogue-in-both-inhibition-of-amyloid-aggregation-and-disaggregation-of-preformed-amyloid-fibrils-toward-introducing-a-kind-of-novel-anti-alzheimer-compounds
#10
Mingyan Dong, Wei Zhao, Dingkun Hu, Hongqi Ai, Baotao Kang
Amyloid-β (Aβ40/Aβ42) peptide with length of 40 or 42 residues is naturally secreted as cleavage product of the amyloid precursor protein, and formation of Aβ aggregates in patient's brain is a hallmark of Alzheimer's disease (AD). Therefore disaggregation and disruption provide potential therapeutic approaches to reduce, inhibit, and even reverse Aβ aggregation. The disaggregation/inhibition effect of the inhibitors applies generally to both Aβ40 and Aβ42 aggregations. Here we capture the atomic-level details of the interaction between Aβ40/Aβ42 and either natural tanshinone compound TS1 or its derivative TS0, and observe novel results by using molecular dynamics simulations...
April 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28406285/serotonin-and-serotonin-transporters-in-the-adrenal-medulla-a-potential-hub-for-modulation-of-the-sympathetic-stress-response
#11
Rebecca L Brindley, Mary Beth Bauer, Randy D Blakely, Kevin P M Currie
Serotonin (5-HT) is an important neurotransmitter in the central nervous system where it modulates circuits involved in mood, cognition, movement, arousal, and autonomic function. The 5-HT transporter (SERT; SLC6A4) is a key regulator of 5-HT signaling, and genetic variations in SERT are associated with various disorders including depression, anxiety, and autism. This review focuses on the role of SERT in the sympathetic nervous system. Autonomic/sympathetic dysfunction is evident in patients with depression, anxiety, and other diseases linked to serotonergic signaling...
April 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28368577/classics-in-chemical-neuroscience-aripiprazole
#12
Austen B Casey, Clinton E Canal
Aripiprazole was the first antipsychotic developed to possess agonist properties at dopamine D2 autoreceptors, a groundbreaking strategy that presented a new vista for schizophrenia drug discovery. The dopamine D2 receptor is the crucial target of all extant antipsychotics, and all developed prior to aripiprazole were D2 receptor antagonists. Extensive blockade of these receptors, however, typically produces extrapyramidal (movement) side effects, which plagued first-generation antipsychotics, such as haloperidol...
April 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28375612/sulpiride-amisulpride-thioridazine-and-olanzapine-interaction-with-model-membranes-thermodynamic-and-structural-aspects
#13
Piotr Skrobecki, Anna Chmielińska, Piotr Bonarek, Piotr Stepien, Anna Wisniewska-Becker, Marta Dziedzicka-Wasylewska, Agnieszka Polit
Neuroleptic drugs are widely applied in effective treatment of schizophrenia and related disorders. The lipophilic character of neuroleptics means that they tend to accumulate in the lipid membranes, impacting their functioning and processing. In this paper, the effect of four drugs, namely, thioridazine, olanzapine, sulpiride, and amisulpride, on neutral and negatively charged lipid bilayers was examined. The interaction of neuroleptics with lipids and the subsequent changes in the membrane physical properties was assessed using several complementary biophysical approaches (isothermal titration calorimetry, electron paramagnetic resonance spectroscopy, dynamic light scattering, and ζ potential measurements)...
April 12, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28368610/bax-activation-blocks-self-renewal-and-induces-apoptosis-of-human-glioblastoma-stem-cells
#14
Simona Daniele, Deborah Pietrobono, Barbara Costa, Mariateresa Giustiniano, Valeria La Pietra, Chiara Giacomelli, Giuseppe La Regina, Romano Silvestri, Sabrina Taliani, Maria Letizia Trincavelli, Federico Da Settimo, Ettore Novellino, Claudia Martini, Luciana Marinelli
Glioblastoma (GBM) is characterized by a poor response to conventional chemotherapeutic agents, attributed to the insurgence of drug resistance mechanisms and to the presence of a subpopulation of glioma stem cells (GSCs). GBM cells and GSCs present, among others, an overexpression of antiapoptotic proteins and an inhibition of pro-apoptotic ones, which help to escape apoptosis. Among pro-apoptotic inducers, the Bcl-2 family protein Bax has recently emerged as a promising new target in cancer therapy along with first BAX activators (BAM7, Compound 106, and SMBA1)...
April 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28378993/serotonin-dysfunction-aggressive-behavior-and-mental-illness-exploring-the-link-using-a-dimensional-approach
#15
Mirko Manchia, Bernardo Carpiniello, Flavia Valtorta, Stefano Comai
Aggressive individuals have higher rates of mental illness compared to non-aggressive individuals. Multiple factors, including psychosocial, genetic, and neurobiological determinants modulate the liability to both aggressive behavior and mental illness. Concerning the latter factors, multiple lines of evidence have shown a dysfunction in the serotonin (5-HT) system occurring in aggressive and in mentally ill individuals. In particular, reduced 5-HT activity has been associated with depression as well as with aggressive behavior, especially with impulsive aggression...
April 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28368571/recent-advances-in-the-realm-of-allosteric-modulators-for-opioid-receptors-for-future-therapeutics
#16
Michael Remesic, Victor J Hruby, Frank Porreca, Yeon Sun Lee
Opioids, and more specifically μ-opioid receptor (MOR) agonists such as morphine, have long been clinically used as therapeutics for severe pain states but often come with serious side effects such as addiction and tolerance. Many studies have focused on bringing about analgesia from the MOR with attenuated side effects, but its underlying mechanism is not fully understood. Recently, focus has been geared toward the design and elucidation of the orthosteric site with ligands of various biological profiles and mixed subtype opioid activities and selectivities, but targeting the allosteric site is an area of increasing interest...
April 7, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28324653/evaluation-of-brain-pharmacokinetic-and-neuropharmacodynamic-attributes-of-an-antiepileptic-drug-lacosamide-in-hepatic-and-renal-impairment-preclinical-evidence
#17
Baldeep Kumar, Manish Modi, Biman Saikia, Bikash Medhi
The knowledge of pharmacokinetic and pharmacodynamic properties of antiepileptic drugs is helpful in optimizing drug therapy for epilepsy. This study was designed to evaluate the pharmacokinetic and pharmacodynamic properties of lacosamide in experimentally induced hepatic and renal impairment in seizure animals. Hepatic or renal impairment was induced by injection of carbon tetrachloride or diclofenac sodium, respectively. After induction, the animals were administered a single dose of lacosamide. At different time points, maximal electroshock (MES) seizure recordings were made followed by isolation of plasma and brain samples for drug quantification and pharmacodynamic measurements...
April 6, 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
#18
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...
April 4, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28375605/raman-spectroscopic-signature-markers-of-dopamine-human-dopamine-transporter-interaction-in-living-cells
#19
Achut Prasad Silwal, Rajeev Yadav, Jon E Sprague, H Peter Lu
Dopamine (DA) controls many psychological and behavioral activities in the central nervous system (CNS) through interactions with the human dopamine transporter (hDAT) and dopamine receptors. The roles of DA in the function of the CNS are affected by the targeted binding of drugs to hDAT; thus, hDAT plays a critical role in neurophysiology and neuropathophysiology. An effective experimental method is necessary to study the DA-hDAT interaction and effects of variety of drugs like psychostimulants and anti-depressants that are dependent on this interaction...
April 4, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28375602/the-marine-guanidine-alkaloid-crambescidin-816-induces-calcium-influx-and-cytotoxicity-in-primary-cultures-of-cortical-neurons-through-glutamate-receptors
#20
Aida G Mendez, Andrea Boente Juncal, Siguara B L Silva, Olivier Paul Thomas, Víctor Martín Vázquez, Amparo Alfonso, Mercedes R Vieytes, Carmen Vale, Luis M Botana
Crambescidin 816 is a guanidine alkaloid produced by the sponge Crambe crambe with known antitumoral activity. While the information describing the effects of this alkaloid in central neurons is scarce, Cramb816 is known to block voltage dependent calcium channels being selective for L-type channels. Moreover, Cramb816 reduced neuronal viability through an unknown mechanism. Here, we aimed to describe the toxic activity of Cramb816 in cortical neurons. Since calcium influx is considered the main mechanism responsible for neuronal cell death, the effects of Cramb816 in the cytosolic calcium concentration of cortical neurons were studied...
April 4, 2017: ACS Chemical Neuroscience
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