Novel Tadalafil Derivatives Ameliorates Scopolamine-Induced Cognitive Impairment in Mice via Inhibition of Acetylcholinesterase (AChE) and Phosphodiesterase 5 (PDE5).

abstract：:Cognitive dysfunctions, including impaired attention, learning, memory, and problem solving, occur in psychiatric diseases, such as depression, and are a hallmark of aging. Altered GABAergic signaling is similarly reported across these conditions, but therapeutic approaches are limited by pan-receptor activities of be...

journal_title：ACS chemical neuroscience

authors： Prevot TD,Li G,Cook JM,Sibille E

更新日期：2019-05-15 00:00:00

abstract：:Serotonin (5-HT) is a key player in many physiological processes in both the adult organism and developing embryo. One of the mechanisms for 5-HT-mediated effects is covalent binding of 5-HT to the target proteins catalyzed by transglutaminases (serotonylation). Despite the implication in a variety of physiological pr...

journal_title：ACS chemical neuroscience

authors： Ivashkin E,Melnikova V,Kurtova A,Brun NR,Obukhova A,Khabarova MY,Yakusheff A,Adameyko I,Gribble KE,Voronezhskaya EE

更新日期：2019-08-21 00:00:00

abstract：:The transporters for the neurotransmitters serotonin and dopamine (SERT and DAT, respectively) are targets for drugs used in the treatment of mental disorders and widely used drugs of abuse. Studies of prokaryotic homologues have advanced our structural understanding of SERT and DAT, but it still remains enigmatic whe...

journal_title：ACS chemical neuroscience

authors： Andersen J,Ladefoged LK,Kristensen TN,Munro L,Grouleff J,Stuhr-Hansen N,Kristensen AS,Schiøtt B,Strømgaard K

更新日期：2016-10-19 00:00:00

abstract：:We previously reported on the synthesis of substituted phenyl-4-hydroxy-1-piperidyl indole analogues with nanomolar affinity at D2 dopamine receptors, ranging from 10- to 100-fold selective for D2 compared to the D3 dopamine receptor subtype. More recently, we evaluated a panel of aripiprazole analogues, identifying s...

journal_title：ACS chemical neuroscience

authors： Luedtke RR,Mishra Y,Wang Q,Griffin SA,Bell-Horner C,Taylor M,Vangveravong S,Dillon GH,Huang RQ,Reichert DE,Mach RH

更新日期：2012-12-19 00:00:00

abstract：:Deltorphins are naturally occurring peptides produced by the skin of the giant monkey frog (Phyllomedusa bicolor). They are δ-opioid receptor-selective agonists. Herein, we report the design and synthesis of a peptide, Tyr-d-Ala-(pI)Phe-Glu-Ile-Ile-Gly-NH2 3 (GATE3-8), based on the [d-Ala(2)]deltorphin II template, wh...

journal_title：ACS chemical neuroscience

authors： Pescatore R,Marrone GF,Sedberry S,Vinton D,Finkelstein N,Katlowitz YE,Pasternak GW,Wilson KR,Majumdar S

更新日期：2015-06-17 00:00:00

abstract：:In vivo fast-scan cyclic voltammetry provides high-fidelity recordings of electrically evoked dopamine release in the rat striatum. The evoked responses are suitable targets for numerical modeling because the frequency and duration of the stimulus are exactly known. Responses recorded in the dorsal and ventral striatu...

journal_title：ACS chemical neuroscience

authors： Walters SH,Taylor IM,Shu Z,Michael AC

更新日期：2014-09-17 00:00:00

abstract：:Tropomyosin receptor kinases (TrkA/B/C) are critically involved in the development of the nervous system, in neurological disorders as well as in multiple neoplasms of both neural and non-neural origins. The development of Trk radiopharmaceuticals would offer unique opportunities toward a more complete understanding o...

journal_title：ACS chemical neuroscience

authors： Bernard-Gauthier V,Aliaga A,Aliaga A,Boudjemeline M,Hopewell R,Kostikov A,Rosa-Neto P,Thiel A,Schirrmacher R

更新日期：2015-02-18 00:00:00

abstract：:Botulinum neurotoxin (BoNT), the etiological agent that causes the neuroparalytic disease botulism, has become a highly studied drug target in light of the potential abuse of this toxin as a weapon of bioterrorism. In particular, small molecule inhibitors of the light chain metalloprotease of BoNT serotype A have rece...

journal_title：ACS chemical neuroscience

authors： Capek P,Zhang Y,Barlow DJ,Houseknecht KL,Smith GR,Dickerson TJ

更新日期：2011-06-15 00:00:00

abstract：:Alcohol abuse is a chronic disease characterized by the consumption of alcohol at a level that interferes with physical and mental health and causes serious and persistent changes in the brain. Lipid metabolism is of particular interest due to its high concentration in the brain. Lipids are the main component of cell ...

journal_title：ACS chemical neuroscience

authors： Roux A,Jackson SN,Muller L,Barbacci D,O'Rourke J,Thanos PK,Volkow ND,Balaban C,Schultz JA,Woods AS

更新日期：2016-08-17 00:00:00

abstract：:The aggregation of α-synuclein (α-Syn) has been implicated strongly in Parkinson's disease (PD). The intrinsically disordered nature of α-Syn makes this protein prone to self-association or heteroassociation with another protein or lipid. While conformational fluctuation and free radical chemistry have been shown to p...

journal_title：ACS chemical neuroscience

authors： Ghosh S,Mahapatra A,Chattopadhyay K

更新日期：2019-03-20 00:00:00

abstract：:The permeation of the potassium ion (K+) through the selectivity filter (SF) of the large conductance Ca2+-activated potassium (Slo1) channel remains an interesting question to study. Although the mode of K+ entering and leaving the SF has been revealed, the mechanism of K+ passing through the SF is still not clear. I...

journal_title：ACS chemical neuroscience

authors： Guo J,Tan Z,Ji Y

更新日期：2019-08-21 00:00:00

abstract：:Carboranes have been extensively investigated as potential drugs for the treatment of malignant human brain tumors by boron neutron capture therapy (BNCT). This noninvasive treatment modality utilizes compounds containing the nonradioactive isotope 10B which has a high propensity to capture slow neutrons. In response,...

journal_title：ACS chemical neuroscience

authors： He T,Chittur SV,Musah RA

更新日期：2019-03-20 00:00:00

abstract：:Amyloid-beta (Aβ) peptide misfolds into fibrillary aggregates (β-sheet) and is deposited as amyloid plaques in the cellular environment, which severely damages intraneuronal connections leading to Alzheimer's disease (AD) pathogenesis. Furthermore, neurons are rich in tubulin/microtubules, and the intracellular networ...

journal_title：ACS chemical neuroscience

authors： Mondal P,Das G,Khan J,Pradhan K,Mallesh R,Saha A,Jana B,Ghosh S

更新日期：2019-05-15 00:00:00

abstract：:Several lines of evidence suggest the presence of severe acute respiratory coronavirus-2 (SARS-CoV-2) in wastewater. The use of sewage water for irrigation is common in many developing countries, and it is only partially treated in the majority of countries with less than 10% of collected wastewater receiving any form...

journal_title：ACS chemical neuroscience

authors： Siddiqui R,Khamis M,Ibrahim T,Khan NA

更新日期：2020-10-07 00:00:00

abstract：:Development of pharmacological tools for the ionotropic glutamate receptors (iGluRs) is imperative for the study and understanding of the role and function of these receptors in the central nervous system. We report the synthesis of 18 analogues of (2 S,3 R)-2-carboxy-3-pyrrolidine acetic acid (3a), which explores the...

journal_title：ACS chemical neuroscience

authors： Poulie CBM,Alcaide A,Krell-Jørgensen M,Larsen Y,Astier E,Bjørn-Yoshimoto WE,Yi F,Syrenne JT,Storgaard M,Nielsen B,Frydenvang KA,Jensen AA,Hansen KB,Pickering DS,Bunch L

更新日期：2019-06-19 00:00:00

abstract：:Metabolic adaptation to stress is a crucial yet poorly understood phenomenon, particularly in the central nervous system (CNS). The ability to identify essential metabolic events which predict neuronal fate in response to injury is critical to developing predictive markers of outcome, for interpreting CNS spectroscopi...

journal_title：ACS chemical neuroscience

authors： McKenzie JR,Palubinsky AM,Brown JE,McLaughlin B,Cliffel DE

更新日期：2012-07-18 00:00:00

abstract：:Amyloid formation and neuroinflammation are major features of Alzheimer's disease pathology. Proinflammatory mediator S100A9 was shown to act as a link between the amyloid and neuroinflammatory cascades in Alzheimer's disease, leading together with Aβ to plaque formation, neuronal loss and memory impairment. In order ...

journal_title：ACS chemical neuroscience

authors： Iashchishyn IA,Gruden MA,Moskalenko RA,Davydova TV,Wang C,Sewell RDE,Morozova-Roche LA

更新日期：2018-06-20 00:00:00

abstract：:Alzheimer's disease is characterized by pathological aggregation of protein tau and amyloid-β peptides, both of which are considered to be toxic to neurons. Naturally occurring dietary flavonoids have received considerable attention as alternative candidates for Alzheimer's therapy taking into account their antiamyloi...

journal_title：ACS chemical neuroscience

authors： Baptista FI,Henriques AG,Silva AM,Wiltfang J,da Cruz e Silva OA

更新日期：2014-02-19 00:00:00

abstract：:Post-translational modifications of proteins are ubiquitous in living organisms, as they enable an accurate control of the interactions of these macromolecules. For mechanistic studies, it would be highly advantageous to be able to produce in vitro post-translationally modified proteins with site-specificity. Here, we...

journal_title：ACS chemical neuroscience

authors： Lindstedt PR,Taylor RJ,Bernardes GJL,Vendruscolo M

更新日期：2021-01-19 00:00:00

abstract：:Aggregation of hyperphosphorylated tau is the hallmark of several tauopathies, including Alzheimer's disease (AD). Although the mechanism underlying tau-associated neuronal damage remains unclear, it is believed that tau hyperphosphorylation is one of the key features in disease progression. A recent study demonstrate...

journal_title：ACS chemical neuroscience

authors： Tripathi T,Prakash J,Shav-Tal Y

更新日期：2019-01-16 00:00:00

abstract：:No selective drugs exist, and we have been designing, synthesizing, and evaluating multitarget-directed ligands since the beginning of modern medicinal chemistry, without knowing it, most possibly. The challenge to discover the efficient Multi-Target Small Molecules (MTSMs) for Alzheimer's disease (AD) therapy implies...

journal_title：ACS chemical neuroscience

authors： Oset-Gasque MJ,Marco-Contelles J

更新日期：2018-03-21 00:00:00

abstract：:Autoantibodies to Parkinson's disease (PD) amyloidogenic protein, α-synuclein, were recognized as a prospective biomarker for early disease diagnostics, yet there is inconsistency in previous reports, potentially related to PD status. Therefore, plasma and cerebrospinal fluid (CSF) of the cross-sectional cohort of 60 ...

journal_title：ACS chemical neuroscience

authors： Horvath I,Iashchishyn IA,Forsgren L,Morozova-Roche LA

更新日期：2017-06-21 00:00:00

abstract：:The glycine receptor (GlyR) is a ligand-activated chloride channel, whose mutations are the major cause of hereditary hyperekplexia. The hyperekplexia-causing R271Q mutation, which is located at the extracellular outer mouth of the channel pore, dramatically impairs the GlyR function manifesting a reduced sensitivity ...

journal_title：ACS chemical neuroscience

authors： Han L,Shan Q

更新日期：2020-10-21 00:00:00

abstract：: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 isorhynchophyll...

journal_title：ACS chemical neuroscience

authors： Li Q,Niu C,Zhang X,Dong M

更新日期：2018-03-21 00:00:00

abstract：:Large aggregates of misfolded α-synuclein inside neuronal cells are the hallmarks of Parkinson's disease. The protein's natural function and its supposed toxicity, however, are believed to be closely related to its interaction with cell and vesicle membranes. Upon this interaction, the protein folds into an α-helical ...

journal_title：ACS chemical neuroscience

authors： Hähl H,Möller I,Kiesel I,Campioni S,Riek R,Verdes D,Seeger S

更新日期：2015-03-18 00:00:00

abstract：:Myasthenia gravis (MG) is an autoimmune T cell-dependent B cell-mediated disorder of the neuromuscular junction (NMJ) characterized by fluctuating skeletal muscle weakness, most commonly attributed to pathogenic autoantibodies against postsynaptic nicotinic acetylcholine receptors (AChRs). Although MG pathogenesis is ...

journal_title：ACS chemical neuroscience

authors： Angelopoulou E,Paudel YN,Piperi C

更新日期：2020-03-04 00:00:00

abstract：:Extensive experimental and computational studies have suggested that multiple Zn(2+) binding modes in amyloid β (Aβ) peptides could exist simultaneously. However, consistent results have not been obtained for the effects of Zn(2+) binding on Aβ structure, dynamics, and kinetics in particular. Some key questions such a...

journal_title：ACS chemical neuroscience

authors： Xu L,Wang X,Wang X

更新日期：2013-11-20 00:00:00

abstract：:Manganese (Mn) may foster aggregation of alpha-synuclein (αSyn) contributing to the pathogenesis of PD. Here, we examined the influence of αSyn overexpression on distribution and oxidation states of Mn in frozen-hydrated primary midbrain neurons (PMNs) by synchrotron-based X-ray fluorescence (XRF) and X-ray absorption...

journal_title：ACS chemical neuroscience

authors： Dučić T,Carboni E,Lai B,Chen S,Michalke B,Lázaro DF,Outeiro TF,Bähr M,Barski E,Lingor P

更新日期：2015-10-21 00:00:00

abstract：:Amyloid-β (Aβ) self-assembly into cross-β amyloid fibrils is implicated in a causative role in Alzheimer's disease pathology. Uncertainties persist regarding the mechanisms of amyloid self-assembly and the role of metastable prefibrillar aggregates. Aβ fibrils feature a sheet-turn-sheet motif in the constituent β-stra...

journal_title：ACS chemical neuroscience

authors： Doran TM,Anderson EA,Latchney SE,Opanashuk LA,Nilsson BL

更新日期：2012-03-21 00:00:00

abstract：:Glioblastoma multiforme, a type of deadly brain cancer, originates most commonly from astrocytes found in the brain. Current multimodal treatments for glioblastoma minimally increase life expectancy, but significant advancements in prognosis have not been made in the past few decades. Here we investigate cellular repr...

journal_title：ACS chemical neuroscience

authors： Lee C,Robinson M,Willerth SM

更新日期：2018-12-19 00:00:00