A Difluoroboron β-Diketonate Probe Shows "Turn-on" Near-Infrared Fluorescence Specific for Tau Fibrils.

abstract：:Indole and indazole synthetic cannabinoids (SCs) featuring l-valinate or l-tert-leucinate pendant group have recently emerged as prevalent recreational drugs, and their use has been associated with serious adverse health effects. Due to the limited pharmacological data available for these compounds, 5F-AMBICA, 5F-AMB,...

journal_title：ACS chemical neuroscience

authors： Banister SD,Longworth M,Kevin R,Sachdev S,Santiago M,Stuart J,Mack JB,Glass M,McGregor IS,Connor M,Kassiou M

更新日期：2016-09-21 00:00:00

abstract：:Recent clinical approvals of brain imaging radiotracers targeting amyloid-β provided clinicians the tools to detect and confirm Alzheimer's disease pathology without autopsy or biopsy. While current imaging agents are effective in postsymptomatic Alzheimer's patients, there is much room for improvement in earlier diag...

journal_title：ACS chemical neuroscience

authors： Neo Shin N,Jeon H,Jung Y,Baek S,Lee S,Yoo HC,Bae GH,Park K,Yang SH,Han JM,Kim I,Kim Y

更新日期：2019-06-19 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：: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：:Selective potentiators of glutamate response at metabotropic glutamate receptor subtype 5 (mGluR5) have exciting potential for the development of novel treatment strategies for schizophrenia. A total of 1,382 compounds with positive allosteric modulation (PAM) of the mGluR5 glutamate response were identified through h...

journal_title：ACS chemical neuroscience

authors： Mueller R,Rodriguez AL,Dawson ES,Butkiewicz M,Nguyen TT,Oleszkiewicz S,Bleckmann A,Weaver CD,Lindsley CW,Conn PJ,Meiler J

更新日期：2010-04-21 00:00:00

abstract：:In this article, we have demonstrated the in vivo efficacy of D-512 and D-440 in a 6-OHDA-induced unilaterally lesioned rat model experiment, a Parkinson's disease animal model. D-512 is a novel highly potent D2/D3 agonist, and D-440 is a novel highly selective D3 agonist. We evaluated the neuroprotective properties o...

journal_title：ACS chemical neuroscience

authors： Santra S,Xu L,Shah M,Johnson M,Dutta A

更新日期：2013-10-16 00:00:00

abstract：:The 5-HT2C receptor has emerged as a promising target in the treatment of a variety of central nervous system disorders. We have first identified aporphines as a new class of 5-HT2C receptor agonists. Structure-activity relationship results indicate that the aporphine core may be required for 5-HT2C receptor activity,...

journal_title：ACS chemical neuroscience

authors： Mao Q,Zhang B,Li W,Tian S,Shui W,Ye N

更新日期：2020-02-19 00:00:00

abstract：:Ca(2+)/calmodulin-dependent protein kinase IIα (CaMKIIα) autophosphorylation at Thr286 and Thr305/Thr306 regulates kinase activity and modulates subcellular targeting and is critical for normal synaptic plasticity and learning and memory. Here, a mass spectrometry-based approach was used to identify Ca(2+)-dependent a...

journal_title：ACS chemical neuroscience

authors： Baucum AJ 2nd,Shonesy BC,Rose KL,Colbran RJ

更新日期：2015-04-15 00:00:00

abstract：:As the first drug to see widespread use for the treatment of attention deficit hyperactivity disorder (ADHD), methylphenidate was the forerunner and catalyst to the modern era of rapidly increasing diagnosis, treatment, and medication development for this condition. During its often controversial history, it has vario...

journal_title：ACS chemical neuroscience

authors： Wenthur CJ

更新日期：2016-08-17 00:00:00

abstract：:An intracerebral hemorrhage (ICH) is a devastating stroke that results in high mortality and significant disability in survivors. Unfortunately, the underlying mechanisms of this injury are not yet fully understood. After the primary (mechanical) trauma, secondary degenerative events contribute to ongoing cell death i...

journal_title：ACS chemical neuroscience

authors： Hackett MJ,DeSouza M,Caine S,Bewer B,Nichol H,Paterson PG,Colbourne F

更新日期：2015-05-20 00:00:00

abstract：:Several antidepressants increase adult hippocampal neurogenesis (ahNG) in rodents, primates, and, potentially, humans. This effect may at least partially account for their therapeutic activity. The availability of antidepressants whose mechanism of action involves different neurotransmitter receptors represents an opp...

journal_title：ACS chemical neuroscience

authors： Bortolotto V,Mancini F,Mangano G,Salem R,Xia E,Del Grosso E,Bianchi M,Canonico PL,Polenzani L,Grilli M

更新日期：2017-09-20 00:00:00

abstract：:Parkinson's disease (PD) is the most widespread form of dementia where there is an age related degeneration of dopaminergic neurons in the substantia nigra region of the brain. Accumulation of α-synuclein (αS) protein aggregate, mitochondrial dysfunction, oxidative stress, and neuronal cell death are the pathological ...

journal_title：ACS chemical neuroscience

authors： Kundu P,Das M,Tripathy K,Sahoo SK

更新日期：2016-12-21 00:00:00

abstract：:The discovery of haloperidol catalyzed a breakthrough in our understanding of the biochemical basis of schizophrenia, improved the treatment of psychosis, and facilitated deinstitutionalization. In doing so, it solidified the role for chemical neuroscience as a means to elucidate the molecular underpinnings of complex...

journal_title：ACS chemical neuroscience

authors： Tyler MW,Zaldivar-Diez J,Haggarty SJ

更新日期：2017-03-15 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 l-enantiomer is the predominant type of amino acid in all living systems. However, d-amino acids, once thought to be "unnatural", have been found to be indigenous even in mammalian systems and increasingly appear to be functioning in essential biological and neurological roles. Both d- and l-amino acid levels in t...

journal_title：ACS chemical neuroscience

authors： Weatherly CA,Du S,Parpia C,Santos PT,Hartman AL,Armstrong DW

更新日期：2017-06-21 00:00:00

abstract：:G protein-coupled receptor 55 (GPR55) is highly expressed in brain and peripheral nervous system. Originally deorphanized as a cannabinoid receptor, recently GPR55 has been described as a lysophospholipid-responsive receptor, specifically toward lysophosphatidylinositol and lysophosphatidyl-β-d-glucoside (LysoPtdGlc)....

journal_title：ACS chemical neuroscience

authors： Guy AT,Kano K,Ohyama J,Kamiguchi H,Hirabayashi Y,Ito Y,Matsuo I,Greimel P

更新日期：2019-01-16 00:00:00

abstract：:Aβ peptides, the main protein components of Alzheimer's disease (AD) plaques, derive from a proteolytic cleavage of the amyloid precursor protein. Due to heterogeneous cleavage sites, a series of Aβ peptides, including the major and widely studied species Aβ1-40 (Aβ40) and Aβ1-42 (Aβ42), are produced. In addition to t...

journal_title：ACS chemical neuroscience

authors： Tomaselli S,Pagano K,D'Arrigo C,Molinari H,Ragona L

更新日期：2017-04-19 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：:Pyramidal cells and astrocytes have differential susceptibility to oxygen-glucose deprivation and reperfusion (OGD-RP). It is known that excessive reactive oxygen species (ROS) in mitochondria initiates cell death, while glutathione (GSH) is one of the major defenses against ROS. Although it is known that astrocytes c...

journal_title：ACS chemical neuroscience

authors： Yin B,Barrionuevo G,Weber SG

更新日期：2018-04-18 00:00:00

abstract：:Fast scan cyclic voltammetry in brain slices (slice voltammetry) has been used over the last several decades to increase substantially our understanding of the complex local regulation of dopamine release and uptake in the striatum. This technique is routinely used for the study of changes that occur in the dopamine s...

journal_title：ACS chemical neuroscience

authors： Ferris MJ,Calipari ES,Yorgason JT,Jones SR

更新日期：2013-05-15 00:00:00

abstract：:Tau proteins are hyperphosphorylated at common sites in their N- and C-terminal domains in at least three neurodegenerative diseases, Parkinson, dementia with Lewy bodies, and Alzheimer's, suggesting specific pathology but general mechanism. Full-length human tau filament comprises a rigid core and a two-layered fuzzy...

journal_title：ACS chemical neuroscience

authors： Xu L,Zheng J,Margittai M,Nussinov R,Ma B

更新日期：2016-05-18 00:00:00

abstract：:Natural environments contain numerous volatile compounds emanating from a large number of sources, and the survival of many animals depends on their ability to segregate odors of interest within complex odorous scenes. In a recent paper, we described how the ability of mice to detect odors within mixtures depends on t...

journal_title：ACS chemical neuroscience

authors： Rokni D,Murthy VN

更新日期：2014-10-15 00:00:00

abstract：:Neurons choose growth pathways with half hearted reluctance, behavior that may be appropriate to maintain fixed long lasting connections but not to regenerate them. We now recognize that intrinsic brakes on regrowth are widely expressed in these hesitant neurons and include classical tumor suppressor molecules. Here, ...

journal_title：ACS chemical neuroscience

authors： Zochodne DW

更新日期：2014-08-20 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：:As the major psychoactive agent in opium and direct precursor for heroin, morphine is a historically critical molecule in chemical neuroscience. A structurally complex phenanthrene alkaloid produced by Papaver somniferum, morphine has fascinated chemists seeking to disentangle pharmacologically beneficial analgesic ef...

journal_title：ACS chemical neuroscience

authors： Devereaux AL,Mercer SL,Cunningham CW

更新日期：2018-10-17 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：: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：:MMP-9 plays a detrimental role in the pathology of several neurological diseases and, thus, represents an important target for intervention. The water-soluble prodrug ND-478 is hydrolyzed to the active MMP-9 inhibitor ND-322, which in turn is N-acetylated to the even more potent metabolite ND-364. We used a sensitive ...

journal_title：ACS chemical neuroscience

authors： Song W,Peng Z,Gooyit M,Suckow MA,Schroeder VA,Wolter WR,Lee M,Ikejiri M,Cui J,Gu Z,Chang M

更新日期：2013-08-21 00:00:00

abstract：:An in vitro model of ischemic cerebral stroke [oxygen-glucose deprivation (OGD) for 6 h followed by 24 h reoxygenation (R)] with PC12 cells increases Ca(2+) influx by upregulating native L-type Ca(2+) channels and reactive oxygen species (ROS) generation. This reactive oxygen species generation and increase in intrace...

journal_title：ACS chemical neuroscience

authors： Agrawal M,Kumar V,Singh AK,Kashyap MP,Khanna VK,Siddiqui MA,Pant AB

更新日期：2013-02-20 00:00:00

abstract：:Interactions between superoxide dismutase-1 (SOD1) and lipid membranes might be directly involved in the toxicity and intercellular propagation of aggregated SOD1 in amyotrophic lateral sclerosis (ALS), but the chemical details of lipid-SOD1 interactions and their effects on SOD1 aggregation remain unclear. This paper...

journal_title：ACS chemical neuroscience

authors： Rasouli S,Abdolvahabi A,Croom CM,Plewman DL,Shi Y,Shaw BF

更新日期：2018-07-18 00:00:00