abstract：:Central norepinephrine (NE) and dopamine (DA) are involved in a variety of physiological functions and behaviors. Accumulating evidence suggests that NE neurons originating from the locus coeruleus (LC) innervate DA neurons of the ventral tegmental area (VTA) and influence VTA-DA neural activity. However, the underlyi...

journal_title：ACS chemical neuroscience

authors： Park JW,Bhimani RV,Park J

更新日期：2017-09-20 00:00:00

abstract：: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'...

journal_title：ACS chemical neuroscience

authors： R Cardoso B,Hare DJ,Lind M,McLean CA,Volitakis I,Laws SM,Masters CL,Bush AI,Roberts BR

更新日期：2017-07-19 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 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：:The gut is the largest producer of serotonin or 5-hydroxytryptamine (5-HT) in the human body, and 5-HT has been recognized as an important signaling molecule in the gut for decades. There are two distinct sources of enteric 5-HT. Mucosal 5-HT is predominantly produced by enterochromaffin (EC) cells of the gastrointest...

journal_title：ACS chemical neuroscience

authors： Shajib MS,Baranov A,Khan WI

更新日期：2017-05-17 00:00:00

abstract：: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 othe...

journal_title：ACS chemical neuroscience

authors： Huot P,Sgambato-Faure V,Fox SH,McCreary AC

更新日期：2017-05-17 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：:Depression, a major cause of disability worldwide, is characterized by a complex and heterogeneous symptomatology. With this respect, cognitive deterioration represents a major problem that has a strong impact on a patient's function. Thus, within the context of a depressive phenotype, it is important to characterize ...

journal_title：ACS chemical neuroscience

authors： Calabrese F,Brivio P,Gruca P,Lason-Tyburkiewicz M,Papp M,Riva MA

更新日期：2017-04-19 00:00:00

abstract：:Quaternary ammonium analogues of atropine that are unable to cross the blood-brain barrier are used to alleviate peripheral muscarinic toxicity in animal models of epilepsy produced by systemic administration of pilocarpine or diisopropylfluorophosphate (DFP). Currently, methylatropine is the most popular and potent o...

journal_title：ACS chemical neuroscience

authors： Rojas A,Ganesh T,Walker A,Dingledine R

更新日期：2017-04-19 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：: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：:Currently, anti-AD drug discovery using target-based approaches is extremely challenging due to unclear etiology of AD and absence of validated therapeutic protein targets. Neuronal death, regardless of causes, plays a key role in AD progression, and it is directly linked to neuroinflammation. Meanwhile, phenotypic sc...

journal_title：ACS chemical neuroscience

authors： Zhou W,Zhong G,Fu S,Xie H,Chi T,Li L,Rao X,Zeng S,Xu D,Wang H,Sheng G,Ji X,Liu X,Ji X,Wu D,Zou L,Tortorella M,Zhang K,Hu W

更新日期：2016-11-16 00:00:00

abstract：:The neurotransmitter dopamine is heavily implicated in intracranial self-stimulation (ICSS). Many drugs of abuse that affect ICSS behavior target the dopaminergic system, and optogenetic activation of dopamine neurons is sufficient to support self-stimulation. However, the patterns of phasic dopamine release during IC...

journal_title：ACS chemical neuroscience

authors： Rodeberg NT,Johnson JA,Bucher ES,Wightman RM

更新日期：2016-11-16 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：:The effect of the bis-sulfonated iron(III) corrole (1-Fe), a potent decomposition catalyst of reactive oxygen species, on rescuing SN4741 cells that were damaged by 6-hydroxydopamine (6-OHDA) was investigated as an in vitro model system for studying cell death of dopaminergic neurons in the substantia nigra. Important...

journal_title：ACS chemical neuroscience

authors： Soll M,Bar Am O,Mahammed A,Saltsman I,Mandel S,Youdim MB,Gross Z

更新日期：2016-10-19 00:00:00

abstract：:The efficacy of positive allosteric modulators (PAMs) of the metabotropic glutamate receptor 4 (mGlu4) in preclinical rodent models of Parkinson's disease has been established by a number of groups. Here, we report an advanced preclinically characterized mGlu4 PAM, N-(3-chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin...

journal_title：ACS chemical neuroscience

authors： Engers DW,Blobaum AL,Gogliotti RD,Cheung YY,Salovich JM,Garcia-Barrantes PM,Daniels JS,Morrison R,Jones CK,Soars MG,Zhuo X,Hurley J,Macor JE,Bronson JJ,Conn PJ,Lindsley CW,Niswender CM,Hopkins CR

更新日期：2016-09-21 00:00:00

abstract：:Several pharmacophore models have been proposed for 5-HT2A serotonin receptor antagonists. These typically consist of two aromatic/hydrophobic moieties separated by a given distance from each other, and from a basic amine. Although specified distances might vary, the models are relatively similar in their general cons...

journal_title：ACS chemical neuroscience

authors： Younkin J,Gaitonde SA,Ellaithy A,Vekariya R,Baki L,Moreno JL,Shah S,Drossopoulos P,Hideshima KS,Eltit JM,González-Maeso J,Logothetis DE,Dukat M,Glennon RA

更新日期：2016-09-21 00:00:00

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：: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：: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：:γ-Secretase is a multiprotein complex that catalyzes intramembrane proteolysis associated with Alzheimer's disease and cancer. Here, we have developed potent sulfonamide clickable photoaffinity probes that target γ-secretase in vitro and in cells by incorporating various photoreactive groups and walking the clickable ...

journal_title：ACS chemical neuroscience

authors： Crump CJ,Murrey HE,Ballard TE,Am Ende CW,Wu X,Gertsik N,Johnson DS,Li YM

更新日期：2016-08-17 00:00:00

abstract：:Amyloid-β (Aβ), the main constituent in senile plaques found in the brain of patients with Alzheimer's disease (AD), is considered as a causative factor in AD pathogenesis. The clinical examination of the brains of patients with AD has demonstrated that caspase-3 colocalizes with senile plaques. Cellular studies have ...

journal_title：ACS chemical neuroscience

authors： Chang YJ,Linh NH,Shih YH,Yu HM,Li MS,Chen YR

更新日期：2016-08-17 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：:The aggregation of amyloid-β (Aβ) peptide induced by Cu(2+) is a key factor in development of Alzheimer's disease (AD), and metal ion chelation therapy enables treatment of AD. Three CQi (i = 1, 2, and 3 with R = H, Cl, and NO2, respectively) drugs had been verified experimentally to be much stronger inhibitors than t...

journal_title：ACS chemical neuroscience

authors： Dong M,Li H,Hu D,Zhao W,Zhu X,Ai H

更新日期：2016-05-18 00:00:00

abstract：:Accumulating evidence suggested that soluble oligomeric β-amyloid protein (Aβ) exerts diverse roles in neuronal cell death, neuroinflammation, oxidative stress, and the eventual dementia associated with Alzheimer's disease (AD). Developing an agent with multiple properties may be a reasonable strategy for the treatmen...

journal_title：ACS chemical neuroscience

authors： Yang S,Liu W,Lu S,Tian YZ,Wang WY,Ling TJ,Liu RT

更新日期：2016-04-20 00:00:00

abstract：:While selective-serotonin reuptake inhibitor (SSRI) antidepressants are commonly prescribed in the treatment of depression, their use during pregnancy leads to fetal drug exposures. According to recent reports, such exposures could affect fetal development and long-term offspring health. A central question is how preg...

journal_title：ACS chemical neuroscience

authors： Velasquez JC,Goeden N,Herod SM,Bonnin A

更新日期：2016-03-16 00:00:00

abstract：:3-Iodobenzoyl naltrexamine (IBNtxA) is a potent analgesic belonging to the pharmacologically diverse 6β-amidoepoxymorphinan group of opioids. We present the synthesis and pharmacological evaluation of five analogs of IBNtxA. The scaffold of IBNtxA was modified by removing the 14-hydroxy group, incorporating a 7,8 doub...

journal_title：ACS chemical neuroscience

authors： Váradi A,Marrone GF,Eans SO,Ganno ML,Subrath JJ,Le Rouzic V,Hunkele A,Pasternak GW,McLaughlin JP,Majumdar S

更新日期：2015-11-18 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：:1-Methyl-4-phenylpyridinium (MPP+) induces microglial activation and degeneration of dopaminergic (DAergic) neurons. Donepezil is a well-known acetylcholinesterase inhibitor used clinically to treat cognitive dysfunction in Alzheimer's disease (AD). In the present study, we tested the hypothesis that MPP+ promotes mic...

journal_title：ACS chemical neuroscience

authors： Chen T,Hou R,Xu S,Wu C

更新日期：2015-10-21 00:00:00

abstract：:This work describes the use of fluorescence correlation spectroscopy (FCS) and a novel amyloid-binding fluorescent probe, ARCAM 1, to monitor the aggregation of the Alzheimer's disease-associated amyloid β-peptide (Aβ). ARCAM 1 exhibits a large increase in fluorescence emission upon binding to Aβ assemblies, making it...

journal_title：ACS chemical neuroscience

authors： Guan Y,Cao KJ,Cantlon A,Elbel K,Theodorakis EA,Walsh DM,Yang J,Shah JV

更新日期：2015-09-16 00:00:00

abstract：:The distribution and density of neurons within the brain poses many challenges when making quantitative measurements of neurotransmission in the extracellular space. A volume neurotransmitter is released into the synapse during chemical communication and must diffuse through the extracellular space to an implanted sen...

journal_title：ACS chemical neuroscience

authors： Atcherley CW,Laude ND,Monroe EB,Wood KM,Hashemi P,Heien ML

更新日期：2015-09-16 00:00:00

abstract：:Amyloid fibrils are the most distinct components of the plaques associated with various neurodegenerative diseases. Kinetic studies of amyloid fibril formation shed light on the microscopic mechanisms that underlie this process as well as the contributions of internal and external factors to the interplay between diff...

journal_title：ACS chemical neuroscience

authors： Nasir I,Linse S,Cabaleiro-Lago C

更新日期：2015-08-19 00:00:00

abstract：:In our efforts to develop hybrid compounds of curcumin and melatonin as potential disease-modifying agents for Alzheimer's disease (AD), a potent lead hybrid compound, Z-CM-I-1, has been recently identified and biologically characterized in vitro. In this work, we report the in vivo effects of Z-CM-I-1 on AD pathologi...

journal_title：ACS chemical neuroscience

authors： Gerenu G,Liu K,Chojnacki JE,Saathoff JM,Martínez-Martín P,Perry G,Zhu X,Lee HG,Zhang S

更新日期：2015-08-19 00:00:00

abstract：:Small hydrophobic oligomers of aggregation-prone proteins are thought to be generically toxic. Here we examine this view by perturbing an early folding contact between Phe19 and Leu34 formed during the aggregation of Alzheimer's amyloid-β (Aβ40) peptide. We find that even conservative single mutations altering this in...

journal_title：ACS chemical neuroscience

authors： Das AK,Rawat A,Bhowmik D,Pandit R,Huster D,Maiti S

更新日期：2015-08-19 00:00:00

abstract：:Ever since the discovery of its neurite growth promoting activity in sympathetic and sensory ganglia, nerve growth factor (NGF) became the prototype of the large family of neurotrophins. The use of primary cultures and clonal cell lines has revealed several distinct actions of NGF and other neurotrophins. Among severa...

journal_title：ACS chemical neuroscience

authors： Travaglia A,Pietropaolo A,Di Martino R,Nicoletti VG,La Mendola D,Calissano P,Rizzarelli E

更新日期：2015-08-19 00:00:00

abstract：:The light emission chemistry of firefly luciferase can be harnessed to reveal otherwise invisible biological processes occurring in the brains of live animals. Though powerful, the need for the luciferase substrate D-luciferin to traverse the blood-brain barrier poses limitations on the sensitivity and interpretation ...

journal_title：ACS chemical neuroscience

authors： Mofford DM,Miller SC

更新日期：2015-08-19 00:00:00

abstract：:Alzheimer's disease (AD) is the most common form of dementia affecting 35 million individuals worldwide. Current AD treatments provide only brief symptomatic relief. It is therefore urgent to replace this symptomatic approach with a curative one. Increasing serotonin signaling as well as developing molecules that enha...

journal_title：ACS chemical neuroscience

authors： Claeysen S,Bockaert J,Giannoni P

更新日期：2015-07-15 00:00:00

abstract：:Stereotypy (e.g., repetitive hand waving) is a key phenotype of autism spectrum disorder, Fragile X and Rett syndromes, and other neuropsychiatric disorders, and its severity correlates with cognitive and attention deficits. There are no effective treatments, however, for stereotypy. Perturbation of serotonin (5-HT) n...

journal_title：ACS chemical neuroscience

authors： Canal CE,Felsing DE,Liu Y,Zhu W,Wood JT,Perry CK,Vemula R,Booth RG

更新日期：2015-07-15 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：:Protein function depends on both protein structure and amino acid (aa) sequence. Here we show that modular features of both structure and function can be quantified economically from the aa sequences alone for the small (40,42 aa) plaque-forming (aggregative) amyloid beta fragments. Some edge and center features of th...

journal_title：ACS chemical neuroscience

authors： Phillips JC

更新日期：2015-05-20 00:00:00