Characterization and first human investigation of FIBT, a novel fluorinated Aβ plaque neuroimaging PET radioligand.

abstract：:The finding that acetylcholinesterase (AChE) colocalizes with β-amyloid (Aβ) and promotes and accelerates Aβ aggregation has renewed an intense interest in developing new multifunctional AChE inhibitors as potential disease-modifying drugs for Alzheimer's therapy. To this end, we have developed a new class of selectiv...

journal_title：ACS chemical neuroscience

authors： Zheng H,Youdim MB,Fridkin M

更新日期：2010-11-17 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：: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：:The melanocortin system regulates an array of diverse physiological functions including pigmentation, feeding behavior, energy homeostasis, cardiovascular regulation, sexual function, and steroidogenesis. Endogenous melanocortin agonist ligands all possess the minimal messaging tetrapeptide sequence His-Phe-Arg-Trp. B...

journal_title：ACS chemical neuroscience

authors： Todorovic A,Lensing CJ,Holder JR,Scott JW,Sorensen NB,Haskell-Luevano C

更新日期：2018-11-21 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：: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：:The amyloid beta (Aβ) fibrillar aggregate is the hallmark of Alzheimer's disease (AD). Disassembling preformed fibril or inhibiting Aβ aggregation is considered as a therapeutic strategy for AD. Increasing evidence shows that green tea extracts, epigallocatechin-3-gallate (EGCG, containing an extra gallic acid ester g...

journal_title：ACS chemical neuroscience

authors： Zhan C,Chen Y,Tang Y,Wei G

更新日期：2020-06-17 00:00:00

abstract：:Glutamate is the major excitatory transmitter in the mammalian CNS, exerting its effects through both ionotropic and metabotropic glutamate receptors. The metabotropic glutamate receptors (mGlus) belong to family C of the G-protein-coupled receptors (GPCRs). The eight mGlus identified to date are classified into three...

journal_title：ACS chemical neuroscience

authors： Lindsley CW,Bates BS,Menon UN,Jadhav SB,Kane AS,Jones CK,Rodriguez AL,Conn PJ,Olsen CM,Winder DG,Emmitte KA

更新日期：2011-08-17 00:00:00

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：:Pentameric glycine receptors (GlyRs) couple agonist binding to activation of an intrinsic ion channel. Substitution of the R271 residue impairs agonist-induced activation and is associated with the human disease hyperekplexia. On the basis of a homology model of the α1 GlyR, we substituted residues in the vicinity of ...

journal_title：ACS chemical neuroscience

authors： Lynagh T,Kunz A,Laube B

更新日期：2013-11-20 00:00:00

abstract：:Opium is the latex from the opium poppy Papaver somniferum L., which humankind has utilized since ancient Mesopotamia all the way to modern times. Opium used to be surrounded in divine mystery or magic-like abilities and was given to cure a wide variety of diseases until its analgesic, antitussive, and antidiarrheal p...

journal_title：ACS chemical neuroscience

authors： Presley CC,Lindsley CW

更新日期：2018-10-17 00:00:00

abstract：:Relapse to cocaine dependence, even after extended abstinence, involves a number of liability factors including impulsivity (predisposition toward rapid, unplanned reactions to stimuli without regard to negative consequences) and cue reactivity (sensitivity to cues associated with cocaine-taking which can promote coca...

journal_title：ACS chemical neuroscience

authors： Cunningham KA,Anastasio NC,Fox RG,Stutz SJ,Bubar MJ,Swinford SE,Watson CS,Gilbertson SR,Rice KC,Rosenzweig-Lipson S,Moeller FG

更新日期：2013-01-16 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：: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：: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：:The present experiments employed in vivo microdialysis to characterize the effects of commonly used endocannabinoid clearance inhibitors on basal and depolarization-induced alterations in interstitial endocannabinoid levels in the nucleus accumbens of rat brain. Compounds targeting the putative endocannabinoid transpo...

journal_title：ACS chemical neuroscience

authors： Wiskerke J,Irimia C,Cravatt BF,De Vries TJ,Schoffelmeer AN,Pattij T,Parsons LH

更新日期：2012-05-16 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：: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：:α-Synuclein (α-syn) is a 140-amino acid protein that plays a central role in the pathogenesis of Parkinson's disease (PD) and other synucleinopathies. However, the molecular determinants that are responsible for triggering and/or propagating α-syn aggregation and toxicity remain poorly understood. Several studies have...

journal_title：ACS chemical neuroscience

authors： Lu Y,Prudent M,Fauvet B,Lashuel HA,Girault HH

更新日期：2011-11-16 00:00:00

abstract：:On the basis of the drug-repositioning and redeveloping strategy, first-generation dual-target inhibitors of acetylcholinesterase (AChE) and phosphodiesterase 5 (PDE5) have been recently reported as a potentially novel therapeutic method for the treatment of Alzheimer's disease (AD), and the lead compound 2 has proven...

journal_title：ACS chemical neuroscience

authors： Ni W,Wang H,Li X,Zheng X,Wang M,Zhang J,Gong Q,Ling D,Mao F,Zhang H,Li J

更新日期：2018-07-18 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

abstract：:A new generation of ligands designed to interact with the α-helix/β-strand discordant region of the amyloid-β peptide (Aβ) and to counteract its oligomerization is presented. These ligands are designed to interact with and stabilize the Aβ central helix (residues 13-26) in an α-helical conformation with increased inte...

journal_title：ACS chemical neuroscience

authors： Honcharenko D,Juneja A,Roshan F,Maity J,Galán-Acosta L,Biverstål H,Hjorth E,Johansson J,Fisahn A,Nilsson L,Strömberg R

更新日期：2019-03-20 00:00:00

abstract：:Chondroitin sulfate proteoglycans (CSPGs) are the most abundant components of glial scar formed after severe traumatic brain injury as well as spinal cord injury and play a crucial inhibitory role in axonal regeneration by selective contraction of filopodia of the growth cone of sprouting neurites. Healing of central ...

journal_title：ACS chemical neuroscience

authors： Mukherjee N,Nandi S,Garg S,Ghosh S,Ghosh S,Samat R,Ghosh S

更新日期：2020-02-05 00:00:00

abstract：:The present study was performed to investigate the possible role of protein kinase C (PKC) in morphine tolerance at spinal levels of rats. Intrathecal injection of 10 μg of morphine induced increases in the hindpaw withdrawal latency (HWL) to noxious thermal and mechanical stimulation in rats. After intrathecal inject...

journal_title：ACS chemical neuroscience

authors： Jin WY,Yu LC

更新日期：2010-02-17 00:00:00

abstract：:Recreational consumption of synthetic cannabinoid receptor agonists (SCRAs) is a growing crisis in public health in many parts of the world. AMB-FUBINACA is a member of this class of drugs and is responsible for a large proportion of SCRA-related toxicity both in New Zealand and internationally. Strikingly, little is ...

journal_title：ACS chemical neuroscience

authors： Finlay DB,Manning JJ,Ibsen MS,Macdonald CE,Patel M,Javitch JA,Banister SD,Glass M

更新日期：2019-10-16 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：: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：:Previous work in our laboratories has identified a series of peptidomimetic 2-pyridone molecules as modulators of alpha-synuclein (α-syn) fibrillization in vitro. As a first step toward developing molecules from this scaffold as positron emission tomography imaging agents, we were interested in evaluating their blood-...

journal_title：ACS chemical neuroscience

authors： Cairns AG,Vazquez-Romero A,Mahdi Moein M,Ådén J,Elmore CS,Takano A,Arakawa R,Varrone A,Almqvist F,Schou M

更新日期：2018-11-21 00:00:00

abstract：:The sensory nervous system controls cardiovascular homeostasis via capsaicin-sensitive neurons that release calcitonin gene-related peptide (CGRP), which subsequently activates CGRP receptors. How this perivascular CGRPergic discharge is modulated, nevertheless, remains unclear. In pithed rats, systemic vasodilation i...

journal_title：ACS chemical neuroscience

authors： Manrique-Maldonado G,Altamirano-Espinoza AH,Rivera-Mancilla E,Hernández-Abreu O,Villalón CM

更新日期：2019-08-21 00:00:00

abstract：:Effective therapies for glioblastoma multiforme (GBM) are not currently available. A small molecule has been identified using fragment-based drug-discovery guided by NMR that targets important protein-protein interactions controlling GBM invasion and pathogenicity. This first generation drug displays excellent pharmac...

journal_title：ACS chemical neuroscience

authors： Das SK,Sarkar D,Cavenee WK,Emdad L,Fisher PB

更新日期：2019-03-20 00:00:00