Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

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：: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：:The delivery of specific genes into neurons offers a potent approach for treatment of diseases as well as for the study of neuronal cell biology. Here we investigated the capabilities of cationic amino acid based lipid assemblies to act as nonviral gene delivery vectors in primary cultured neurons. An arginine-based l...

journal_title：ACS chemical neuroscience

authors： Aoshima Y,Hokama R,Sou K,Sarker SR,Iida K,Nakamura H,Inoue T,Takeoka S

更新日期：2013-12-18 00:00:00

abstract：:A hallmark of Alzheimer's disease (AD) is the formation of senile plaques comprised of the β-amyloid (Aβ) peptide. Aβ fibrillization is a complex nucleation-dependent process involving a variety of metastable intermediate aggregates and features the formation of inter- and intramolecular salt bridges involving lysine ...

journal_title：ACS chemical neuroscience

authors： Pilkington AW 4th,Schupp J,Nyman M,Valentine SJ,Smith DM,Legleiter J

更新日期：2020-01-15 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：:Neuronal cytotoxicity observed in Alzheimer's disease (AD) is linked to the aggregation of β-amyloid peptide (Aβ) into toxic forms. Increasing evidence points to oligomeric materials as the neurotoxic species, not Aβ fibrils; disruption or inhibition of Aβ self-assembly into oligomeric or fibrillar forms remains a via...

journal_title：ACS chemical neuroscience

authors： Bett CK,Ngunjiri JN,Serem WK,Fontenot KR,Hammer RP,McCarley RL,Garno JC

更新日期：2010-09-15 00:00:00

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：: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：:The 5-HT2A receptor (5-HT2AR) and 5-HT2CR are localized to the same neurons within the medial prefrontal cortex (mPFC), which regulates executive function, decision-making, and reward-guided learning and memory processes. The 5-HT2AR and 5-HT2CR coimmunoprecipitate in the mPFC of male Sprague-Dawley rats, while in vit...

journal_title：ACS chemical neuroscience

authors： Price AE,Sholler DJ,Stutz SJ,Anastasio NC,Cunningham KA

更新日期：2019-07-17 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：: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：: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：:In humans, genetic defects of the synthesis or regeneration of tetrahydrobiopterin (BH4), an essential cofactor in hydroxylation reactions, are associated with severe neurological disorders. The diagnosis of these conditions relies on the determination of BH4, dihydrobiopterin (BH2), and dihydroneopterin (NH2) in cere...

journal_title：ACS chemical neuroscience

authors： Guibal P,Lévêque N,Doummar D,Giraud N,Roze E,Rodriguez D,Couderc R,Billette De Villemeur T,Moussa F

更新日期：2014-07-16 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：:Of the free-living amoebae (FLA) Naegleria fowleri, Balamuthia mandrillaris, and Acanthamoeba spp. are known to cause encephalitis. Coined with the term "brain-eating amoebae" (BEA), infection of the central nervous system with FLA has a high mortality rate. A combination of diagnostic delay, lack of new drug developm...

journal_title：ACS chemical neuroscience

authors： Baig AM,Khaleeq A,Nazim F

更新日期：2020-08-19 00:00:00

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：: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：: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：:Baicalein, a flavonoid derived from the roots of Scutellariae baicalensis Georgi, has shown health benefits for an array of human diseases including dementia. The senescence-accelerated mouse prone 8 (SAMP8) strain is extensively used as a senile dementia model. To further investigate the effects of baicalein in SAMP8...

journal_title：ACS chemical neuroscience

authors： Gao L,Li J,Zhou Y,Huang X,Qin X,Du G

更新日期：2018-07-18 00:00:00

abstract：:Modulation of the neuropeptide S (NPS) system has been linked to a variety of CNS disorders such as panic disorder, anxiety, sleeping disorders, asthma, obesity, PTSD, and substance abuse. In this study, a series of diphenyltetrahydro-1H-oxazolo[3,4-α]pyrazin-3(5H)-ones were synthesized and evaluated for antagonist ac...

journal_title：ACS chemical neuroscience

authors： Hassler C,Zhang Y,Gilmour B,Graf T,Fennell T,Snyder R,Deschamps JR,Reinscheid RK,Garau C,Runyon SP

更新日期：2014-08-20 00:00:00

abstract：:Krokodil is the street name for a homemade mixture that has been used as a cheap substitute for heroin. The main active substance in krokodil is desomorphine, an opioid that is 10 times more potent than morphine. Krokodil use began in Russia and Ukraine but has spread throughout several countries in Europe and North A...

journal_title：ACS chemical neuroscience

authors： Alves EA

更新日期：2020-09-17 00:00:00

abstract：:Calcitonin gene-related peptide (α-CGRP) released from perivascular sensory nerves induces decreases in diastolic blood pressure (DBP). Experimentally, this can be shown by spinal thoracic (T9-T12) electrical stimulation of these afferent fibers. Because ergotamine inhibits these neurogenic vascular responses and disp...

journal_title：ACS chemical neuroscience

authors： González-Hernández A,Marichal-Cancino BA,Lozano-Cuenca J,MaassenVanDenBrink A,Villalón CM

更新日期：2019-07-17 00:00:00

abstract：:The Chinese mitten crab (Eriocheir sinensis) is a commercially important crab in China and is usually managed at high stocking densities. Agonistic behavior directly impacts crab integrity, survival, and growth and results in economic losses. In the present study, we evaluated the modulatory effects of serotonin (5-HT...

journal_title：ACS chemical neuroscience

authors： Pang YY,Song YM,Zhang L,Song XZ,Zhang C,Lv JH,He L,Cheng YX,Yang XZ

更新日期：2019-11-20 00:00:00

abstract：:No universally efficacious therapy exists for chronic pain, a disease affecting one-fifth of the global population. An overreliance on the prescription of opioids for chronic pain despite their poor ability to improve function has led to a national opioid crisis. In 2018, the NIH launched a Helping to End Addiction Lo...

journal_title：ACS chemical neuroscience

authors： Shan Z,Cai S,Yu J,Zhang Z,Vallecillo TGM,Serafini MJ,Thomas AM,Pham NYN,Bellampalli SS,Moutal A,Zhou Y,Xu GB,Xu YM,Luo S,Patek M,Streicher JM,Gunatilaka AAL,Khanna R

更新日期：2019-06-19 00:00:00

abstract：:Alzheimer's disease (AD) is a slow-progressing disease of the brain characterized by symptoms such as impairment of memory and other cognitive functions. AD is associated with an inflammatory process that involves astrocytes and microglial cells, among other components. Astrocytes are the most abundant type of glial c...

journal_title：ACS chemical neuroscience

authors： De Vita T,Albani C,Realini N,Migliore M,Basit A,Ottonello G,Cavalli A

更新日期：2019-03-20 00:00:00

abstract：:The nonmedical (i.e., recreational) misuse of synthetic cannabinoids (SCs) is a worldwide public health problem. When compared to cannabis, the misuse of SCs is associated with a higher incidence of serious adverse effects, suggesting the possible involvement of noncannabinoid sites of action. Here, we find that, unli...

journal_title：ACS chemical neuroscience

authors： Yano H,Adhikari P,Naing S,Hoffman AF,Baumann MH,Lupica CR,Shi L

更新日期：2020-05-20 00:00:00

abstract：:The development of a noninvasive method for the detection of Alzheimer's disease is of high current interest, which can be critical in early diagnosis and in guiding treatment of the disease. The aggregates of β-amyloid are a pathological hallmark of Alzheimer's disease. Carbohydrates such as gangliosides have been sh...

journal_title：ACS chemical neuroscience

authors： Kouyoumdjian H,Zhu DC,El-Dakdouki MH,Lorenz K,Chen J,Li W,Huang X

更新日期：2013-04-17 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：: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：: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