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CNS & Neurological Disorders Drug Targets

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https://www.readbyqxmd.com/read/29336270/in-silico-ligand-based-identification-of-novel-acetylcholinesterase-inhibitors-against-alzheimer-s-disease-ad
#1
Mohammad Usman Mirza, Nazia Ikram, Nauman Mazhar, Kanzal Iman, Mehwish Riaz, Mohammad A Kamal
Alzheimer disease (AD) is a hot research topic currently across the world, characterized by the formation of β-amyloid plaques and neurofibrillary tangles. Inhibition of acetylcholinesterase (AChE) has gained much importance since the discovery of the involvement of peripheral anionic site (PAS) as an allosteric regulator of AChE. Progression of this neurodegenerative disorder causes a deficit in the cholinergic activity that leads towards cognitive decline. Therapeutic interventions in AD are largely focused upon AChE inhibitors designed essentially to prevent the loss of cholinergic function...
January 15, 2018: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29318979/role-of-epigenetics-and-oxidative-stress-in-gliomagenesis
#2
Edgar Rangel-Lopez, Yesennia Sanchez-Perez, Ernesto Soto-Reyes, Claudia Maria Garcia-Cuellar, Bernardo Cacho-Diaz, Abel Santamaria
Malignant gliomas constitute more than 49% of all central nervous system (CNS) tumors and exhibit very poor prognosis. Two main events involved with the progression of gliomas are the deregulation of genes by genetic events and cellular damage elicited by the formation of reactive oxygen species (ROS). In gliomas, epigenetic abnormalities implicated in the deregulation of DNA methylation, nucleosome rearrangement, and acetylation of histones have been depicted. The overproduction of ROS has been implicated in the promotion of these modifications...
January 10, 2018: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29318978/cognitive-rehabilitation-of-cerebellar-deficits
#3
Peter Marien, Kim van Dun, Frank Van Overwalle
During the past 3 decades numerous neurophysiological, neuroimaging, experimental and clinical studies have evidenced a crucial role for the cerebellum in cognitive, affective and behavioral functions. As a result of the acknowledged modulatory role of the cerebellum upon remote structures such as the cerebral cortex, cerebellar injury may give rise to a constellation of behavioral, affective and cognitive symptoms (Schmahmann's Syndrome). In sharp contrast to the wide range of therapeutical interventions to treat cognitive and affective disorders following cerebral cortical lesions and despite the consequences of Schmahmann's syndrome upon daily life activities, the literature is surprisingly only scantly documented with studies investigating the impact of cognitive therapies on cerebellar induced cognitive and affective disorders...
January 10, 2018: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29299992/development-of-a-nasal-donepezil-loaded-microemulsion-for-treatment-of-alzheimer-s-disease-in-vitro-and-ex-vivo-characterization
#4
Lupe Carolina Espinoza, Marisol Vacacela, Beatriz Clares, Maria Luisa Garcia, Maria Jose Fabrega, Ana Cristina Calpena
BACKGROUND: Donepezil (DPZ) is widely prescribed as a specific and reversible acetylcholinesterase inhibitor for the symptomatic treatment of mild to moderate Alzheimer's disease (AD). OBJECTIVE: Considering the therapeutic potential of DPZ and the advantages offered by the intranasal route as an alternative for drug administration, the aim of this study was the development and characterization of a DPZ microemulsion (ME) for nose-to-brain delivery. METHOD: The ME was developed by construction of pseudoternary phase diagrams and characterized by dynamic light scattering and transmission electron microscopy...
January 4, 2018: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29299991/crosstalk-between-gut-microbiota-and-the-central-nervous-system-in-multiple-sclerosis-strengths-weaknesses-opportunities-and-threats-analysis-of-the-use-of-an-experimental-model
#5
Carmen Padilla Del Campo, Isaac Tunez
No abstract text is available yet for this article.
January 3, 2018: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29268693/advances-in-therapies-of-cerebellar-disorders-immune-mediated-ataxias
#6
Marios Hadjivassiliou
The identification of an increasing number of immune mediated ataxias suggests that the cerebellum is often a target organ for autoimmune insults. The diagnosis of immune mediated ataxias remains challenging as there is significant clinical overlap between immune mediated and other forms of ataxia. Furthermore the classification of immune mediated ataxias requires further clarification particularly for those ataxias where no specific antigenic trigger and associated antibodies have been identified. Recognition of immune mediated ataxias remains imperative as therapeutic interventions can often be effective, although given the relative rarity of this entity, large-scale treatment trials may not be feasible...
December 20, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29268692/literature-evidence-and-arrive-assessment-on-neuroprotective-effects-of-flavonols-in-neurodegenerative-diseases-models
#7
Ana Carolina Bombardi Duarte, Maycon Giovanni Santana, Guilherme di Camilo Orfali, Carlos Tadeu Parisi, Denise Goncalves Priolli
Neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease and Huntington's disease, represent worldwide a major health problem with great financial impact. They are multifactorial diseases, hallmarked by similar pathogenesis that covers conditions such as oxidative stress, formation of free radicals, abnormal protein dynamics (degradation and aggregation), mitochondrial dysfunction, lipid peroxidation and cellular death or senescence. Flavonols are polyphenolic compounds, widely distributed in the plant kingdom and found in high concentrations in vegetables, fruits and teas...
December 20, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29268691/mambalgins-the-venom-origin-peptides-as-a-potentially-novel-group-of-analgesics-mini-review
#8
Maksymilian Aleksander Brzezicki, Przemyslaw Temistokles Zakowicz
BACKGROUND Despite a wide variety of current analgesia regimens, chronic pain is an incredibly difficult condition to treat. Its pathophysiology, initiation, development, and course involve a range of different receptors and transmitters. The acid-sensing ion channels (ASICs) are being attributed to an increasingly larger significance in pain aetiology. Over the last few years, the mechanism of ASICs action, their antagonists/agonists influence and clinical applications have been well described. However, the importance of this protein is significantly larger, not only in the perspective of pain management, but also in psychiatry of addiction or fear...
December 20, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29237386/the-combined-effects-of-%C3%AF-3-fatty-acids-and-nano-curcumin-supplementation-on-intercellular-adhesion-molecule-1-icam-1-gene-expression-and-serum-level-in-migraine-patients
#9
Neda Soveyd, Mina Abdolahi, Mahmoud Djalali, Mahsa Hatami, Abbas Tafakhori, Payam Sarraf, Niyaz Mohammadzadeh Honarvar
BACKGROUND: Migraine is an episodic headache that endothelial disorder and neuro inflammation basic. Intercellular Adhesion Molecule-1(ICAM-1) as an endothelial factor lead to adhesion of leukocytes to the walls of cerebral blood vessels which it's an important step in the inflammation process. Curcumin and omega-3 fatty acids by affecting on transcription factors can regulate the gene expression and serum level of ICAM-1.Thus we aimed to evaluate synergistic effects of ω-3 fatty acids and nano-curcumin on ICAM-1 gene expression and serum levels in migraine patients...
December 13, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29237385/systemic-administrations-of-antipsychotic-asenapine-pre-or-postnatal-does-not-induce-anxiety-like-behaviors-in-mice
#10
Maria Silvia Oliveira, Thais Souza Barbosa de Souza, Daniela Miranda Farias, Rozimeri Fatima Coletti, Jorge Aparecido de Barros, Carolina Gomes Carrilho, Susana Elisa Moreno, Eric Murillo Murillo Rodriguez, Sergio Machado, Andre Barciela Veras
Asenapine is an atypical antipsychotic approved by US Food and Drug Administration in 2009 and by European Medicines Agency in 2010 for schizophrenia and bipolar disorder treatment. Currently, many studies have been developed in an attempt to clarify and minimize the risks related to the use of psychotropic during pre/postnatal period on patients with a history of mental disorders. To this finality, the purpose of the following work was to test on animal models the impact of being exposed to this medication during perinatal period upon anxiety and exploration/emotionality of female mice's descendants submitting them, in adulthood, to the Open Field and Elevated Plus Maze test...
December 13, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29173188/innate-immune-surveillance-in-the-central-nervous-system-in-legionella-pneumophila-infection
#11
Pasqualina Lagana, Luca Soraci, Maria Elsa Gambuzza, Santi Delia
Innate immune response represents a common event in many neuroinflammatory diseases. The resident immune cells of the central nervous system (CNS) are capable of sensing and reacting to both infections and sterile trauma. Peripheral immune cell migration into CNS is regulated by the blood-brain barrier (BBB), although peripheral immune cells can invade CNS through meninges, choroid plexus, perivascular spaces, and cerebrospinal fluid. Consequently, in the brain immune reactions can be mediated by both resident and peripheral immune cells...
November 23, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29110629/commentary-endophenotypes-as-disease-modifiers-decoding-the-biology-of-alzheimer-s-by-genome-wide-association-studies
#12
A R Neelakandan, G K Rajanikant
No abstract text is available yet for this article.
November 6, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29090671/targeted-blockade-of-tarp-g8-associated-ampa-receptors-anticonvulsant-activity-with-the-selective-antagonist-ly3130481-cerc-611
#13
Jeffrey M Witkin, Douglas A Schober, Scott D Gleason, John T Catlow, Warren J Porter, Jon Reel, X Jin, J Hobbs, Donald Gehlert, Douglas L Gernert, Kevin M Gardinier, Akihiko S Kato, X Ping, J L Smith
6-[(1S)-1-[1-[5-(2-hydroxyethoxy)-2-pyridyl]pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one (LY3130481 or CERC-611) is a selective antagonist of AMPA receptors containing transmembrane AMPA receptor regulatory protein (TARP) g-8 that is under development for epilepsy. The present study provided a broad inquiry into its anticonvulsant properties. LY3130481 was anticonvulsant in multiple acute seizure provocation models in mice and rats. In addition, LY3130481 was effective against absence seizures in the GAERS genetic model and in the Frings mouse model...
November 1, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29076437/book-review-dendrites-third-edition
#14
Gislaine Z Réus
No abstract text is available yet for this article.
October 27, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29076436/low-dose-of-anisodine-hydrobromide-induced-neuroprotective-effects-in-chronic-cerebral-hypoperfusion-rats
#15
Dandan Chen, Xiaofang Xie, Qiuling Chen, Han Liu, Shiyang Zhang, Feng Wan, Hui Ao, Cheng Peng
BACKGROUND: Chronic cerebral hypoperfusion is a common pathophysiological state in various cerebrovascular diseases. Anisodine has been reported to exerts neuroprotective effects in cerebral ischemia/reperfusion(I/R) animal model. However, it is poorly understood whether anisodine hydrobromide, the hydrochloride format of anisodine, one of tropic alkanes alkaloids, processes the same neuroprotective effect on chronic cerebral hypoperfusion(CCH) rats. Herein, we designed a way to evaluate these issues...
October 26, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/29065845/identification-of-electrophysiological-changes-in-alzheimer-s-disease-a-microarray-based-transcriptomics-and-molecular-pathway-analysis-study
#16
Zeenat Mirza, Nisreen Rajeh
Involvement of amyloid beta and tau proteins in pathogenesis of Alzheimer's disease (AD) has been studied extensively. However, electrophysiological activity, and cellular processes like membrane transport are mostly unstudied. Electrophysiological processes provide a bridge between brain activity and cognition, and show promise as translatable biomarkers in preclinical and clinical applications. Biochemical imbalance leads to change in glutamate-based neurotransmission, antioxidant capacity, and in membrane polarization-repolarization events, eventually, resulting in AD...
October 23, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28982340/the-18-kda-translocator-protein-tspo-as-a-cns-drug-target-finding-our-way-through-the-neuroinflammation-fog
#17
Michaela D Filiou, Richard B Rabati, Manuel B Graeber
The 18-kDa translocator protein (TSPO) is located in the outer mitochondrial membrane where it is thought to co-regulate steroidogenesis, cellular bioenergetics as well as several other cellular processes. Originally discovered as a binding site for diazepam outside the CNS, notably in steroidogenic tissue and mononuclear phagocytes, the TSPO's historical designation was peripheral benzodiazepine receptor. Much of the recent interest in the TSPO is due to the observation that its regulation in the brain is associated with microglial activation...
October 4, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28969559/genetic-signatures-in-ischemic-stroke-focus-on-aspirin-resistance
#18
Anjana Munshi, Kanika Vasudeva, Pratibha Chaurasia, Sulena Singh
Stroke is one of the leading causes of death. There has been compelling evidence that stroke has a genetic component. Genetic variants not only influence susceptibility to stroke but have also been found to alter the response to pharmacological agents and influence the clinical outcome of the disease. Stroke patients are treated with antiplatelet drugs like aspirin and clopidogrel to prevent a secondary stroke. Inspite the fact that many new antiplatelet drugs have been developed; aspirin is still considered as a golden standard for the antiplatelet therapy...
October 2, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28933261/pharmacological-treatment-of-cognitive-symptoms-in-major-depressive-disorder
#19
Zihang Pan, Radu C Grovu, Danielle S Cha, Nicole E Carmona, Mehala Subramaniapillai, Margarita Shekotikhina, Carola Rong, Yena Lee, Roger S McIntyre
: Background: Cognitive dysfunction is a core transdiagnostic domain of Major Depressive Disorder (MDD) and is a principal determinant of functional recovery. However, it has been insufficiently targeted within the current therapeutic framework for MDD. OBJECTIVE: To highlight these unmet cognitive needs in MDD. METHODS: An article search was conducted using PubMed from inception to November 2016: Major Depressive Disorder (and/or variant) was cross-referenced with the following terms: antidepressants, augmentation, cognition, cognitive deficits, cognitive dysfunction, functional outcomes, mechanism of action, and treatment...
September 18, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28933260/older-and-newer-strategies-for-the-pharmacological-treatment-of-agitation-in-schizophrenia-and-bipolar-disorder
#20
Giovanni Amodeo, Andrea Fagiolini, Gabriele Sachs, Andreas Erfurth
BACKGROUND: Treatment of acute agitation in patients with bipolar disorder and schizophrenia is a multifaceted and dynamic task, which presents unique and complex challenges to healthcare providers. OBJECTIVE: To ascertain and describe which medications are best to use in agitated patients with schizophrenia or bipolar disorder Method: Selective review of current guidelines and of the literature pertaining to the treatment of agitation in patients with schizophrenia or bipolar disorder Results: Pharmacologic treatment of agitation should be based on an assessment of the most likely cause of the agitation...
September 18, 2017: CNS & Neurological Disorders Drug Targets
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