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Current Neuropharmacology

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https://www.readbyqxmd.com/read/28183245/ykl-40-as-a-potential-biomarker-and-a-possible-target-in-therapeutic-strategies-of-alzheimer-s-disease
#1
Paweł Muszyński, Magdalena Groblewska, Agnieszka Kulczyńska-Przybik, Alina Kułakowska, Barbara Mroczko
BACKGROUND: Growing body of evidence suggests that pathogenesis of Alzheimer's disease (AD), a progressing neurodegenerative condition, is not limited to the neuronal compartment, but also involves various immunological mechanisms. Insoluble Aβ aggregates in the brain can induce the activation of microglia, resulting in synthesis of proinflammatory mediators, which further can stimulate astrocytic expression of YKL-40. Therefore, the aim of the current review is to present up-to-date data about the role of YKL-40 as a biomarker of AD as well as the possibility of therapeutic strategies targeting neuroinflammation...
February 8, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28093977/the-amyloid-cascade-hypothesis-in-alzheimer-s-disease-it-s-time-to-change-our-mind
#2
Roberta Ricciarelli, Ernesto Fedele
Since its discovery in 1984, the beta amyloid peptide has treaded the boards of neurosciences as the star molecule in Alzheimer's disease pathogenesis. In the last decade, however, this vision has been challenged by evidence-based medicine showing the almost complete failure of clinical trials that experimented anti-amyloid therapies with great hopes. Moreover, data have accumulated which clearly indicates that this small peptide plays a key role in the physiological processes of memory formation. In the present review, we will discuss the different aspects of the amyloid cascade hypothesis, highlighting its pros and cons, and we will analyse the results of the therapeutic approaches attempted to date that should change the direction of Alzheimer's disease research in the future...
January 16, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28093976/chemoinformatics-profiling-of-the-chromone-nucleus-as-a-mao-b-a2aar-dual-binding-scaffold
#3
Maykel Cruz-Monteagudo, Fernanda Borges, M Natália D S Cordeiroc, Aliuska Morales Helguerad, Eduardo Tejerab, Cesar Paz-Y-Miñob, Aminael Sánchez-Rodrígueze, Yunier Perera-Sardiñaf, Yunierkis Perez-Castillo
BACKGROUND: In the context of the current drug discovery efforts to find disease modifying therapies for Parkinson´s disease (PD) the current single target strategy has proved inefficient. Consequently, the search for multi-potent agents is attracting more and more attention due to the multiple pathogenetic factors implicated in PD. Multiple evidences points to the dual inhibition of the monoamine oxidase B (MAO-B), as well as adenosine A2A receptor (A2AAR) blockade, as a promising approach to prevent the neurodegeneration involved in PD...
January 16, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28088912/melatonin-as-a-therapeutic-resource-for-inflammatory-visual-diseases
#4
Marcos L Aranda, María Florencia González Fleitas, Hernán Dieguez, Agustina Iaquinandi, Pablo H Sande, Damián Dorfman, Ruth E Rosenstein
BACKGROUND: Uveitis and optic neuritis are prevalent ocular inflammatory diseases, and highly damaging ocular conditions. Both diseases are currently treated with corticosteroids, but they do not have adequate efficacy and are often associated with severe side effects. Thus, uveitis and optic neuritis remain a challenging field to ophthalmologists and a significant public health concern. OBJECTIVE: This review summarizes findings showing the benefits of a treatment with melatonin in experimental models of these inflammatory ocular diseases...
January 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28088914/diverse-functions-and-mechanisms-of-pericytes-in-ischemic-stroke
#5
Shuai Yang, Huijuan Jin, Yiyi Zhu, Yan Wan, Lingqiang Zhu, Bo Hu
Pericytes are mural cells embedded in the basement membrane of microvessels. Because of such a unique position in the blood-brain barrier (BBB) and neurovascular unit (NVU), they receive, orchestrate and process signals from their neighboring cells to generate diverse neurovascular functions, including regulation of capillary hemodynamics, BBB permeability, clearance of toxic metabolites, angiogenesis, neuroinflammation and stem cell activity. During the different stages of ischemic stroke, pericytes play different roles: 1) On the hyperacute phase of stroke, pericytes constriction and death may be a cause of the no-reflow phenomenon in brain capillaries; 2) During the acute phase, pericytes detach from microvessels and participate in inflammatory-immunological response, resulting in the BBB damage and brain edema...
January 12, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28088913/a-comparative-study-of-short-term-efficacy-of-aripiprazole-and-risperidone-in-schizophrenia
#6
P B Sajeev Kumar, Ravi S Pandey, Jagadisha Thirthali, P T Siva Kumar, C Naveen Kumar
Objective To compare the short term anti-schizophrenic efficacy and side effect profile of aripiprazole with risperidone. Methodology The study was a non-randomized, naturalistic, rater blinded, prospective, 8-12 weeks, comparative trial between risperidone and aripiprazole in patients with schizophrenia. Patients already getting treatment with aripiprazole (10 to 30 mg/day) or risperidone (3 to 8mg/day) are recruited. Mini International Neuropsychiatric Interview (MINI) Plus, Positive and Negative Syndrome Scale (PANSS), Abnormal Involuntary Movement Scale (AIMS), Simpson Angus Scale (SAS), Udvalg for Klinske Undersogelser (UKU) Scale, Clinical Global Impression-severity scales were administered by principal investigator on the day of recruitment...
January 12, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28067172/fusing-docking-scoring-functions-improves-the-virtual-screening-performance-for-discovering-parkinson-s-disease-dual-target-ligands
#7
Yunierkis Perez-Castillo, Aliuska Morales Helguera, M Natália D S Cordeiro, Eduardo Tejera, Cesar Paz-Y-Miño, Aminael Sánchez-Rodríguez, Fernanda Borges, Maykel Cruz-Monteagudo
Virtual methodologies have become essential components of the drug discovery pipeline. Specifically, structure-based drug design methodologies exploit the 3D structure of molecular targets to discover new drug candidates through molecular docking. Recently, dual target ligands of the Adenosine A2A Receptor and Monoamine Oxidase B enzyme have been proposed as effective therapies for the treatment of Parkinson's disease. To the best of our knowledge, no theoretical study has been devoted to developing structure-based virtual screening methodologies for the discovery of dual A2AAR antagonists and MAO-B inhibitors...
January 9, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28042767/advantages-of-structure-based-drug-design-approaches-in-neurological-disorders
#8
Murali Aarthy, Umesh Panwar, Chandrabose Selvaraj, Sanjeev Kumar Singh
The nerve impulse that function during abnormal or due in illness may due to several genetic factors, metabolic, biological conditions or environmental components denominated as Neuro-biological disorders. This illness occurs mostly due to the innumerable biological modifications that alters the mechanistic condition of the brain. As per current update, more than a millions of people around the world are suffering through various kinds of neurological disorders. In case, 50 million people with Epilepsy, 35 million with dementia, mainly included Alzheimer's disease and the rest of other cases with Parkinson's, Migraine and Stroke...
2, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28034283/in-silico-studies-revealed-multiple-neurological-targets-for-the-antidepressant-molecule-ursolic-acid
#9
Rajeev K Singla, Luciana Scotti, Ashok K Dubey
BACKGROUND: Ursolic acid, a bioactive pentacyclic triterpenoid had been evaluated for its interaction with the neurological targets associated with antidepressant drugs. Current study was to mechanistically analyze the probable site of action for ursolic acid on the target proteins. METHODS: Ursolic acid has been docked with monoamine oxidase isoforms: MAO-A and MAO-B, LeuT (homologue of SERT, NET, DAT) and Human C-terminal CAP1 using GRIP docking methodology. RESULTS: Results revealed its non-selective antidepressant action with strong binding affinity towards LeuT and MAO-A proteins, which was found to be comparable with the reference ligands like chlorgyline, clomipramine, sertraline and deprenyl / selegiline...
December 29, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/28031015/melatonin-pharmacology-functions-and-therapeutic-benefits
#10
Sylvie Tordjman, Sylvie Chokron, Richard Delorme, Annaëlle Charrier, Eric Bellissant, Nemat Jaafari, Claire Fougerou
Melatonin synchronizes central but also peripheral oscillators (fetal adrenal gland, pancreas, liver, kidney, heart, lung, fat, gut, etc.), allowing temporal organization of biological functions through circadian rhythms in relation to periodic environmental changes and therefore adaptation of the individual to his/her internal and external environment. Measures of melatonin are considered the best peripheral indices of human circadian timing. First, the pharmacology of melatonin (biosynthesis and circadian rhythms, pharmacokinetics and mechanisms of action) is described, allowing a better understanding of the short and long term effects of melatonin following its immediate or prolonged release...
December 28, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/28029073/exploring-optic-nerve-axon-regeneration
#11
Hong-Jiang Li, Zhao-Liang Sun, Xi-Tao Yang, Liang Zhu, Dong-Fu Feng
Traumatic optic nerve (ON) injury is a leading cause of irreversible visual impairment worldwide. To date, neither pharmacological nor surgical interventions are sufficient to halt or reverse the progression of visual loss. Axon regeneration is critical for functional recovery of vision following ON injury. After ON injury, retinal ganglion cells (RGCs) axons usually fail to regrow and instead die back, leading to the death of the RGCs and subsequently causing the functional loss of vision. However, the detailed molecular mechanisms underlying axon regeneration after ON injury remain poorly understood...
December 27, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/28000553/new-psychoactive-substances-nps-a-new-global-issue-neuropharmacological-chemical-and-toxicological-aspects
#12
Simona Pichini, Francesco P Busardo, Roberta Pacifici, Pascal Kintz
No abstract text is available yet for this article.
December 20, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27964705/biological-drugs-in-guillain-barr%C3%A3-syndrome-an-update
#13
Nazgol Motamed-Gorji, Nassim Matin, Omidreza Tabatabaie, Piero Pavone, Catia Romano, Raffaele Falsaperla, Giovanna Vitaliti
BACKGROUND: Guillain-Barré Syndrome (GBS) is currently considered the most common global cause of acute flaccid paralysis. Currently, standard therapy for Guillain-Barré Syndrome includes intravenous immunoglobulin or plasma exchange. Despite medical advances regarding these treatments many patients treated with them do not reach full recovery. Therefore, during last decades several biological agents have attracted the attentions from researchers and various studies have investigated their role in Guillain-Barré Syndrome...
December 13, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27964704/common-sar-derived-from-linear-and-non-linear-qsar-studies-on-ache-inhibitors-used-in-the-treatment-of-alzheimer-s-disease
#14
Babitha Pallikkara Pulikkal, Sahila Mohammed Marunnan, Srinivas Bandaru, Mukesh Yadav, Anuraj Nayarisseri, Sivanpillai Sureshkumar
Two different sets of AChE inhibitors, dataset-I (30 compounds) and dataset-II (20 compounds) were investigated through MLR aided linear and SVM aided non-linear QSAR models. The obtained QSAR models were found statistically fit, stable and predictive on validation scales. These QSAR models were further investigated for their common structure-activity relationship in terms of overlapping molecular descriptors selection. Atomic mass weighted 3D Morse descriptors (MATS5m) and Radial Distribution Function (RDF045m) descriptors were found in common SAR for both the datasets...
December 13, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27964703/implications-of-epigenetic-mechanisms-and-their-targets-in-cerebral-ischemia-model
#15
Priya Jhelum, Bhanu Chandra Karisetty, Arvind Kumar, Sumana Chakravarty
Understanding the complexities associated with ischemic condition and identifying therapeutic targets in ischemia is a continued challenging in stroke biology. Emerging evidence reveals potential involvement of epigenetic mechanisms in the incident and outcome of stroke, suggesting novel therapeutic options of targeting different molecules related to epigenetic regulation. This review summarizes our current understanding of ischemia pathophysiology, describes various in vivo and in vitro models of ischemia, and examines epigenetic modifications associated with ischemic condition...
December 13, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27928949/from-leflunomide-to-teriflunomide-drug-development-and-immunosuppressive-oral-drugs-in-the-treatment-of-multiple-sclerosis
#16
Lilian Aly, Bernhard Hemmer, Thomas Korn
Immunosuppressive drugs have been used in the treatment of multiple sclerosis (MS) for a long time. Today, the increased number of approved substances and the possibility of an oral availability of some immunomodulators improve the therapeutic repertory and increase patient satisfaction and compliance. Teriflunomide is indicated as first line oral disease modifying therapy (DMT) in relapsing-remitting MS (RRMS). Its immunosuppressive capacity results from an inhibition of de novo pyrimidine synthesis in rapidly proliferating lymphocytes...
December 8, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27928948/revisiting-antipsychotic-induced-akathisia-current-issues-and-prospective-challenges
#17
Haitham Salem, Caesa Nagpal, Teresa Pigott, Antonio Lucio Teixeira
Akathisia continues to be a significant challenge in current neurological and psychiatric practice. Prompt and accurate detection is often difficult and there is a lack of consensus concerning the neurobiological basis of akathisia. No definitive treatment has been established for akathisia despite numerous preclinical and clinical studies. With these issues in mind, we reviewed antipsychotic-induced akathisia including its clinical presentation, proposed underlying pathophysiology, and an update of potential treatment strategies...
December 8, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27919210/three-dimensional-modelling-of-the-voltage-gated-sodium-ion-channel-from-anopheles-gambiae-reveals-spatial-clustering-of-evolutionarily-conserved-acidic-residues-at-the-extracellular-sites
#18
Rithvik S Vinekar, Ramanathan Sowdhamini
The eukaryotic voltage-gated sodium channel(e-Nav) is a large asymmetric transmembrane protein with important functions concerning neurological function. No structure has been resolved at high resolution for this protein. A homology model of the transmembrane and extracellular regions of an Anopheles gambiae para-like channel with emphasis on the pore entrance has been constructed, based upon the templates provided by a prokaryotic sodium channel and a potassium two-pore channel. The latter provides a template for the extracellular regions, which are located above the entrance to the pore, which is likely to open at a side of a dome formed by these loops...
December 5, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27908258/neurotoxicity-induced-by-mephedrone-an-up-to-date-review
#19
Flaminia Pantano, Roberta Tittarelli, Giulio Mannocchi, Roberta Pacifici, Alessandro di Luca, Francesco Paolo Busardò, Enrico Marinelli
Mephedrone is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. The aim of this review was to examine the emerging scientific literature on the possible mephedrone-induced neurotoxicity, yet not well defined due to the limited number of experimental studies, mainly carried on animal models. Relevant scientific articles were identified from international literature databases (Medline, Scopus, etc...
November 30, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/28125955/editorial-thematic-selection-spinal-neuropharmacological-agents-for-the-management-of-pain
#20
EDITORIAL
Rui V Duarte, Jon H Raphael, Sam Eldabe
No abstract text is available yet for this article.
2017: Current Neuropharmacology
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