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https://www.readbyqxmd.com/read/29226687/validation-of-a-new-scoring-scale-for-behavioral-assessment-of-l-dopa-induced-dyskinesia-in-the-rat-a-new-tool-for-early-decision-making-in-drug-development
#1
Simon Loiodice, Anne-Sophie Denibaud, Wendy Deffains, Magali Alix, Pierre Montagne, Marine Seffals, Christophe Drieu La Rochelle
The 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated non-human primate (NHP) has been described as the most translatable model for experimental reproduction of L-dopa-induced dyskinesia (LID). However, from a drug discovery perspective, the risk associated with investment in this type of model is high due to the time and cost. The 6-hydroxydopamine (6-OHDA) rat dyskinesia model is recommended for testing compounds but relies on onerous, and non-standard behavioral rating scales. We sought to develop a simplified and sensitive method aiming at assessing LID in the rat...
December 11, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29210473/binding-pathway-analysis-of-influenza-virus-m2-channel-blockers-by-metadynamics-simulation
#2
Yuri Sakai, Atsushi Kawaguchi, Kyosuke Nagata, Takatsugu Hirokawa
M2 protein of influenza A virus is a proton channel spanning the viral envelope. This proton channel activity is required for uncoating of viral particles and equilibrating the pH across the trans-Golgi apparatus to prevent a conformational change of hemagglutinin. Amantadine is an anti-influenza A virus drug which inhibits M2 proton channel activity by binding to the channel pore, however, the majority of currently circulating influenza A viruses are amantadine-resistant. The most prevalent resistant mutation is a substitution from Ser31 to Asn31 in M2...
December 6, 2017: Microbiology and Immunology
https://www.readbyqxmd.com/read/29197671/the-in-vitro-renal-cell-toxicity-of-some-unconventional-anticancer-phenanthroline-based-platinum-ii-complexes
#3
Neville S Ng, Ming J Wu, Simon J Myers, Janice R Aldrich-Wright
The cytotoxicity of platinum(II) complexes coordinated to a chiral diamine, 1S,2S-diaminocyclohexane or 1R,2R-diaminocyclohexane and 1,10-phenanthroline or 3,4,7,8-tetramethyl-1,10-phenanthroline has been investigated in the renal proximal tubule HK-2 cell line. All platinum(II) complexes exhibited lower cytotoxicity in HK-2 cells (IC50 1.7-25μM) than in A2780 ovarian cancer cells or cisplatin-resistant A2780cisR cells (IC50 0.2-2.1μM) (at 48h). PHENSS ([Pt(1,10-phenanthroline)(1S,2S-dach)]2+) induced apoptosis and necrosis in ovarian cancer cells at concentrations that are relatively cytostatic to renal cells...
November 30, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/29186084/extended-release-amantadine-gocovri-for-dyskinesia-in-parkinson-s-disease
#4
(no author information available yet)
No abstract text is available yet for this article.
December 4, 2017: Medical Letter on Drugs and Therapeutics
https://www.readbyqxmd.com/read/29169687/understanding-the-inhibitory-mechanism-of-bit225-drug-against-p7-viroporin-using-computational-study
#5
Esmaeil Behmard, Parviz Abdolmaleki, Majid Taghdir
P7 is the only viral channel encoded by the Hepatitis C Virus (HCV) genome. It is a small, highly hydrophobic protein containing 63 amino acids. Structural studies have shown that p7 has two transmembrane (TM) α helices linked by a short dibasic cytoplasmic loop. P7, mostly placed in the endoplasmic reticulum (ER), is a membrane-associated protein. The results obtained from different studies revealed that p7 is a polytopic membrane protein that could oligomerize in membrane bilayer to create ion channels with cation selectivity...
November 16, 2017: Biophysical Chemistry
https://www.readbyqxmd.com/read/29166788/histopathological-indices-and-inflammatory-response-in-the-digestive-gland-of-the-mussel-mytilus-galloprovincialis-as-biomarker-of-immunotoxicity-to-silver-nanoparticles
#6
Younes Bouallegui, Ridha Ben Younes, Houda Bellamine, Ridha Oueslati
BACKGROUND: Histopathological assessments approaches in bivalves have become an important tool in environmental toxicology. This study seeks to develop a quantitative histopathological index (Ih) and inflammation score as biomarkers in the aim to assess the health status of nanoparticles exposed mussels. METHODS: Digestive gland Hematoxylin and eosin (H&E) stained sections from Mytilus galloprovincialis were assessed after in vivo exposure (for 3, 6 and 12h) to silver nanoparticles (Ag-NPs < 50nm and Ag-NPs < 100nm) prior and after manipulating the potential uptake pathways (clathrin- and caveolae-mediated endocytosis) using amantadine and nystatin as blockers...
November 23, 2017: Biomarkers: Biochemical Indicators of Exposure, Response, and Susceptibility to Chemicals
https://www.readbyqxmd.com/read/29155717/synthesis-of-high-purity-nonsymmetric-dialkylphosphinic-acid-extractants
#7
Junlian Wang, Meiying Xie, Xinyu Liu, Shengming Xu
We present the synthesis of (2,3-dimethylbutyl)(2,4,4'-trimethylpentyl)phosphinic acid as an example to demonstrate a method for the synthesis of high purity nonsymmetric dialkylphosphinic acid extractants. Low toxic sodium hypophosphite was chosen as the phosphorus source to react with olefin A (2,3-dimethyl-1-butene) to generate a monoalkylphosphinic acid intermediate. Amantadine was adopted to remove the dialkylphosphinic acid byproduct, as only the monoalkylphosphinic acid can react with amantadine to form an amantadine∙mono-alkylphosphinic acid salt, while the dialkylphosphinic acid cannot react with amantadine due to its large steric hindrance...
October 19, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/29139041/drug-safety-analysis-in-a-real-life-cohort-of-parkinson-s-disease-patients-with-polypharmacy
#8
Saskia Müller-Rebstein, Claudia Trenkwalder, Jens Ebentheuer, Wolfgang H Oertel, Carsten Culmsee, Günter U Höglinger
BACKGROUND: Polypharmacy is common in geriatric Parkinson's disease (PD) patients in advanced disease stages with multiple comorbidities, bearing multiple risks for drug safety in theory. OBJECTIVE: The aim of this study was to empirically identify the most frequent and relevant contraindications and drug interactions actually occurring and compromising drug safety in PD in real life. METHODS: We conducted a prospective observational study in a multimorbid cohort of PD patients with polypharmacy admitted to a specialized hospital...
November 14, 2017: CNS Drugs
https://www.readbyqxmd.com/read/29114728/ads-5102-amantadine-extended-release-for-levodopa-induced-dyskinesia
#9
Rajesh Pahwa, Robert A Hauser
No abstract text is available yet for this article.
November 6, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/29114722/ads-5102-amantadine-extended-release-for-levodopa-induced-dyskinesia-reply
#10
Aparna Wagle Shukla
No abstract text is available yet for this article.
November 6, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/29113955/treatment-of-fatigue-with-methylphenidate-modafinil-and-amantadine-in-multiple-sclerosis-triumphant-ms-study-design-for-a-pragmatic-randomized-double-blind-crossover-clinical-trial
#11
Bardia Nourbakhsh, Nisha Revirajan, Emmanuelle Waubant
BACKGROUND: Fatigue is the most common symptom of multiple sclerosis (MS). Amantadine, modafinil and amphetamine-like stimulants are commonly used in clinical practice for treatment of fatigue; however, the evidence supporting their effectiveness is sparse and conflicting. OBJECTIVE: To describe the design of a trial study funded by Patient-Centered Outcome Research Institute (PCORI) that will compare the efficacy of commonly used fatigue medications in patients with MS...
November 4, 2017: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/29104273/study-of-absorption-characteristics-of-the-total-saponins-from-radix-ilicis-pubescentis-in-an-in-situ-single-pass-intestinal-perfusion-spip-rat-model-by-using-ultra-performance-liquid-chromatography-uplc
#12
Guojun Kuang, Huan Yi, Mingjuan Zhu, Jie Zhou, Xueying Shang, Zhongxiang Zhao, Chenchen Zhu, Qiongfeng Liao, Shixia Guan, Lei Zhang
In contrast to the extensively reported therapeutic activities, far less attention has been paid to the intestinal absorption of the total saponins from Radix Ilicis Pubescentis (in Chinese Mao-Dong-Qing, MDQ). This study aimed to investigate the intestinal absorption characteristics of ilexgenin A (C1), ilexsaponin A1 (C2), ilexsaponin B1 (C3), ilexsaponin B2 (C4), ilexsaponin B3 (DC1), and ilexoside O (DC2) when administrated with the total saponins from MDQ (MDQ-TS). An UPLC method for simultaneous determination of C1, C2, C3, C4, DC1, and DC2 in intestinal outflow perfusate was developed and validated...
November 1, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29100803/the-effects-of-cysteamine-in-a-mouse-model-of-levodopa-induced-dyskinesias
#13
Linda S David, Martine Saint-Pierre, Jérôme Lamontagne-Proulx, Francesca Cicchetti
Levo-dopa (L-DOPA) has shown significant and long-lasting efficacy in the treatment of motor features characteristic of Parkinson's disease (PD). However, the effects tend to wear off at a time typically when side-effects, such as L-DOPA induced dyskinesias (LIDs), start to emerge and for which the treatment options are very limited. In recent years, we have reported on the neuroprotective and neurorestorative properties of the compounds cystamine/cysteamine in ameliorating several aspects of PD. Building on these observations, we set out to further evaluate the benefits of cysteamine on LIDs...
October 31, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29049110/evidence-for-the-efficacy-of-systemic-opioid-sparing-analgesics-in-pediatric-surgical-populations-a-systematic-review
#14
REVIEW
Alyssa Zhu, Hubert A Benzon, T Anthony Anderson
While a large number of studies has examined the efficacy of opioid-sparing analgesics in adult surgical populations, fewer studies are available to guide postoperative pain treatment in pediatric patients. We systematically reviewed available publications on the use of systemic nonopioid agents for postoperative analgesia in pediatric surgical populations. A comprehensive literature search identified meta-analyses and randomized controlled trials (RCTs) assessing the effects of systemic, nonopioid agents on postoperative narcotic requirements or pain scores in pediatric surgical populations...
November 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29032206/divalent-copper-complexes-as-influenza-a-m2-inhibitors
#15
Nathan A Gordon, Kelly L McGuire, Spencer K Wallentine, Gregory A Mohl, Jonathan D Lynch, Roger G Harrison, David D Busath
New M2 blockers effective against the ubiquitous amantadine-resistant S31N M2 mutation in influenza A are needed. Six copper complexes, 2, 4, 6, 8, 9, and 10, were synthesized and found to block both wild type and S31N M2. Free Cu(2+) also blocks M2 S31N but not S31N/H37A. The copper complexes do not block M2 H37A (either S31 or S31N). The complexes were effective against three influenza A strains in cell-culture assays, but less toxic to cells than CuCl2. For example 4, Cu(cyclooctylamineiminodiacetate), which was stable at pH > 4 in the buffers used, had an EC50 against A/Calif/07/2009 H1N1 of 0...
October 12, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29021008/medication-review-and-transitions-of-care-a-case-report-of-a-decade-old-medication-error
#16
Rachel Comer, Mitsi Lizer
A 69-year-old Caucasian male with a 25-year history of paranoid schizophrenia was brought to the emergency department because of violence toward the staff in his nursing facility. He was diagnosed with a urinary tract infection and was admitted to the behavioral health unit for medication stabilization. History included a five-year state psychiatric hospital admission and nursing facility placement. Because of poor cognitive function, the patient was unable to corroborate medication history, so the pharmacy student on rotation performed an in-depth chart review...
October 1, 2017: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
https://www.readbyqxmd.com/read/28991714/the-pharmacological-and-non-pharmacological-interventions-for-the-management-of-fatigue-related-multiple-sclerosis
#17
REVIEW
Philippa Miller, Andrew Soundy
AIM: The clinical aim was to provide up-to-date evidence-based recommendations for the treatment of MS-related fatigue (MSRF). The scientific aim was to prioritise topics for future randomised clinical trials with sufficient power. METHODS: A systematic search of review based research that considered MSRF in adults (18years and over) was undertaken in May 2016. Data from reviews was extracted, critically appraised and synthesised using four specific techniques. RESULTS: A total of 24 reviews were identified (17 non-pharmacological, 5 pharmacological, 2 combining both), which contained 339 studies on interventions deigned to improve MSRF...
October 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28958678/oseltamivir-amantadine-and-ribavirin-combination-antiviral-therapy-versus-oseltamivir-monotherapy-for-the-treatment-of-influenza-a-multicentre-double-blind-randomised-phase-2-trial
#18
John H Beigel, Yajing Bao, Joy Beeler, Weerawat Manosuthi, Alex Slandzicki, Sadia M Dar, John Panuto, Richard L Beasley, Santiago Perez-Patrigeon, Gompol Suwanpimolkul, Marcelo H Losso, Natalie McClure, Dawn R Bozzolo, Christopher Myers, H Preston Holley, Justin Hoopes, H Clifford Lane, Michael D Hughes, Richard T Davey
BACKGROUND: Influenza continues to have a substantial socioeconomic and health impact despite a long established vaccination programme and approved antivirals. Preclinical data suggest that combining antivirals might be more effective than administering oseltamivir alone in the treatment of influenza. METHODS: We did a randomised, double-blind, multicentre phase 2 trial of a combination of oseltamivir, amantadine, and ribavirin versus oseltamivir monotherapy with matching placebo for the treatment of influenza in 50 sites, consisting of academic medical centre clinics, emergency rooms, and private physician offices in the USA, Thailand, Mexico, Argentina, and Australia...
September 22, 2017: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/28917837/memantine-inhibits-%C3%AE-amyloid-aggregation-and-disassembles-preformed-%C3%AE-amyloid-aggregates
#19
Kaori Takahashi-Ito, Mitsuhiro Makino, Keiko Okado, Taisuke Tomita
Memantine, an uncompetitive glutamatergic N-methyl-d-aspartate (NMDA) receptor antagonist, is widely used as a medication for the treatment of Alzheimer's disease (AD). We previously reported that chronic treatment of AD with memantine reduces the amount of insoluble β-amyloid (Aβ) and soluble Aβ oligomers in animal models of AD. The mechanisms by which memantine reduces Aβ levels in the brain were evaluated by determining the effect of memantine on Aβ aggregation using thioflavin T and transmission electron microscopy...
November 4, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28915672/an-updated-meta-analysis-of-amantadine-for-treating-dyskinesia-in-parkinson-s-disease
#20
Min Kong, Maowen Ba, Chao Ren, Ling Yu, Shengjie Dong, Guoping Yu, Hui Liang
In recent years, a few of randomized controlled trials (RCTs) about amantadine for treating dyskinesia in Parkinson's disease (PD) were completed. Here, we conducted a systematic literature review about the clinical research to provide the updated evidence for treating dyskinesia. Electronic search of Medline, PubMed, Cochrane Library, and other databases up to May 2016 for relevant studies was performed. We selected the Unified Parkinson's Disease Rating Scale IV (UPDRS IV) and Dyskinesia Rating Scales (DRS) as efficacy outcomes of amantadine on dyskinesia...
August 22, 2017: Oncotarget
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