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https://www.readbyqxmd.com/read/29159774/pharmacokinetics-pharmacodynamics-and-safety-of-rasagiline-transdermal-patch-a-preliminary-study-in-healthy-chinese-subjects
#1
Wenjia Zhou, Chengzhe Lv, Quanying Zhang, Shunlin Zong, Meng Wang
BACKGROUND AND OBJECTIVES: Rasagiline tablet is an oral MAO-B inhibitor applied in early or advanced Parkinson's disease (PD). However, when patients with PD cannot take their usual oral medications, a rasagiline transdermal patch can be used as a way to offer continuous rasagiline while avoiding plasma concentration peaks and troughs. The objectives of this study were to investigate the pharmacokinetics, pharmacodynamics, and safety of the rasagiline transdermal patch in healthy Chinese subjects...
November 20, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29133700/wearing-off-a-complex-phenomenon-often-poorly-recognized-in-parkinson-s-disease-a-study-with-the-woq-19-questionnaire
#2
Michele Pistacchi, Manuela Gioulis, Flavio Sanson, Sandro Z Marsala
BACKGROUND: 'Wearing off' refers to the phenomenology of movement disorders in Parkinson's disease (PD) that appears early and is much commoner than generally believed. It may be present in the form of either motor symptoms or non-motor symptoms. AIM: To investigate the utility of wearing-off questionnaire (WOQ-19, Italian version) in the outpatient clinical practice to assess the suitability of different combinations of treatment, in various stages of PD. METHODS: 73 consecutive patients (58% male and 42% female) suffering from PD were recruited through the Santorso Hospital and San Martino Hospital from September 2012 to March 2014...
November 2017: Neurology India
https://www.readbyqxmd.com/read/29115745/asymmetric-imine-hydroboration-catalyzed-by-chiral-diazaphospholenes
#3
Matt Rhodes Adams, Chieh-Hung Tien, Robert McDonald, Alexander William Harrison Speed
The first use of diazaphospholenes as chiral catalysts has been demonstrated with enantioselective imine hydroboration. A chiral diazaphospholene prepared in a simple three-step synthesis from commercial materials has been shown to achieve the highest enantioselectivity for hydroboration of alkyl imines with pinacolborane reported to date. Enantiomer ratios of up to 88:12 were obtained with low (2 mol %) catalyst loadings. Shown are 20 examples of asymmetric reduction employing this main-group catalysis protocol, including the synthesis of the pharmaceuticals ent-rasagiline and fendiline...
November 8, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/29079063/neuroprotective-and-neuro-restorative-effects-of-minocycline-and-rasagiline-in-a-zebrafish-6-hydroxydopamine-model-of-parkinson-s-disease
#4
Aileen Cronin, Maura Grealy
Parkinson's disease is a common, debilitating, neurodegenerative disorder for which the current gold standard treatment, levodopa (L-DOPA) is symptomatic. There is an urgent, unmet need for neuroprotective or, ideally, neuro-restorative drugs. We describe a 6-hydroxydopamine (6-OHDA) zebrafish model to screen drugs for neuroprotective and neuro-restorative capacity. Zebrafish larvae at two days post fertilization were exposed to 6-OHDA for three days, with co-administration of test drugs for neuroprotection experiments, or for 32 h, with subsequent treatment with test drugs for neuro-restoration experiments...
October 24, 2017: Neuroscience
https://www.readbyqxmd.com/read/28980620/-pharmacoeconomic-aspects-of-combined-treatment-of-advanced-stage-of-parkinson-s-disease
#5
A V Rudakova, O S Levin
AIM: To assess the cost-efficiency of the fixed levodopa/carbidopa/entacapone combination and the free combination of levodopa/carbidopa with rasagiline. MATERIAL AND METHODS: An analysis was performed using the Markov model including three clinical states: duration of off-time ≤25%, duration of off-time >25% and fatal outcome. Costs of the drugs were calculated based on the results of auctions for 2016 by IMS Health data. RESULTS: In basic variant (drugs containing levodopa, 5-times a day), costs of treatment with the fixed levodopa/carbidopa/entacapone combination were 2...
2017: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
https://www.readbyqxmd.com/read/28962525/from-the-cover-manganese-and-rotenone-induced-oxidative-stress-signatures-differ-in-ipsc-derived-human-dopamine-neurons
#6
M Diana Neely, Carrie Ann Davison, Michael Aschner, Aaron B Bowman
Parkinson's disease (PD) is the result of complex interactions between genetic and environmental factors. Two chemically distinct environmental stressors relevant to PD are the metal manganese and the pesticide rotenone. Both are thought to exert neurotoxicity at least in part via oxidative stress resulting from impaired mitochondrial activity. Identifying shared mechanism of action may reveal clues towards an understanding of the mechanisms underlying PD pathogenesis. Here we compare the effects of manganese and rotenone in human-induced pluripotent stem cells-derived postmitotic mesencephalic dopamine neurons by assessing several different oxidative stress endpoints...
October 1, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28956175/rasagiline-for-dysexecutive-symptoms-during-wearing-off-in-parkinson-s-disease-a-pilot-study
#7
Domiziana Rinaldi, Francesca Assogna, Michela Sforza, Stefania Tagliente, Francesco E Pontieri
Wearing-off refers to the predictable worsening of motor and sometimes non-motor symptoms of Parkinson's disease occurring at the end of levodopa dose that improves with the next drug dose. Here, we investigated the efficacy of rasagiline on executive functions at the end of levodopa dose in patients displaying symptoms of wearing-off. Rasagiline was well-tolerated and produced a significant improvement at the Frontal Assessment Battery, together with improvement of motor symptoms at the end of levodopa dose...
September 27, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28937665/a-reductive-aminase-from-aspergillus-oryzae
#8
Godwin A Aleku, Scott P France, Henry Man, Juan Mangas-Sanchez, Sarah L Montgomery, Mahima Sharma, Friedemann Leipold, Shahed Hussain, Gideon Grogan, Nicholas J Turner
Reductive amination is one of the most important methods for the synthesis of chiral amines. Here we report the discovery of an NADP(H)-dependent reductive aminase from Aspergillus oryzae (AspRedAm, Uniprot code Q2TW47) that can catalyse the reductive coupling of a broad set of carbonyl compounds with a variety of primary and secondary amines with up to >98% conversion and with up to >98% enantiomeric excess. In cases where both carbonyl and amine show high reactivity, it is possible to employ a 1:1 ratio of the substrates, forming amine products with up to 94% conversion...
October 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28923922/trkb-neurotrophic-activities-are-blocked-by-%C3%AE-synuclein-triggering-dopaminergic-cell-death-in-parkinson-s-disease
#9
Seong Su Kang, Zhentao Zhang, Xia Liu, Fredric P Manfredsson, Matthew J Benskey, Xuebing Cao, Jun Xu, Yi E Sun, Keqiang Ye
BDNF/TrkB neurotrophic signaling is essential for dopaminergic neuronal survival, and the activities are reduced in the substantial nigra (SN) of Parkinson's disease (PD). However, whether α-Syn (alpha-synuclein) aggregation, a hallmark in the remaining SN neurons in PD, accounts for the neurotrophic inhibition remains elusive. Here we show that α-Syn selectively interacts with TrkB receptors and inhibits BDNF/TrkB signaling, leading to dopaminergic neuronal death. α-Syn binds to the kinase domain on TrkB, which is negatively regulated by BDNF or Fyn tyrosine kinase...
October 3, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28872217/adverse-effects-produced-by-different-drugs-used-in-the-treatment-of-parkinson-s-disease-a-mixed-treatment-comparison
#10
Bao-Dong Li, Zhen-Yun Bi, Jing-Feng Liu, Wei-Jun Si, Qian-Qian Shi, Li-Peng Xue, Jing Bai
OBJECTIVE: This mixed treatment comparison is used to compare the adverse effects of eleven different drugs used to treat Parkinson's disease (PD). The drugs that we compare include the following: ropinirole, rasagiline, rotigotine, entacapone, apomorphine, pramipexole, sumanirole, bromocriptine, piribedil, pergolide, and levodopa. METHODS: PubMed, EMBASE, and Cochrane Library were searched from the inception to December 2015. Our analysis combines the evidences of direct comparison and indirect comparison between various literatures...
October 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/28831499/erratum-to-efficacy-of-rasagiline-and-selegiline-in-parkinson-s-disease-a-head-to-head-3-year-retrospective-case-control-study
#11
Emanuele Cereda, Roberto Cilia, Margherita Canesi, Silvana Tesei, Claudio Bruno Mariani, Anna Lena Zecchinelli, Gianni Pezzoli
No abstract text is available yet for this article.
September 2017: Journal of Neurology
https://www.readbyqxmd.com/read/28772050/the-neuroprotective-agent-rasagiline-mesylate-attenuates-cardiac-remodeling-after-experimental-myocardial-infarction
#12
Aimilia Varela, Manolis Mavroidis, Michalis Katsimpoulas, Irini Sfiroera, Niki Kappa, Angelica Mesa, Nikolaos G Kostomitsopoulos, Dennis V Cokkinos
AIM: Rasagiline mesylate (N-propargyl-1 (R)-aminoindan) (RG) is a selective, potent irreversible inhibitor of monoamine oxidase-B with cardioprotective and anti-apoptotic properties. We investigated whether it could be cardioprotective in a rat model undergoing experimental myocardial infarction (MI) by permanent ligation of the left anterior descending coronary artery. METHODS AND RESULTS: RG was administered, intraperitoneally, for 28 days (2 mg/kg) starting 24 h after MI induction...
August 2017: ESC Heart Failure
https://www.readbyqxmd.com/read/28767029/recurrent-impulse-control-disorder-associated-with-rasagiline-treatment-of-parkinson-s-disease
#13
Ariel Levy, Anthony E Lang
No abstract text is available yet for this article.
July 2017: Canadian Journal of Neurological Sciences. le Journal Canadien des Sciences Neurologiques
https://www.readbyqxmd.com/read/28753970/reversed-phase-uhplc-enantiomeric-separation-of-rasagiline-salts-using-a-chiralpak-%C3%A2-agp-column
#14
Nagarajan Balaji, Sayeeda Sultana
We report the first rapid ultra-high performance liquid chromatographic (UHPLC) enantiomeric reversed-phase separation of rasagiline mesylate and its tartrate salts using a Chiralpak(®) AGP column (50 mm × 2.1 mm, 5 μm) as a stationary phase. This method was developed as an alternative to the usage of previously reported normal-phase chiral LC columns for isomer separation. Our method is based on an isocratic approach using a mixture of ammonium acetate and isopropyl alcohol (90:10, v/v) as the mobile phase (0...
July 19, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28682929/determination-of-monoamine-oxidase-a-and-b-activity-in-long-term-treated-patients-with-parkinson-disease
#15
Thomas Müller, Peter Riederer, Edna Grünblatt
BACKGROUND: Biogenic amines and monoamine oxidase inhibitors influence peripheral monoamine oxidase enzyme activity in chronic levodopa/dopa decarboxylase inhibitor-treated patients with Parkinson disease. Rasagiline is an irreversible inhibitor of monoamine oxidase B. Safinamide blocks this isoenzyme in a reversible fashion. OBJECTIVES: The aim of this study was to determine monoamine oxidase A (plasma) and B (platelets) enzyme activity in long-term levodopa-treated patients without and with additional oral intake of 50- or 100-mg safinamide or 1-mg rasagiline or first-time intake of rasagiline...
September 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28577058/type-b-and-a-monoamine-oxidase-and-their-inhibitors-regulate-the-gene-expression-of-bcl-2-and-neurotrophic-factors-in-human-glioblastoma-u118mg-cells-different-signal-pathways-for-neuroprotection-by-selegiline-and-rasagiline
#16
Keiko Inaba-Hasegawa, Masayo Shamoto-Nagai, Wakako Maruyama, Makoto Naoi
Type B monoamine oxidase (MAO-B) in glial cells has been considered to be associated with neuronal death in Parkinson's disease. MAO-B inhibitors, rasagiline and selegiline [(-)deprenyl], protect neurons in animal and cellular models of neurodegeneration. However, the role of MAO-B itself in the regulation of cell death processing remains elusive, whereas type A MAO (MAO-A) mediates the induction of anti-apoptotic Bcl-2 genes by rasagiline and selegiline. In this paper, the involvement of MAOs in the induction of neuroprotective genes by MAO inhibitors was investigated in human glioblastoma U118MG cells expressing mainly MAO-B...
June 2, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28550482/efficacy-of-rasagiline-and-selegiline-in-parkinson-s-disease-a-head-to-head-3-year-retrospective-case-control-study
#17
Emanuele Cereda, Roberto Cilia, Margherita Canesi, Silvana Tesei, Claudio Bruno Mariani, Anna Lena Zecchinelli, Gianni Pezzoli
Monoamine oxidase type B (MAO-B) inhibitors, such as selegiline and rasagiline, can be used as monotherapy or adjuvant therapy to levodopa in Parkinson's disease (PD). Data on long-term efficacy of MAO-B inhibitors are limited with no head-to-head comparison available to date. The aim of this case-control retrospective study was to analyze data from patients with PD attending the Parkinson Institute (Milan, Italy) over a 6-year period (2009-2015) and compare the effects of selegiline and rasagiline on levodopa treatment outcomes...
June 2017: Journal of Neurology
https://www.readbyqxmd.com/read/28515684/selegiline-ameliorates-depression-like-behavior-in-mice-lacking-the-cd157-bst1-gene-a-risk-factor-for-parkinson-s-disease
#18
Satoka Kasai, Toru Yoshihara, Olga Lopatina, Katsuhiko Ishihara, Haruhiro Higashida
Parkinson's disease (PD), a neurodegenerative disorder, is accompanied by various non-motor symptoms including depression and anxiety, which may precede the onset of motor symptoms. Selegiline is an irreversible monoamine oxidase-B (MAO-B) inhibitor, and is widely used in the treatment of PD and major depression. However, there are few reports about the effects of selegiline on non-motor symptoms in PD. The aim of this study was to explore the antidepressant and anxiolytic effects of selegiline, using CD157/BST1 knockout (CD157 KO) mouse, a PD-related genetic model displaying depression and anxiety, compared with other antiparkinsonian drugs and an antidepressant, and was to investigate the effects of selegiline on biochemical parameters in emotion-related brain regions...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28506583/synthesis-of-enantiomerically-enriched-drug-precursors-and-an-insect-pheromone-via-reduction-of-ketones-using-commercially-available-carbonyl-reductase-screening-kit-chiralscreen%C3%A2-oh
#19
Toshiya Nagai, Saki Sakurai, Naoki Natori, Manaka Hataoka, Takako Kinoshita, Hiroyoshi Inoue, Kengo Hanaya, Mitsuru Shoji, Takeshi Sugai
Commercially available "Chiralscreen® OH" starter kit containing five types of carbonyl reductases (E001, E007, E031, E039, and E078) was used for the reduction of several aromatic and aliphatic ketones to obtain enantiomerically enriched drug precursors and an insect pheromone. Almost stereochemically pure secondary alcohols, used in the synthesis of drugs such as (R)-rasagiline mesylate, (S)-rivastigmine, (R)-chlorphenesin carbamate, and (R)-mexiletine, and the insect pheromone (4S,5R)-sitophilure, were conveniently obtained...
April 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28490648/randomized-trial-of-preladenant-given-as-monotherapy-in-patients-with-early-parkinson-disease
#20
RANDOMIZED CONTROLLED TRIAL
Fabrizio Stocchi, Olivier Rascol, Robert A Hauser, Susan Huyck, Anjela Tzontcheva, Rachel Capece, Tony W Ho, Peter Sklar, Christopher Lines, David Michelson, David J Hewitt
OBJECTIVE: To evaluate the adenosine 2a receptor antagonist preladenant as a nondopaminergic drug for the treatment of Parkinson disease (PD) when given as monotherapy. METHODS: This was a randomized, 26-week, placebo- and active-controlled, parallel-group, multicenter, double-blind trial conducted in adults diagnosed with PD for <5 years who were not yet receiving l-dopa or dopamine agonists. Patients with a Unified Parkinson's Disease Rating Scale (UPDRS) part 3 (motor function) score ≥10 and Hoehn & Yahr score ≤3 were randomized 1:1:1:1:1 to preladenant 2, 5, or 10 mg twice daily, rasagiline 1 mg (active-control) once daily, or placebo...
June 6, 2017: Neurology
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