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https://www.readbyqxmd.com/read/28153587/a-stereoselective-catalytic-strategy-for-the-in-flow-synthesis-of-advanced-precursors-of-rasagiline-and-tamsulosin
#1
Davide Brenna, Margherita Pirola, Laura Raimondi, Anthony J Burke, Maurizio Benaglia
The diastereoselective, trichlorosilane-mediate reduction of imines, bearing different and removable chiral auxiliaries, in combination either with achiral bases or catalytic amounts of chiral Lewis bases, was investigated to afford immediate precursors of chiral APIs (Active Pharmaceutical Ingredients). The carbon-nitrogen double bond reduction was successfully performed in batch and in flow mode, in high yields and almost complete stereocontrol. By this metal-free approach, the formal synthesis of rasagiline and tamsulosin was successfully accomplished in micro(meso) flow reactors, under continuous flow conditions...
January 21, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28148284/rasagiline-induced-severe-recurrent-hypoglycemia-in-a-young-woman-without-diabetes-a-case-report
#2
Fawzi A Bachet Ibrahim, Fauzia Rashid, Azza A Bin Hussain, Fatheya Alawadi, A Bashier
BACKGROUND: We report a case of a patient with recurrent severe hypoglycemia after initiating the drug rasagiline (Azilect) for Parkinson disease. CASE PRESENTATION: A 25-year-old Emirati woman who had been diagnosed with Parkinson disease due to a genetic mutation since the age of 18 years presented to our hospital. She had been treated with a rotigotine patch 2 mg per day along with carbidopa + levodopa + entacapone 25 mg/100 mg/200 mg (Stalevo) over these years...
February 2, 2017: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/28145614/diazaphospholene-precatalysts-for-imine-and-conjugate-reductions
#3
Matt R Adams, Chieh-Hung Tien, Blake S N Huchenski, Michael J Ferguson, Alexander W H Speed
The first examples of 1,3,2-diazaphospholene-catalyzed imine reduction and conjugate reduction reactions are reported. This approach employs readily synthesized alkoxydiazaphospholene precatalysts that can be handled in open air. Reduction of substrates containing Lewis basic functionality, isolated unsaturation, and protic functional groups was accomplished. The synthetic utility of this approach is demonstrated by the synthesis of the important antiparkinson medicine rasagiline and the natural product zingerone...
February 1, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28124620/monoamine-oxidase-b-inhibitors-in-parkinson-s-disease
#4
Livia Dézsi, László Vécsei
BACKGROUND: Parkinson's disease (PD) is a neurodegenerative disorder with a prevalence increasing with age. Oxidative stress and glutamate toxicity are involved in its pathomechanism. There are still many unmet needs of PD patients, including the alleviation of motor fluctuations and dyskinesias, and the development of therapies with neuroprotective potential. OBJECTIVE: To give an overview of the pharmacological properties, the efficacy and safety of the monoamine oxidase B (MAO-B) inhibitors in the treatment of PD, with special focus on the results of randomized clinical trials...
January 24, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28097005/the-cardioprotective-efficacy-of-tvp1022-against-ischemia-reperfusion-injury-and-cardiac-remodeling-in-rats
#5
Assaf Malka, Offir Ertracht, Noa Bachner-Hinenzon, Irina Reiter, Ofer Binah
Following acute myocardial infarction (MI), early and successful reperfusion is the most effective strategy for reducing infarct size and improving the clinical outcome. However, immediate restoration of blood flow to the ischemic zone results in myocardial damage, defined as "reperfusion-injury". Whereas we previously reported that TVP1022 (the S-isomer of rasagiline, FDA-approved anti-Parkinson drug) decreased infarct size 24 h post ischemia reperfusion (I/R) in rats, in this study we investigated the chronic cardioprotective efficacy of TVP1022 14 days post-I/R...
December 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/27984078/anti-inflammatory-and-protective-effects-of-mt-031-a-novel-multitarget-mao-a-and-ache-buche-inhibitor-in-scopolamine-mouse-model-and-inflammatory-cells
#6
Wei Liu, Alon Rabinovich, Yuval Nash, Dan Frenkel, Yuqiang Wang, Moussa B H Youdim, Orly Weinreb
Previous study demonstrated that the novel multitarget compound, MT-031 preserved in one molecule entity the beneficial properties of its parent drugs, rasagiline and rivastigmine, and exerted high dual potencies of monoamine oxidase-A (MAO-A) and cholinesterase (ChE) inhibition in acute-treated mice and neuroprotective effects against H2O2-induced neurotoxicity in human neuroblastoma SH-SY5Y cells. The present study aimed to further investigate the anti-inflammatory and protective effects of MT-031 in scopolamine mouse model and inflammatory cell cultures...
October 28, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27833522/histamine-h3-receptors-and-its-antagonism-as-a-novel-mechanism-for-antipsychotic-effect-a-current-preclinical-clinical-perspective
#7
REVIEW
Danish Mahmood
Histamine H3 receptors are present as autoreceptors on histaminergic neurons and as heteroreceptors on nonhistaminergic neurones. They control the release and synthesis of histamine and several other key neurotransmitters in the brain. H3 antagonism may be a novel approach to develop a new class of antipsychotic medications given the gathering evidence reporting therapeutic efficacy in several central nervous system disorders. Several medications such as cariprazine, lurasidone, LY214002, bexarotene, rasagiline, raloxifene, BL-1020 and ITI-070 are being developed to treat the negative symptoms and cognitive impairments of schizophrenia...
October 2016: International Journal of Health Sciences
https://www.readbyqxmd.com/read/27829318/cognitive-effects-of-rasagiline-in-mild-to-moderate-stage-parkinson-s-disease-without-dementia
#8
Laura L Frakey, Joseph H Friedman
The authors studied the effects of rasagiline on cognition in a sample of 50 nondemented patients with mild to moderate Parkinson's disease (PD) using a double-blind, placebo controlled design. Cognition and motor symptoms were assessed at baseline and after 6 months of receiving either rasagiline or placebo. Participants receiving rasagiline showed improvement in their motor symptoms of PD compared to participants receiving placebo. No significant changes in performance on neuropsychological measures of cognition were observed between the groups...
2017: Journal of Neuropsychiatry and Clinical Neurosciences
https://www.readbyqxmd.com/read/27827298/open-label-study-of-sleep-disturbances-in-patients-with-parkinson-s-disease-treated-with-rasagiline
#9
MULTICENTER STUDY
Michel Panisset, Jean-Louis Stril, Manon Bélanger, Geneviève Lehoux, Donna Coffin, Sylvain Chouinard
BACKGROUND: The prevalence of sleep disturbances among patients with Parkinson's disease (PD) is estimated to occur in 37% to 98% of patients. Sleep disturbances have been associated with a reduced quality of life for patients with PD. The objective of this study was to assess the impact of rasagiline treatment on the severity of sleep disturbances among patients with idiopathic PD. METHODS: In this open-label, multicentre study, 110 adult patients with idiopathic PD were treated with rasagiline either as monotherapy or as adjunct therapy...
November 2016: Canadian Journal of Neurological Sciences. le Journal Canadien des Sciences Neurologiques
https://www.readbyqxmd.com/read/27803666/inhibitors-of-mao-a-and-mao-b-in-psychiatry-and-neurology
#10
REVIEW
John P M Finberg, Jose M Rabey
Inhibitors of MAO-A and MAO-B are in clinical use for the treatment of psychiatric and neurological disorders respectively. Elucidation of the molecular structure of the active sites of the enzymes has enabled a precise determination of the way in which substrates and inhibitor molecules are metabolized, or inhibit metabolism of substrates, respectively. Despite the knowledge of the strong antidepressant efficacy of irreversible MAO inhibitors, their clinical use has been limited by their side effect of potentiation of the cardiovascular effects of dietary amines ("cheese effect")...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27729794/rasagiline-for-sleep-disorders-in-patients-with-parkinson-s-disease-a-prospective-observational-study
#11
Carla Schettino, Clemente Dato, Guglielmo Capaldo, Simone Sampaolo, Giuseppe Di Iorio, Mariarosa Ab Melone
INTRODUCTION: Rasagiline is a selective, irreversible monoamine oxidase B inhibitor that ameliorates the symptoms of Parkinson's disease (PD) by inhibiting striatal dopamine metabolism. There is also evidence that monoamine oxidase B inhibitors increase melatonin levels in the pineal gland and may have a beneficial effect on sleep disorders, which are a common feature in patients with PD. METHODS: This single-center, prospective, observational, 12-week study compared the effect of combination therapy with levodopa 200-300 mg/d + rasagiline 1 mg/d (n=19) with levodopa 200-300 mg/d alone (n=19) in the treatment of sleep disorders in patients with idiopathic PD...
2016: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/27715253/an-overview-of-analytical-methods-for-the-determination-of-monoamine-oxidase-inhibitors-in-pharmaceutical-formulations-and-biological-fluids
#12
REVIEW
Cafer Saka
Monoamine oxidase inhibitors (MAOIs) were the first type of antidepressant developed. MAOIs elevate the levels of norepinephrine, serotonin, and dopamine by inhibiting an enzyme called monoamine oxidase. They are also used in the treatment of Parkinson's disease, tuberculosis, and several other disorders. Therefore, it is very important to develop efficient analytical methods for monitoring and management. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. In this article, analyses of MAOIs in pharmaceutical formulations and biological fluids were reviewed from 2000 to the present, including all types of chromatographic, spectrophotometric, electrophoretic, and voltammetric techniques, focusing on isoniazid, tranylcypromine, moclobemide, rasagiline, and selegiline...
January 2, 2017: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/27651784/no-synergism-between-bis-propyl-cognitin-and-rasagiline-on-protecting-dopaminergic-neurons-in-parkinson-s-disease-mice
#13
Cheng-You Zheng, Bao-Jian Guo, Wei Cai, Wei Cui, Shing-Hung Mak, Yu-Qiang Wang, Simon Ming-Yuen Lee, Yi-Fan Han, Zai-Jun Zhang
Rasagiline, a monoamine oxidase-B inhibitor, and bis(propyl)-cognitin (B3C), a novel dimer are reported to be neuroprotective. Herein, the synergistical neuroprotection produced by rasagiline and B3C was investigated in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mice of Parkinsonism. By using neurobehavioural tests, high-performance liquid chromatography and western blot assay, we showed that B3C at 0.3 mg/kg, rasagiline at 0.02 mg/kg, as well as co-treatment with B3C and rasagiline prevented MPTP-induced behavioural abnormities, increased the concentrations of dopamine and its metabolites in the striatum, and up-regulated the expression of tyrosine hydroxylase in the substantia nigra...
August 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/27618783/patterns-and-predictors-of-freezing-of-gait-improvement-following-rasagiline-therapy-a-pilot-study
#14
Fariborz Rahimi, Angela C Roberts, Mandar Jog
OBJECTIVES: Freezing of gait (FoG) is a challenging clinical symptom in Parkinson's disease with variable improvements in FoG with rasagiline. In this prospective, uncontrolled, pre-/post- treatment pilot study, we explore the clinical variables that contribute to this variability and those that predict improvement. PATIENTS AND METHODS: Frequency and duration of FoG, along with other standardized scales, were evaluated in 18 optimally medicated PD participants with intractable FoG, prior to and after completion of a 90-day course of 1mg daily rasagiline...
November 2016: Clinical Neurology and Neurosurgery
https://www.readbyqxmd.com/read/27503749/a-spectrophotometric-assay-for-monoamine-oxidase-activity-with-2-4-dinitrophenylhydrazine-as-a-derivatized-reagent
#15
Guili Huang, Fei Zhu, Yuhang Chen, Shiqiang Chen, Zhonghong Liu, Xin Li, Linlin Gan, Li Zhang, Yu Yu
A simple, rapid and reliable spectrophotometry was developed to determine monoamine oxidase (MAO). In this study, 2,4-dinitrophenylhydrazine (DNPH), a classic derivatizing reagent, was used to detect MAO-dependent aldehyde production; and traditional DNPH spectrophotometry was simplified. Benzylamine and serotonin oxidation were catalyzed by MAO-B and MAO-A, respectively, to aldehydes. These were derivatized with DNPH, and the corresponding quinones were further formed by adding NaOH. These DNPH derivatives with large conjugated structures were directly measured spectrophotometrically at 465 nm and 425 nm, without the need for precipitating, washing and suspending procedures...
November 1, 2016: Analytical Biochemistry
https://www.readbyqxmd.com/read/27474888/minimally-clinically-important-decline-in-the-parkinsonian-variant-of-multiple-system-atrophy
#16
Florian Krismer, Klaus Seppi, Gregor K Wenning, Victor Abler, Spyridon Papapetropoulos, Werner Poewe
INTRODUCTION: We provide the first characterization of the minimally clinically important difference on the Unified Multiple System Atrophy Rating Scale in patients with the parkinsonian variant of early MSA. METHODS: Data from a randomized controlled trial of rasagiline were analyzed using clinical global impression as an anchor. Because too few patients improved with treatment, analyses were limited to defining scale cutoffs that discriminated between minimal worsening and no change...
October 2016: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/27465906/is-it-possible-to-achieve-bio-equivalence-between-an-oral-solid-immediate-release-and-an-analogue-enteric-coated-formulation
#17
Dannit Licht, Rachel Cohen, Ofer Spiegelstein, Laura Rabinovich-Guilatt, Marina Zholkovsky, Adrian Gilbert, Jennifer B Dressman, Muhammad Safadi
OBJECTIVES: While bioequivalence between enteric-coated and immediate-release formulations can be achieved in terms of AUC, gastric emptying of enteric-coated dosage forms is a stochastic event, usually leading to lower Cmax values than those observed with the corresponding immediate release. This article examines challenges of developing enteric-coated dosage forms which are bioequivalent to the corresponding immediate-release formulations in terms of both AUC and Cmax using rasagiline as a model compound...
October 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27438181/comparison-of-selegiline-and-rasagiline-therapies-in-parkinson-disease-a-real-life-study
#18
COMPARATIVE STUDY
Chava Peretz, Hagar Segev, Violet Rozani, Tanya Gurevich, Baruch El-Ad, Judith Tsamir, Nir Giladi
BACKGROUND: We aimed to compare indicators of Parkinson disease (PD) progression between patients first prescribed either selegiline or rasagiline as their antiparkinsonian drugs (APDs) on the basis of real-life data. METHODS: Pharmacy data on members of a large Israeli health maintenance organization, treated as patients with PD during 2001-2012 and prescribed selegiline or rasagiline as their first APD, were analyzed. The first APD was selegiline for 349 patients (2001-2006) and rasagiline for 485 patients (2007-2012)...
September 2016: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/27431201/long-term-effects-of-rasagiline-and-the-natural-history-of-treated-parkinson-s-disease
#19
Olivier Rascol, Robert A Hauser, Fabrizio Stocchi, Cheryl J Fitzer-Attas, Yulia Sidi, Victor Abler, C Warren Olanow
BACKGROUND: The Attenuation of Disease progression with Azilect GIven Once-daily (ADAGIO) delayed-start study demonstrated a benefit of early-start treatment with rasagiline 1 mg/day versus delayed-start treatment in PD. This follow-up study aimed to assess whether these benefits persist and the clinical progression rate during long-term naturalistic treatment. METHODS: The ADAGIO Follow-Up study was initiated approximately 26 months after completion of the ADAGIO study...
July 19, 2016: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/27386592/-comorbid-states-in-parkinson-s-disease-an-effect-of-mao-b-inhibitors
#20
N V Titova, E A Katunina, N N Sotnikova
The comorbidity in Parkinson's disease (PD), which is closely related to the tolerability of antiparkinsonian drugs, is-'analyzed. The authors present the results of the studies that have confirmed the greater safety of rasagiline compared to dopamine receptor agonists in elderly patients. The effects of rasagiline, including combinations of this drug with antidepressants, on-depression in PD and the low risk,of the serotonin -syndrome caused by these combinations are considered. The studies demonstrated the effect of rasagiline on fatigue and cognitive functions in PD patients are described...
2016: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
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