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Selegiline

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https://www.readbyqxmd.com/read/28643087/antioxidant-and-antiapoptotic-actions-of-selegiline-protect-against-3-np-induced-neurotoxicity-in-rats
#1
Sara A Wahdan, Mariane G Tadros, Amani E Khalifa
The present study was designed to investigate the neuroprotective effect of selegiline on 3-nitropropionic acid (3-NP)-induced neurotoxicity. Selegiline was intraperitoneally injected at doses 2.5, 5, and 10 mg/kg, 3 days prior to and continued daily, 30 min before 3-NP administration. 3-NP (20 mg/kg, i.p.) was administered for four consecutive days. 3-NP-treated rats exhibited PPI deficits, locomotor hypoactivity, increased striatal and cortical lipid peroxidation, and reduced respective glutathione (GSH) levels as well as catalase and superoxide dismutase (SOD) activities...
June 23, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28625785/cerebral-ischemia-repefusion-injury-from-bench-space-to-bedside
#2
REVIEW
Z Nagy, S Nardai
While stroke research represents the primary interface between circulation and brain research, the hemostasis system also carries a pivotal role in the mechanism of vascular brain injury. The complex interrelated events triggered by the energy crisis have a specific spatial and temporal pattern arching from the initial damage to the final events of brain repair. The complexity of the pathophysiology make it difficult to model this disease, therefore it is challenging to find appropriate therapeutic targets...
June 15, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28623006/a-longevity-study-with-enhancer-substances-selegiline-bpap-detected-an-unknown-tumor-manifestation-suppressing-regulation-in-rat-brain
#3
J Knoll, K Baghy, S Eckhardt, P Ferdinandy, M Garami, L G Harsing, P Hauser, Z Mervai, T Pocza, Z Schaff, D Schuler, I Miklya
AIMS: First proof to show that (-)-deprenyl/selegiline (DEP), the first selective inhibitor of MAO-B, later identified as the first β-phenylethylamine (PEA)-derived synthetic catecholaminergic activity enhancer (CAE) substance and (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP), the tryptamine-derived presently known most potent, selective, synthetic enhancer substance, are specific markers of unknown enhancer-sensitive brain regulations. MAIN METHODS: Longevity study disclosing the operation of tumor-manifestation-suppressing (TMS) regulation in rat brain...
June 13, 2017: Life Sciences
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
#4
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/28567124/monitoring-the-level-of-14-c-labelled-selegiline-following-oral-administration
#5
Huba Kalász, Kornélia Tekes, Erzsébet B Faigl, Zita Pöstényi, Eszter Berekméri, Gellért Karvaly, Ernest Adeghate
BACKGROUND: Selegiline [(-)-deprenyl] is widely used for the treatment of Parkinson's disease in humans. OBJECTIVE: Time-dependence of tissue distribution of selegiline following per os administration to rats. METHOD: Oral administration of radiolabeled selegiline to rats resulted in a pattern of tissue distribution similar to that following intraperitoneal injection. Analyses were done using both reversed-phase HPLC and also by counting radioactivity in various body compartments of rats...
2017: Open Medicinal Chemistry Journal
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
#6
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
#7
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/28501290/use-of-transdermal-selegiline-in-pregnancy-and-lactation-a-case-report
#8
Rebecca L Bauer, Joanne Orfei, Christina L Wichman
No abstract text is available yet for this article.
March 15, 2017: Psychosomatics
https://www.readbyqxmd.com/read/28482547/development-and-in-vitro-evaluation-of-potential-electromodulated-transdermal-drug-delivery-systems-based-on-carbon-nanotube-buckypapers
#9
Alex Schwengber, Héctor J Prado, Pablo R Bonelli, Ana L Cukierman
Buckypapers based on different types of carbon nanotubes with and without the addition of four model drugs, two of basic nature (clonidine hydrochloride, selegiline hydrochloride) and the others of acidic character (flurbiprofen, ketorolac tromethamine) were prepared and characterized. The influence of the conditions employed in the preparation of the buckypapers (dispersion time and solvents used in the preparation, as well as the type of carbon nanotubes used and the characteristics of the drug involved) on their conductivity was especially examined...
July 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28374775/comparison-for-efficacy-and-tolerability-among-ten-drugs-for-treatment-of-parkinson-s-disease-a-network-meta-analysis
#10
Chuanjun Zhuo, Xiaodong Zhu, Ronghuan Jiang, Feng Ji, Zhonghua Su, Rong Xue, Yuying Zhou
Parkinson's disease (PD) is a long term disorder affects the central nervous system and we aim to determine the relative efficacy of the current available drugs used in PD. Firstly, we performed a systematic review in current literature and eligible studies were retrieved from online databases, relevant data were extracted. Efficacy of these medications was assessed by different Unified Parkinson's Disease Rating Scales (UPDRS). Mean difference (MD) and odds ratio (OR) were produced by pairwise or network meta-analysis (NMA)...
April 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28359327/monoamine-oxidase-b-inhibitor-selegiline-reduces-18-f-thk5351-uptake-in-the-human-brain
#11
Kok Pin Ng, Tharick A Pascoal, Sulantha Mathotaarachchi, Joseph Therriault, Min Su Kang, Monica Shin, Marie-Christine Guiot, Qi Guo, Ryuichi Harada, Robert A Comley, Gassan Massarweh, Jean-Paul Soucy, Nobuyuki Okamura, Serge Gauthier, Pedro Rosa-Neto
BACKGROUND: (18)F-THK5351 is a quinoline-derived tau imaging agent with high affinity to paired helical filaments (PHF). However, high levels of (18)F-THK5351 retention in brain regions thought to contain negligible concentrations of PHF raise questions about the interpretation of the positron emission tomography (PET) signals, particularly given previously described interactions between quinolone derivatives and monoamine oxidase B (MAO-B). Here, we tested the effects of MAO-B inhibition on (18)F-THK5351 brain uptake using PET and autoradiography...
March 31, 2017: Alzheimer's Research & Therapy
https://www.readbyqxmd.com/read/28302559/in-vitro-monoamine-oxidase-inhibition-potential-of-alpha-methyltryptamine-analog-new-psychoactive-substances-for-assessing-possible-toxic-risks
#12
Lea Wagmann, Simon D Brandt, Pierce V Kavanagh, Hans H Maurer, Markus R Meyer
Tryptamines have emerged as new psychoactive substances (NPS), which are distributed and consumed recreationally without preclinical studies or safety tests. Within the alpha-methylated tryptamines, some of the psychoactive effects of the prototypical alpha-methyltryptamine (AMT) have been described decades ago and a contributing factor of its acute toxicity appears to involve the inhibition of monoamine oxidase (MAO). However, detailed information about analogs is scarce. Therefore, thirteen AMT analogs were investigated for their potential to inhibit MAO...
April 15, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28301816/mao-enzymes-inhibitory-activity-of-new-benzimidazole-derivatives-including-hydrazone-and-propargyl-side-chains
#13
Özgür Devrim Can, Derya Osmaniye, Ümide Demir Özkay, Begüm Nurpelin Sağlık, Serkan Levent, Sinem Ilgın, Merve Baysal, Yusuf Özkay, Zafer Asım Kaplancıklı
In the present work, 15 new N'-(arylidene)-4-(1-(prop-2-yn-1-yl)-1H-benzo[d]imidazol-2-yl)benzohydrazide (4a-4o) were designed and synthesized. The structures of the synthesized compounds were elucidated using FT-IR, (1)H-NMR, (13)C-NMR, and HRMS spectral data. The inhibitory activity of the compounds 4a-4o against hMAO-A and hMAO-B enzymes was evaluated by using in vitro Amlex Red(®) reagent based fluorometric method. Due to lots of high-cost kits including this assay, we determined the ingredients of the kits from the data sheets of several suppliers, and adjusted a protocol by working with various concentrations and volumes of these ingredients...
May 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28299453/simultaneous-determination-of-mao-a-and-b-activity-following-first-time-intake-of-an-irreversible-mao-b-inhibitor-in-patients-with-parkinson-s-disease
#14
Thomas Müller, Peter Riederer, Edna Grünblatt
We determined monoamine oxidase-A (plasma) and -B (platelets) enzyme activity in chronic levodopa treated patients with Parkinson's disease after first time intake of an irreversible monoamine oxidase-B inhibitor. One patient received 10 mg selegiline and eleven patients took 1 mg rasagiline. A significant decrease of monoamine oxidase-B activity appeared 2 and 4 h following monoamine oxidase-B inhibitor intake in comparison to baseline. We confirm with this design, that rasagiline and selegiline inhibit monoamine oxidase-B but not monoamine oxidase-A after single dosing...
June 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28273839/parkinson-s-disease-from-pathogenesis-to-pharmacogenomics
#15
REVIEW
Ramón Cacabelos
Parkinson's disease (PD) is the second most important age-related neurodegenerative disorder in developed societies, after Alzheimer's disease, with a prevalence ranging from 41 per 100,000 in the fourth decade of life to over 1900 per 100,000 in people over 80 years of age. As a movement disorder, the PD phenotype is characterized by rigidity, resting tremor, and bradykinesia. Parkinson's disease -related neurodegeneration is likely to occur several decades before the onset of the motor symptoms. Potential risk factors include environmental toxins, drugs, pesticides, brain microtrauma, focal cerebrovascular damage, and genomic defects...
March 4, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28137602/identification-of-human-flavin-containing-monooxygenase-3-substrates-by-a-colorimetric-screening-assay
#16
Gianluca Catucci, Isabelle Polignano, Debora Cusumano, Claudio Medana, Gianfranco Gilardi, Sheila J Sadeghi
Human hepatic flavin-containing monooxygenase 3 is a phase I drug-metabolizing enzyme that is responsible for the oxidation of a variety of drugs and xenobiotics. This work reports on a high throughput rapid colorimetric assay for the screening of substrates or inhibitors of this enzyme. The method is based on the competition of two substrates for access to the active site of hFMO3 whereby the enzymatic product of the first drug converts nitro-5-thiobenzoate (TNB, yellow) to 5,5'-dithiobis (2-nitrobenzoate) (DTNB, colourless)...
April 1, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28124620/monoamine-oxidase-b-inhibitors-in-parkinson-s-disease
#17
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/28108387/inhibition-of-monoamine-oxidase-b-by-selegiline-reduces-cigarette-smoke-induced-oxidative-stress-and-inflammation-in-airway-epithelial-cells
#18
Yuting Cui, Kenneth W K Liu, Yingmin Liang, Mary S M Ip, Judith C W Mak
Chronic obstructive pulmonary disease (COPD) is caused by the build-up of oxidative stress-induced damages due to cigarette smoking, but how monoamine oxidase (MAO)-B signaling is involved remains unclear. This study aims to establish the involvement of MAO-B signaling pathways in cigarette smoke medium (CSM)-induced oxidative stress and inflammation in human airway epithelial cells (AECs). CSM treatment increased MAO-B activity, ROS levels and IL-8 release in AECs. Pretreatment with MAO-B selective inhibitor selegiline reversed the CSM-induced changes in MAO-B activity, ROS levels and IL-8 release in a dose-dependent manner...
February 15, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28034283/in-silico-studies-revealed-multiple-neurological-targets-for-the-antidepressant-molecule-ursolic-acid
#19
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/28013042/production-of-stable-gfp-expressing-neural-cells-from-p19-embryonal-carcinoma-stem-cells
#20
Hedayatollah Shirzad, Fariba Esmaeili, Shabnam Bakhshalizadeh, Marzieh Ebrahimie, Esmaeil Ebrahimie
Murine P19 embryonal carcinoma (EC) cells are convenient to differentiate into all germ layer derivatives. One of the advantages of P19 cells is that the exogenous DNA can be easily inserted into them. Here, at the first part of this study, we generated stable GFP-expressing P19 cells (P19-GFP(+)). FACS and western-blot analysis confirmed stable expression of GFP in the cells. We previously demonstrated the efficient induction of neuronal differentiation from mouse ES and EC cells by application of a neuroprotective drug, selegiline In the second part of this study selegiline was used to induce differentiation of P19-GFP(+) into stable GFP-expressing neuron-like cells...
December 21, 2016: Molecular and Cellular Probes
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