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https://www.readbyqxmd.com/read/28875405/appraisal-of-transdermal-water-in-oil-nanoemulgel-of-selegiline-hcl-for-the-effective-management-of-parkinson-s-disease-pharmacodynamic-pharmacokinetic-and-biochemical-investigations
#1
Sonal Setya, Tushar Madaan, Mohammad Tariq, B K Razdan, Sushama Talegaonkar
In the present study, the potential of transdermal nanoemulsion gel of selegiline hydrochloride for the treatment of Parkinson's disease was investigated. Water-in-oil nanoemulsions were developed by comparing low- and high-energy methods and were subjected to thermodynamic stability tests, in vitro permeation, and characterization studies. In vitro studies indicated that components of nanoemulsion acted as permeation enhancers with highest flux of 3.531 ± 1.94 μg/cm(2)/h from nanoemulsion SB6 containing 0...
September 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28857772/a-randomized-double-blind-placebo-controlled-phase-iii-trial-of-selegiline-monotherapy-for-early-parkinson-disease
#2
Yoshikuni Mizuno, Nobutaka Hattori, Tomoyoshi Kondo, Masahiro Nomoto, Hideki Origasa, Ryosuke Takahashi, Mitsutoshi Yamamoto, Nobuo Yanagisawa
BACKGROUND: In Japan, selegiline has been approved for combination therapy with levodopa for Parkinson disease (PD). We conducted a trial of selegiline monotherapy for early PD. METHODS: In this 12-week controlled phase III trial, a total of 292 subjects were randomized to receive placebo (n = 146) (full analysis set 140) or selegiline (n = 146) (full analysis set 139). The primary outcome measure was the change in the Unified Parkinson Disease Rating Scale part I + II + III total score from baseline to the final visit...
September 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28840582/n-acetylcysteine-prevents-the-increase-in-spontaneous-oxidation-of-dopamine-during-monoamine-oxidase-inhibition-in-pc12-cells
#3
David S Goldstein, Yunden Jinsmaa, Patti Sullivan, Yehonatan Sharabi
The catecholaldehyde hypothesis for the pathogenesis of Parkinson's disease proposes that the deaminated dopamine metabolite 3,4-dihydroxyphenylacetaldehyde (DOPAL) is toxic to nigrostriatal dopaminergic neurons. Inhibiting monoamine oxidase (MAO) should therefore slow the disease progression; however, MAO inhibition increases spontaneous oxidation of dopamine, as indicated by increased 5-S-cysteinyl-dopamine (Cys-DA) levels, and the oxidation products may also be toxic. This study examined whether N-acetylcysteine (NAC), a precursor of the anti-oxidant glutathione, attenuates the increase in Cys-DA production during MAO inhibition...
August 24, 2017: Neurochemical Research
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
#4
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/28774283/effectiveness-of-spinal-cord-stimulation-for-painful-camptocormia-with-pisa-syndrome-in-parkinson-s-disease-a-case-report
#5
Hisanao Akiyama, Saki Nukui, Masashi Akamatu, Yasuhiro Hasegawa, Osamu Nishikido, Soichiro Inoue
BACKGROUND: Spinal cord stimulation (SCS) has recently been reported to be effective for truncal postural abnormalities such as camptocormia and Pisa syndrome in Parkinson's disease. In this case report, we describe a case of a woman with Parkinson's disease in whom SCS was effective for painful camptocormia with Pisa syndrome. CASE PRESENTATION: A 65-year-old woman was admitted to our hospital because of painful camptocormia. She had noticed resting tremor in the left upper limb and aprosody at 48 years of age...
August 3, 2017: BMC Neurology
https://www.readbyqxmd.com/read/28738644/biosensor-for-the-characterisation-of-hmao-b-inhibitors-and-the-quantification-of-selegiline
#6
Maximilian Aigner, Patricia Preissegger, Kurt Kalcher, Eda Mehmeti, Peter Macheroux, Dale Edmondson, Astrid Ortner
A novel human monoamine oxidase B (hMAO B) based biosensor for inhibitory measurements was developed. It allows both the characterisation of the type of enzyme inhibition and the sensitive and simple determination of inhibitors like selegiline hydrochloride. The sensor consists of a screen printed carbon working electrode modified with 20% manganese dioxide (MnO2) and the enzyme hMAO B, which was immobilised on the electrode via a dialysis membrane (regenerated cellulose, molecular weight cut-off 14000). Inhibition of hMAO B is evaluated by adding different concentrations of the inhibitor selegiline hydrochloride to the enzyme and applying a defined amount of the hMAO B substrate phenylethylamine (PEA)...
November 1, 2017: Talanta
https://www.readbyqxmd.com/read/28737446/quantitative-in-vitro-phenotyping-and-prediction-of-drug-interaction-potential-of-cyp2b6-substrates-as-victims
#7
Raghava Choudary Palacharla, Ramakrishna Nirogi, Venkatesham Uthukam, Arunkumar Manoharan, Ranjith Kumar Ponnamaneni, Ilayaraja Kalaikadhiban
1. Determination of fm, CYP for a compound is critical to assess the potential risk of a drug candidate as a victim of DDI. Several compounds are identified as CYP2B6 substrates but the fm, CYP2B6 values are not determined quantitatively 2. Two methods of reaction phenotyping, the chemical inhibition method, and metabolism in rCYP enzymes, were used to determine the relative contributions of the enzymes. Chemical inhibition method was also conducted in the presence of BSA (0.5% w/v) 3. The results confirm with the earlier studies concerning the identity of the CYP2B6 enzyme...
July 24, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28682134/brain-targeted-delivery-of-mucoadhesive-thermosensitive-nasal-gel-of-selegiline-hydrochloride-for-treatment-of-parkinson-s-disease
#8
Vinay Sridhar, Sarika Wairkar, Ram Gaud, Amrita Bajaj, Pramod Meshram
Selegiline hydrochloride (SL), is an Anti-Parkinson's agent, has low oral bioavailability due to its high first pass metabolism and scarce oral absorption. In the present study, SL mucoadhesive nasal thermosensitive gel (SNT-gel) was prepared to enhance the bioavailability and subsequently, its concentration in the brain. The SNT-gel was prepared using Poloxamer 407-Chitosan combination and optimized formulation was further evaluated for physicochemical parameters. The comparative pharmacodynamic studies including behavioral studies, biochemical testing and histopathology of the brain was carried out in rats for SNT-gel, SL-nasal solution and SL Marketed Tablets...
July 6, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28649132/reassessment-of-subacute-mptp-treated-mice-as-animal-model-of-parkinson-s-disease
#9
Qiu-Shuang Zhang, Yang Heng, Zheng Mou, Ju-Yang Huang, Yu-He Yuan, Nai-Hong Chen
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model remains the most commonly used animal model of Parkinson's disease (PD). There are three MPTP-treatment schemes: acute, subacute and chronic. Considering the advantages of the period and similarity to PD, the subacute model was often chosen to assess the validity of new candidates, but the changes caused by the subacute MPTP treatment and the appropriate positive control for this model remain to be further confirmed. The aim of this study was: 1 to estimate the value of the subacute MPTP mouse model in aspects of behavioral performance, biochemical changes and pathological abnormalities, and 2 to find effective positive drugs...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28643087/antioxidant-and-antiapoptotic-actions-of-selegiline-protect-against-3-np-induced-neurotoxicity-in-rats
#10
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
#11
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
#12
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...
August 1, 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
#13
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
#14
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
#15
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
#16
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
#17
Rebecca L Bauer, Joanne Orfei, Christina L Wichman
No abstract text is available yet for this article.
July 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
#18
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
#19
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
#20
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
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