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https://www.readbyqxmd.com/read/28634836/test-retest-reproducibility-of-11-c-l-deprenyl-d2-binding-to-mao-b-in-the-human-brain
#1
Ryosuke Arakawa, Per Stenkrona, Akihiro Takano, Sangram Nag, Rafael S Maior, Christer Halldin
BACKGROUND: [(11)C]-L-deprenyl-D2 is a positron emission tomography (PET) radioligand for measurement of the monoamine oxidase B (MAO-B) activity in vivo brain. The estimation of the test-retest reproducibility is important for accurate interpretation of PET studies. RESULTS: We performed two [(11)C]-L-deprenyl-D2 scans for six healthy subjects and evaluated the test-retest variability of this radioligand. MAO-B binding was quantified by two tissue compartment model (2TCM) with three rate constants (K 1, k 2, k 3) using metabolite-corrected plasma radioactivity...
December 2017: EJNMMI Research
https://www.readbyqxmd.com/read/28623006/a-longevity-study-with-enhancer-substances-selegiline-bpap-detected-an-unknown-tumor-manifestation-suppressing-regulation-in-rat-brain
#2
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
#3
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
#4
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/28450149/free-radical-production-and-antioxidant-status-in-brain-cortex-non-synaptic-mitochondria-and-synaptosomes-at-alcohol-hangover-onset
#5
Analía G Karadayian, Gabriela Malanga, Analía Czerniczyniec, Paulina Lombardi, Juanita Bustamante, Silvia Lores-Arnaiz
Alcohol hangover (AH) is the pathophysiological state after a binge-like drinking. We have previously demonstrated that AH induced bioenergetics impairments in a total fresh mitochondrial fraction in brain cortex and cerebellum. The aim of this work was to determine free radical production and antioxidant systems in non-synaptic mitochondria and synaptosomes in control and hangover animals. Superoxide production was not modified in non-synaptic mitochondria while a 17.5% increase was observed in synaptosomes...
April 24, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28374768/cortical-laminar-tau-deposits-and-activated-astrocytes-in-alzheimer-s-disease-visualised-by-3-h-thk5117-and-3-h-deprenyl-autoradiography
#6
Laetitia Lemoine, Laure Saint-Aubert, Inger Nennesmo, Per-Göran Gillberg, Agneta Nordberg
Hyperphosphorylated tau protein deposits and, inflammatory processes are characteristic components of Alzheimer disease (AD) pathology. We here aimed to visualize in vitro the distribution of tau deposits and activated astrocytes across the cortical layers in autopsy AD brain tissue using the radiotracers (3)H-THK5117 and (3)H-deprenyl. (3)H-THK5117 and (3)H-deprenyl autoradiographies were carried out on frozen brain sections from three AD patients and one healthy control. (3)H-THK5117 showed a distinct laminar cortical binding similar to (3)H-deprenyl autoradiography, with an extensive binding in the superficial and deep layers of the temporal neocortices, whereas the middle frontal gyrus showed an even binding throughout the layers...
April 4, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28283959/neuroinflammation-in-neurodegenerative-disorders-a-review
#7
REVIEW
Martin Schain, William Charles Kreisl
The potential for positron emission tomography (PET) to detect neuroinflammation in vivo has sparked a remarkable interest in various disciplines of neuroscience. Early PET radioligands, such as [(11)C]PK(R)-11195 for the 18-kDa translocator protein (TSPO) and [(11)C]L-deprenyl for monoamine oxidase B, have been used in studies designed to clarify the role of neuroinflammation in a variety of psychiatric and neurological disorders. Recent years have witnessed the development of several second-generation PET radioligands for TSPO and radioligands to measure endogenous targets that are active in various stages of the inflammatory cascade, such as cyclooxygenase and arachidonic acid...
March 2017: Current Neurology and Neuroscience Reports
https://www.readbyqxmd.com/read/28034283/in-silico-studies-revealed-multiple-neurological-targets-for-the-antidepressant-molecule-ursolic-acid
#8
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/27977122/comparative-analysis-of-the-neurochemical-profile-and-mao-inhibition-properties-of-n-furan-2-ylmethyl-n-methylprop-2-yn-1-amine
#9
Philippe De Deurwaerdère, Claudia Binda, Rémi Corne, Cosima Leone, Aurora Valeri, Massimo Valoti, Rona R Ramsay, Yagamare Fall, José Marco-Contelles
The regulation of brain monoamine levels is paramount for cognitive functions, and the monoamine oxidase (MAO A and B) enzymes play a central role in these processes. The aim of this study was to evaluate whether the procognitive properties exerted by propargylamine N-(furan-2-ylmethyl)-N-methylprop-2-yn-1-amine (F2MPA) are related to changes in monoamine content via MAO inhibition. In vivo microdialysis and ex vivo amine metabolite measurement demonstrated region-specific alterations in monoamine metabolism that differ from both of the classic MAO A and MAO B inhibitors, clorgyline and l-deprenyl, respectively...
December 30, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27901472/effects-of-low-and-high-deprenyl-dose-on-antioxidant-enzyme-activities-in-the-adult-rat-brain
#10
Maria Lalkovicova, Frantiska Horvathova, Igor Sulla, Jozef Mihalik, Viera Danielisova
We evaluated the effects of low dose deprenyl (LDD, 0.0025 mg/kg per day) and high dose deprenyl (HDD, 0.25 mg/kg per day) treatment of male Wistar rats for 30 days on the activities of SOD and CAT in the cortex, striatum, and hippocampus. Total SOD and MnSOD activities were increased with LDD (p <0.05) in the cortex (0.74 ± 0.03; 0.31 ± 0.02), striatum (0.75 ± 0.02; 0.27 ± 0.03) and CA1 region of the hippocampus (0.75 ± 0.02; 0.29 ± 0.03) compared to the control (0.53 ± 0.02; 0.15 ± 0.02), but reduced (p <0...
January 2017: General Physiology and Biophysics
https://www.readbyqxmd.com/read/27861613/non-serotonergic-neurotoxicity-by-mdma-ecstasy-in-neurons-derived-from-mouse-p19-embryonal-carcinoma-cells
#11
Dina Popova, Andréas Forsblad, Sanaz Hashemian, Stig O P Jacobsson
3,4-methylenedioxymethamphetamine (MDMA; ecstasy) is a commonly abused recreational drug that causes neurotoxic effects in both humans and animals. The mechanism behind MDMA-induced neurotoxicity is suggested to be species-dependent and needs to be further investigated on the cellular level. In this study, the effects of MDMA in neuronally differentiated P19 mouse embryonal carcinoma cells have been examined. MDMA produces a concentration-, time- and temperature-dependent toxicity in differentiated P19 neurons, as measured by intracellular MTT reduction and extracellular LDH activity assays...
2016: PloS One
https://www.readbyqxmd.com/read/27777099/longevity-study-with-low-doses-of-selegiline-deprenyl-and-2r-1-1-benzofuran-2-yl-n-propylpentane-2-amine-bpap
#12
J Knoll, I Miklya
AIMS: The first longevity study demonstrating that rats treated with the MAO-B inhibitory dose of (-)-deprenyl (0.25mg/kg) lived significantly longer than their saline-treated peers was published in 1988, and corroborated in many papers. The recent findings that (-)-deprenyl is primarily a PEA-derived synthetic catecholaminergic activity enhancer substance; (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP) is a tryptamine-derived synthetic enhancer substance, initiated our first longevity study on rats with low enhancer doses of (-)-deprenyl and BPAP to test the enhancer effect's role in life extension...
December 15, 2016: Life Sciences
https://www.readbyqxmd.com/read/27633250/positron-emission-tomography-measurement-of-brain-mao-b-inhibition-in-patients-with-alzheimer-s-disease-and-elderly-controls-after-oral-administration-of-sembragiline
#13
MULTICENTER STUDY
Stefan Sturm, Anton Forsberg, Stephane Nave, Per Stenkrona, Nicholas Seneca, Andrea Varrone, Robert A Comley, Patrik Fazio, Candice Jamois, Ryuji Nakao, Zbigniew Ejduk, Nabil Al-Tawil, Ulrika Akenine, Christer Halldin, Niels Andreasen, Benedicte Ricci
PURPOSE: In Alzheimer's disease (AD), increased metabolism of monoamines by monoamine oxidase type B (MAO-B) leads to the production of toxic reactive oxygen species (ROS), which are thought to contribute to disease pathogenesis. Inhibition of the MAO-B enzyme may restore brain levels of monoaminergic neurotransmitters, reduce the formation of toxic ROS and reduce neuroinflammation (reactive astrocytosis), potentially leading to neuroprotection. Sembragiline (also referred as RO4602522, RG1577 and EVT 302 in previous communications) is a potent, selective and reversible inhibitor of MAO-B developed as a potential treatment for AD...
March 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/27597816/key-targets-for-multi-target-ligands-designed-to-combat-neurodegeneration
#14
REVIEW
Rona R Ramsay, Magdalena Majekova, Milagros Medina, Massimo Valoti
HIGHLIGHTS Compounds that interact with multiple targets but minimally with the cytochrome P450 system (CYP) address the many factors leading to neurodegeneration.Acetyl- and Butyryl-cholineEsterases (AChE, BChE) and Monoamine Oxidases A/B (MAO A, MAO B) are targets for Multi-Target Designed Ligands (MTDL).ASS234 is an irreversible inhibitor of MAO A >MAO B and has micromolar potency against the cholinesterases.ASS234 is a poor CYP substrate in human liver, yielding the depropargylated metabolite.SMe1EC2, a stobadine derivative, showed high radical scavenging property, in vitro and in vivo giving protection in head trauma and diabetic damage of endothelium...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27548849/longitudinal-changes-in-csf-alpha-synuclein-species-reflect-parkinson-s-disease-progression
#15
Nour K Majbour, Nishant N Vaikath, Paolo Eusebi, Davide Chiasserini, Mustafa Ardah, Shiji Varghese, M Emdadul Haque, Takahiko Tokuda, Peggy Auinger, Paolo Calabresi, Lucilla Parnetti, Omar M A El-Agnaf
BACKGROUND: Parkinson's disease (PD) diagnosis is mainly based on clinical criteria, with a high risk of misdiagnosis. The identification of reliable biomarkers for disease diagnosis and progression has a key role for developing disease-modifying therapies. In this article, we investigated the longitudinal changes of CSF α-synuclein species in early PD patients and explored the potential use of these species as surrogate biomarkers for PD progression. METHODS: We used our newly developed enzyme-linked immunosorbent assay systems for measuring different forms of α-synuclein, such as oligomeric-α-synuclein, phosphorylated-α-synuclein at serine 129, or total-α-synuclein in CSF from the longitudinal Deprenyl and Tocopherol Antioxidative Therapy for Parkinsonism study cohort (n = 121)...
October 2016: Movement Disorders: Official Journal of the Movement Disorder Society
https://www.readbyqxmd.com/read/27292162/the-effect-of-r-deprenyl-administration-on-antioxidant-enzymes-in-rat-testis
#16
Františka Horváthová, Viera Danielisová, Iveta Domoráková, Peter Solár, Silvia Rybárová, Ingrid Hodorová, Jozef Mihalik
The aim of the study was to investigate the effect of R-(-)-deprenyl administration on the activity and localization of superoxide dismutases (SODs) and catalase (CAT) in rat testis. After 30 days of intraperitoneal administration of either saline (control) or R-(-)-deprenyl dissolved in saline at concentrations of 0.0025mg/kg (low dose of deprenyl, LDD) or 0.25mg/kg (high dose of deprenyl, HDD), males were killed by thiopental, and their testes were collected. We found that deprenyl administration significantly increased the activity of antioxidant enzymes, and this effect varied by dosage...
October 5, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27163379/rats-bred-for-helplessness-exhibit-positive-reinforcement-learning-deficits-which-are-not-alleviated-by-an-antidepressant-dose-of-the-mao-b-inhibitor-deprenyl
#17
Daniela Schulz, Fritz A Henn, David Petri, Joseph P Huston
Principles of negative reinforcement learning may play a critical role in the etiology and treatment of depression. We examined the integrity of positive reinforcement learning in congenitally helpless (cH) rats, an animal model of depression, using a random ratio schedule and a devaluation-extinction procedure. Furthermore, we tested whether an antidepressant dose of the monoamine oxidase (MAO)-B inhibitor deprenyl would reverse any deficits in positive reinforcement learning. We found that cH rats (n=9) were impaired in the acquisition of even simple operant contingencies, such as a fixed interval (FI) 20 schedule...
August 4, 2016: Neuroscience
https://www.readbyqxmd.com/read/27118978/evaluation-of-the-isoflavone-genistein-as-reversible-human-monoamine-oxidase-a-and-b-inhibitor
#18
Najla O Zarmouh, Samia S Messeha, Faisel M Elshami, Karam F A Soliman
Monoamine oxidases inhibitors (MAOIs) are effective therapeutic drugs for managing Parkinson's disease (PD) and depression. However, their irreversibility may lead to rare but serious side effects. As finding safer and reversible MAOIs is our target, we characterized the recombinant human (h) MAO-A and MAO-B inhibition potentials of two common natural isoflavones, genistein (GST) and daidzein (DZ) using luminescence assay. The results obtained showed that DZ exhibits partial to no inhibition of the isozymes examined while GST inhibited hMAO-B (IC50 of 6...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27058977/high-throughput-screening-and-radioligand-binding-studies-reveal-monoamine-oxidase-b-as-the-primary-binding-target-for-d-deprenyl
#19
Anna Lesniak, Mikko Aarnio, Anna Jonsson, Thomas Norberg, Fred Nyberg, Torsten Gordh
AIMS: d-deprenyl is a useful positron emission tomography tracer for visualization of inflammatory processes. Studies with [(11)C]-d-deprenyl showed robust uptake in peripheral painful sites of patients with rheumatoid arthritis or chronic whiplash injury. The mechanism of preferential d-deprenyl uptake is not yet known, but the existence of a specific binding site was proposed. Thus, in the present study, we sought to identify the binding site for d-deprenyl and verify the hypothesis about the possibility of monoamine oxidase enzymes as major targets for this molecule...
May 1, 2016: Life Sciences
https://www.readbyqxmd.com/read/26912447/comparison-of-early-phase-11c-deuterium-l-deprenyl-and-11c-pittsburgh-compound-b-pet-for-assessing-brain-perfusion-in-alzheimer-disease
#20
Elena Rodriguez-Vieitez, Stephen F Carter, Konstantinos Chiotis, Laure Saint-Aubert, Antoine Leuzy, Michael Schöll, Ove Almkvist, Anders Wall, Bengt Långström, Agneta Nordberg
UNLABELLED: The PET tracer (11)C-deuterium-L-deprenyl ((11)C-DED) has been used to visualize activated astrocytes in vivo in patients with Alzheimer disease (AD). In this multitracer PET study, early-phase (11)C-DED and (11)C-Pittsburgh compound B ((11)C-PiB) (eDED and ePiB, respectively) were compared as surrogate markers of brain perfusion, and the extent to which (11)C-DED binding is influenced by brain perfusion was investigated. METHODS: (11)C-DED, (11)C-PiB, and (18)F-FDG dynamic PET scans were obtained in age-matched groups comprising AD patients (n = 8), patients with mild cognitive impairment (n = 17), and healthy controls (n = 16)...
July 2016: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
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