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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/28634060/potent-inhibitions-of-monoamine-oxidase-a-and-b-by-acacetin-and-its-7-o-6-o-malonylglucoside-derivative-from-agastache-rugosa
#2
Hyun Woo Lee, Hyung Won Ryu, Seung Cheol Baek, Myung-Gyun Kang, Daeui Park, Hyoung-Yun Han, Ju Hyeon An, Sei-Ryang Oh, Hoon Kim
Five compounds were isolated from the leaves of Agastache rugosa and tested for monoamine oxidase (MAO) inhibitory activity. Acacetin, a flavonoid, potently inhibited recombinant human MAO-A and MAO-B (IC50=0.19 and 0.17μM, respectively), and reversibly and competitively inhibited MAO-A and MAO-B (Ki=0.045 and 0.037μM, respectively). Acacetin 7-O-(6-O-malonylglucoside) (AMG) was also found to effectively inhibit MAO-A and MAO-B (IC50=2.34 and 1.87μM, respectively), and to reversibly and competitively inhibit MAO-A and MAO-B (Ki=1...
June 17, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28629145/synthesis-and-evaluation-of-phenylxanthine-derivatives-as-potential-dual-a2ar-antagonists-mao-b-inhibitors-for-parkinson-s-disease
#3
Xuebao Wang, Chao Han, Yong Xu, Kaiqi Wu, Shuangya Chen, Mangsha Hu, Luyao Wang, Yun Ye, Faqing Ye
The aim of this research was to prove the speculation that phenylxanthine (PX) derivatives possess adenosine A2A receptor (A2AR)-blocking properties and to screening and evaluate these PX derivatives as dual A2AR antagonists/MAO-B inhibitors for Parkinson's disease. To explore this hypothesis, two series of PX derivatives were prepared and their antagonism against A2AR and inhibition against MAO-B were determined in vitro. In order to evaluate further the antiparkinsonian properties, pharmacokinetic and haloperidol-induced catalepsy experiments were carried out in vivo...
June 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28623006/a-longevity-study-with-enhancer-substances-selegiline-bpap-detected-an-unknown-tumor-manifestation-suppressing-regulation-in-rat-brain
#4
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/28611642/a-case-report-of-severe-delirium-after-amantadine-withdrawal
#5
Franz Marxreiter, Jürgen Winkler, Martin Uhl, Dominik Madžar
Amantadine is frequently used in addition to dopaminergic substances like dopamine agonists or L-Dopa in advanced Parkinson disease (PD). However, adverse effects like hallucinations limit its use. PD patients developing severe psychotic symptoms upon treatment with either dopaminergic substances and/or amantadine need to stop intake of any psychotropic substance. Here, we report the case of a 71-year-old PD patient without previously known cognitive impairment. He presented with drug-induced psychotic symptoms due to changes in his therapeutic regimen (increase in COMT inhibitors, newly introduced MAO B inhibitors)...
January 2017: Case Reports in Neurology
https://www.readbyqxmd.com/read/28599322/monoamine-oxidase-a-upregulated-by-chronic-intermittent-hypoxia-activates-indoleamine-2-3-dioxygenase-and-neurodegeneration
#6
Chun-Sing Lam, Jing-Jie Li, George Lim Tipoe, Moussa B H Youdim, Man-Lung Fung
Co-morbid depression is prevalent in patients with obstructive sleep apnea. Here we report that monoamine oxidase A (MAO-A) plays pathogenic roles in the comorbidity. We found that chronic intermittent hypoxia significantly increased the MAO-A expression in the rat hippocampus and markedly decreased the dendritic length and spine density in the pyramidal neurons with less pre- and post-synaptic proteins. The MAO-A upregulation resulted in increased 5-hydroxyindoleacetic acid/serotonin ratio, oxidative stress, leading to NF-κB activation, inflammation and apoptosis...
2017: PloS One
https://www.readbyqxmd.com/read/28577983/monoamine-oxidase-inhibitory-activity-of-methoxy-substituted-chalcones
#7
Bijo Mathew, Githa Elizabeth Mathew, Gulberk Ucar, Monu Joy, E K Nafna, Jerad Suresh
The MAO-B inhibitory activity of chalcone (1, 3- diphenyl-2-propen-1-one) based compounds arise from its structural similarity with 1, 4-diphenyl-2-butene, a known MAO-B inhibitor. Based on our previous report, the methoxy-substituted with fluorine containing chalcones are promising reversible MAO-B inhibitors, while in the present study, a series of methoxylated chalcones (C1-C9) bearing substitution on the para position of ring B was synthesized and evaluated for their human monoamine oxidase inhibitory activity...
May 31, 2017: International Journal of Biological Macromolecules
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
#8
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/28554414/treatment-strategies-in-early-parkinson-s-disease
#9
Luca Marsili, Roberto Marconi, Carlo Colosimo
The clinicians' approach to the treatment of early Parkinson's disease (PD) should take into account numerous aspects, including how to inform a patient upon diagnosis and the critical decision of what therapy to adopt and when to start it. The treatment of the motor disorder associated with early PD needs to consider several crucial factors, such as age at onset, comorbidities, and the patient's functional requirements, and cannot be summarized in a simple formula. In younger patients (i.e., before the age of 70) and in those without high functional requirements, treatment is usually initiated with dopamine agonists and/or monoamine oxidase-B enzyme inhibitors (MAO-B I)...
2017: International Review of Neurobiology
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
#10
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/28550255/sembragiline-in-moderate-alzheimer-s-disease-results-of-a-randomized-double-blind-placebo-controlled-phase-ii-trial-mayflower-road
#11
Stephane Nave, Rachelle S Doody, Mercè Boada, Timo Grimmer, Juha-Matti Savola, Paul Delmar, Meike Pauly-Evers, Tania Nikolcheva, Christian Czech, Edilio Borroni, Benedicte Ricci, Juergen Dukart, Marie Mannino, Tracie Carey, Emma Moran, Inma Gilaberte, Nicoletta Milani Muelhardt, Irene Gerlach, Luca Santarelli, Susanne Ostrowitzki, Paulo Fontoura
BACKGROUND: Sembragiline is a potent, selective, long-acting, and reversible MAO-B inhibitor developed as a potential treatment for Alzheimer's disease (AD). OBJECTIVE: To evaluate the safety, tolerability, and efficacy of sembragiline in patients with moderate AD. METHODS: In this Phase II study (NCT01677754), 542 patients with moderate dementia (MMSE 13-20) on background acetylcholinesterase inhibitors with/without memantine were randomized (1:1:1) to sembragiline 1 mg, 5 mg, or placebo once daily orally for 52 weeks...
May 26, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28546851/monoamine-oxidases-oxidative-stress-and-altered-mitochondrial-dynamics-in-cardiac-ageing
#12
REVIEW
Damien Maggiorani, Nicola Manzella, Dale E Edmondson, Andrea Mattevi, Angelo Parini, Claudia Binda, Jeanne Mialet-Perez
The advances in healthcare over the past several decades have resulted in populations now living longer. With this increase in longevity, a wider prevalence of cardiovascular diseases is more common and known to be a major factor in rising healthcare costs. A wealth of scientific evidence has implicated cell senescence as an important component in the etiology of these age-dependent pathologies. A number of studies indicate that an excess of reactive oxygen species (ROS) contributes to trigger and accelerate the cardiac senescence processes, and a new role of monoamine oxidases, MAO-A and MAO-B, is emerging in this context...
2017: Oxidative Medicine and Cellular Longevity
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
#13
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/28462452/saffron-crocus-sativus-l-tea-intake-prevents-learning-memory-defects-and-neurobiochemical-alterations-induced-by-aflatoxin-b1-exposure-in-adult-mice
#14
Zacharoula I Linardaki, Fotini N Lamari, Marigoula Margarity
This study aimed to investigate the potential neurotoxic effects of aflatoxin B1 (AFB1) and the preventive effects of saffron. Male Balb-c mice received AFB1 (0.6 mg/kg/day intraperitoneally for 4 days), saffron infusion (90 mg styles/200 mL, ad libitum access for 2 weeks) or saffron infusion plus AFB1 (saffron treatment as previously plus 0.6 mg AFB1/kg/day intraperitoneally for the last 4 days). Control mice were intraperitoneally injected with DMSO:saline (1:1, v/v) during AFB1 treatment. Learning/memory was assessed by passive avoidance task...
May 2, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28456940/mptp-mouse-model-of-preclinical-and-clinical-parkinson-s-disease-as-an-instrument-for-translational-medicine
#15
Eduard R Mingazov, Gulnara R Khakimova, Elena A Kozina, Alexei E Medvedev, Olga A Buneeva, Ara S Bazyan, Michael V Ugrumov
Parkinson's disease (PD) is characterized by the appearance of motor symptoms many years after the onset of neurodegeneration, which explains low efficiency of therapy. Therefore, one of the priorities in neurology is to develop an early diagnosis and preventive treatment of PD, based on knowledge of molecular mechanisms of neurodegeneration and neuroplasticity in the nigrostriatal system. However, due to inability to diagnose PD at preclinical stage, research and development must be performed in animal models by comparing the nigrostriatal system in the models of asymptomatic and early symptomatic stages of PD...
April 29, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28456030/the-evaluation-of-1-4-benzoquinones-as-inhibitors-of-human-monoamine-oxidase
#16
Samantha Mostert, Anél Petzer, Jacobus P Petzer
The monoamine oxidase (MAO) enzymes are of considerable pharmacological interest and inhibitors are used in the clinic for the treatment of major depressive disorder and Parkinson's disease. A limited number of studies have shown that the quinone class of compounds possesses MAO inhibition properties. Most notable among these is a report that 2,3,6-trimethyl-1,4-naphthoquinone (TMN), present in extracts of cured tobacco leafs, is a non-selective inhibitor of both MAO isoforms. An older study reports that 1,4-benzoquinone inhibits MAO-A and MAO-B from human synaptosomes...
April 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28435530/small-molecule-lysyl-oxidase-like-2-loxl2-inhibitors-the-identification-of-an-inhibitor-selective-for-loxl2-over-lox
#17
John H Hutchinson, Martin W Rowbottom, David Lonergan, Janice Darlington, Pat Prodanovich, Christopher D King, Jilly F Evans, Gretchen Bain
Two series of novel LOXL2 enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)methanamine 20 (hLOXL2 IC50 = 126 nM), was shown to be selective for LOXL2 over LOX and three other amine oxidases (MAO-A, MAO-B, and SSAO). Compound 20 is the first published small molecule inhibitor selective for LOXL2 over LOX.
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28435083/subchronic-glucocorticoids-glutathione-depletion-and-a-postpartum-model-elevate-monoamine-oxidase-a-activity-in-the-prefrontal-cortex-of-rats
#18
Sofia Raitsin, Junchao Tong, Stephen Kish, Xin Xu, Lilia Magomedova, Carolyn Cummins, Ana C Andreazza, Gustavo Scola, Glen Baker, Jeffrey H Meyer
Recent human brain imaging studies implicate dysregulation of monoamine oxidase-A (MAO-A), in particular in the prefrontal cortex (PFC) and anterior cingulate cortex (ACC), in the development of major depressive disorder (MDD). This study investigates the influence of four alterations underlying important pathologies of MDD, namely, chronic elevation of glucocorticoid levels, glutathione depletion, changes in female gonadal sex hormones and serotonin concentration fluctuation, on MAO-A and MAO-B activity in rats...
April 20, 2017: Brain Research
https://www.readbyqxmd.com/read/28419969/neurotoxic-effects-of-silver-nanoparticles-and-the-protective-role-of-rutin
#19
Mona M Ahmed, Mohamed M A Hussein
The toxicological studies on silver nanoparticles (Ag-NPs) have become a hot topic over the past few decades due to their unique properties on the nanoscale and widespread in many commercial products that launched into the market recently. This study was undertaken to shed light on Ag-NPs toxicity on neurotransmitters with special emphasis on the impact of concurrent administration of rutin with Ag-NPs in the experimental rats. The oral administration of Ag-NPs in rats induced brain oxidative stress, significant alterations in neurotransmitters and amino acids...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28377303/the-monoamine-oxidase-inhibition-properties-of-selected-structural-analogues-of-methylene-blue
#20
COMPARATIVE STUDY
Anzelle Delport, Brian H Harvey, Anél Petzer, Jacobus P Petzer
The thionine dye, methylene blue (MB), is a potent inhibitor of monoamine oxidase (MAO) A, a property that may, at least in part, mediate its antidepressant effects in humans and animals. The central inhibition of MAO-A by MB has also been linked to serotonin toxicity (ST) which may arise when MB is used in combination with serotonergic drugs. Structural analogues and the principal metabolite of MB, azure B, have also been reported to inhibit the MAO enzymes, with all compounds exhibiting specificity for the MAO-A isoform...
June 15, 2017: Toxicology and Applied Pharmacology
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