keyword
MENU ▼
Read by QxMD icon Read
search

MAO-B

keyword
https://www.readbyqxmd.com/read/28435530/small-molecule-lysyl-oxidase-like-2-loxl2-inhibitors-the-identification-of-an-inhibitor-selective-for-loxl2-over-lox
#1
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
#2
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
#3
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...
April 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28377303/the-monoamine-oxidase-inhibition-properties-of-selected-structural-analogues-of-methylene-blue
#4
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...
April 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28368606/anisucoumaramide-a-bioactive-coumarin-from-clausena-anisum-olens
#5
Yun-Song Wang, Bi-Tao Li, Shi-Xi Liu, Zheng-Qi Wen, Jing-Hua Yang, Hong-Bin Zhang, Xiao-Jiang Hao
A new coumarin, anisucoumaramide (1), and a new δ-truxinate derivative, anisumic acid (2), were isolated from Clausena anisum-olens. Their structures were elucidated from extensive NMR and MS data. The absolute configurations of the coumarins were assigned using the experimental and calculated electronic circular dichroism data. Anisucoumaramide (1) represents the first example of a naturally occurring coumarin of which the terpenoidal side chain does not comply with the biosynthesis isoprene rule due to the presence of an unprecedented acetamido motif directly connected with the terpenoidal side chain...
April 3, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28359327/monoamine-oxidase-b-inhibitor-selegiline-reduces-18-f-thk5351-uptake-in-the-human-brain
#6
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/28342849/comparative-effects-of-etoh-consumption-and-thiamine-deficiency-on-cognitive-impairment-oxidative-damage-and-%C3%AE-amyloid-peptide-overproduction-in-the-brain
#7
Yu-Shi Gong, Kun Hu, Lu-Qi Yang, Juan Guo, Yong-Qing Gao, Feng-Lin Song, Fang-Li Hou, Cui-Yi Liang
The effects of chronic EtOH consumption, associated or not with thiamine deficiency (TD), on cognitive impairment, oxidative damage, and β-amyloid (Aβ) peptide accumulation in the brain were investigated in male C57BL/6 mice. We established an alcoholic mouse model by feeding an EtOH liquid diet, a TD mouse model by feeding a thiamine-depleted liquid diet, and an EtOH treatment associated with TD mouse model by feeding a thiamine-depleted EtOH liquid diet for 7 weeks. The learning and memory functions of the mice were detected through the Y-maze test...
March 22, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#8
Min-Ho Nam, Moosung Park, Hyeri Park, Youngjae Kim, Seulki Yoon, Vikram Shahaji Sawant, Ji Won Choi, Jong-Hyun Park, Ki Duk Park, Sun-Joon Min, C Justin Lee, Hyunah Choo
To develop novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was compound 5b, 6-fluoro-2-(1-methyl-1H-indol-5-yl)benzo[d]thiazole with an IC50 value of 28 nM with no apparent effect on MAO-A activity at 10 μM. Based on the reversibility assay, compound 5b turned out to be fully reversible with over 95% of recovery of enzyme activity after washout of the compound...
March 30, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28320274/brain-mitochondrial-subproteome-of-rpn10-binding-proteins-and-its-changes-induced-by-the-neurotoxin-mptp-and-the-neuroprotector-isatin
#9
A E Medvedev, O A Buneeva, A T Kopylov, O V Tikhonova, M V Medvedeva, L N Nerobkova, I G Kapitsa, V G Zgoda
Mitochondria play an important role in molecular mechanisms of neuroplasticity, adaptive changes of the brain that occur in the structure and function of its cells in response to altered physiological conditions or development of pathological disorders. Mitochondria are a crucial target for actions of neurotoxins, causing symptoms of Parkinson's disease in various experimental animal models, and also neuroprotectors. Good evidence exists in the literature that mitochondrial dysfunction induced by the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) influences functioning of the ubiquitin-proteasomal system (UPS) responsible for selective proteolytic degradation of proteins from various intracellular compartments (including mitochondria), and neuroprotective effects of certain antiparkinsonian agents (monoamine oxidase inhibitors) may be associated with their effects on UPS...
March 2017: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/28320234/gelidiella-acerosa-protects-against-a%C3%AE-25-35-induced-toxicity-and-memory-impairment-in-swiss-albino-mice-an-in-vivo-report
#10
Syad Arif Nisha, Kasi Pandima Devi
CONTEXT: Alzheimer's disease (AD) is believed to develop due to deposition of β-amyloid (Aβ) peptide. Hence, efforts are being made to develop potent drug that target amyloid hypothesis. OBJECTIVE: The present study explores the effect of the seaweed Gelidiella acerosa (Forsskål) Feldmann & Hamel (Gelidiellaceae) against Aβ 25-35 peptide in Swiss albino mice. MATERIALS AND METHODS: The animals were administered through intracerebroventricular (ICV) injection with the Aβ 25-35 peptide (10 μg/10 μL/ICV site) on 21st day of the pretreatment of G...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28302559/in-vitro-monoamine-oxidase-inhibition-potential-of-alpha-methyltryptamine-analog-new-psychoactive-substances-for-assessing-possible-toxic-risks
#11
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...
March 13, 2017: Toxicology Letters
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
#12
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...
March 15, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28294055/therapeutic-molecular-and-computational-aspects-of-novel-monoamine-oxidase-mao-inhibitors
#13
M Ramesh, Yussif M Dokurugu, Michael D Thompson, Mahmoud Soliman
Due to the limited number of MAOs inhibitors in the clinic and several research efforts are aimed at the discovery of novel MAOs inhibitors. At present, high specificity and a reversible mode of inhibition of MAO-A/B are cited as desirable traits in drug discovery process. This will help to reduce the probability of causing target disruption and may increase the duration of action. Most of the existing MAO inhibitors lead to side effects due to lack of affinity and selectivity. Therefore, there is an urgent need to design novel, potent, reversible and selective inhibitors for MAO-A/B...
March 10, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28291352/understanding-the-molecular-determinant-of-reversible-human-monoamine-oxidase-b-inhibitors-containing-2h-chromen-2-one-core-structure-based-and-ligand-based-derived-three-dimensional-quantitative-structure-activity-relationships-predictive-models
#14
Milan Mladenović, Alexandros Patsilinakos, Adele Pirolli, Manuela Sabatino, Rino Ragno
Monoamine oxidase B (MAO B) catalyzes the oxidative deamination of aryalkylamines neurotransmitters with concomitant reduction of oxygen to hydrogen peroxide. Consequently, the enzyme's malfunction can induce oxidative damage to mitochondrial DNA and mediates development of Parkinson's disease. Thus, MAO B emerges as a promising target for developing pharmaceuticals potentially useful to treat this vicious neurodegenerative condition. Aiming to contribute to the development of drugs with the reversible mechanism of MAO B inhibition only, herein, an extended in silico-in vitro procedure for the selection of novel MAO B inhibitors is demonstrated, including the following: (1) definition of optimized and validated structure-based three-dimensional (3-D) quantitative structure-activity relationships (QSAR) models derived from available cocrystallized inhibitor-MAO B complexes; (2) elaboration of SAR features for either irreversible or reversible MAO B inhibitors to characterize and improve coumarin-based inhibitor activity (Protein Data Bank ID: 2V61 ) as the most potent reversible lead compound; (3) definition of structure-based (SB) and ligand-based (LB) alignment rule assessments by which virtually any untested potential MAO B inhibitor might be evaluated; (4) predictive ability validation of the best 3-D QSAR model through SB/LB modeling of four coumarin-based external test sets (267 compounds); (5) design and SB/LB alignment of novel coumarin-based scaffolds experimentally validated through synthesis and biological evaluation in vitro...
April 24, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28289795/-pharmacological-treatment-of-motor-symptoms-in-parkinson-s-diseases
#15
W H Jost
Since the 1960s many substance classes have been introduced for treatment of idiopathic Parkinson's disease. The most important and effective medication is levodopa (L-dopa) always in combination with a decarboxylase inhibitor. In addition, dopamine agonists, monoamine oxidase B (MAO-B) inhibitors, catechol-o-methyltransferase (COMT) inhibitors, N‑methyl-D-aspartate (NMDA) antagonists and very rarely anticholinergics are administered depending on the motor symptoms, age and a multitude of other factors. Fortunately, within the substance classes there are various preparations, which also have different effects...
March 13, 2017: Der Nervenarzt
https://www.readbyqxmd.com/read/28279509/-medical-and-surgical-treatment-of-parkinson-s-disease
#16
REVIEW
Luc Defebvre, Caroline Moreau
The treatment of Parkinson's disease is symptomatic with the use of dopaminergic medications: levodopa, dopaminergic agonists and enzymatic inhibitors. At the initial stage, the main goals are to improve the quality of life of patients and delay the onset of motor complications, using a combination of these therapies taking into account both clinical disability and tolerance of different treatments. At the stage of motor and non-motor fluctuations inhibitors of MAO-B and COMT are proposed; amantadine may limit moderate dyskinesias...
March 2017: La Presse Médicale
https://www.readbyqxmd.com/read/28273563/discovery-of-highly-selective-and-potent-monoamine-oxidase-b-inhibitors-contribution-of-additional-phenyl-rings-introduced-into%C3%A2-2-aryl-1-3-4-oxadiazin-5-6h-one
#17
Jungeun Lee, Yeongcheol Lee, So Jung Park, Joohee Lee, Yeong Shik Kim, Young-Ger Suh, Jeeyeon Lee
Monoamine oxidase B (MAO-B) is a flavin adenine dinucleotide (FAD)-containing enzyme that plays a major role in the oxidative deamination of biogenic amines and neurotransmitters. Inhibiting MAO-B activity is a promising approach in the treatment of neurological disorders. Here, we report a series of 2-aryl-1,3,4-oxadiazin-5(6H)-one derivatives as highly selective and potent MAO-B inhibitors. Analysis of the binding sites of hMAO-A and hMAO-B led to design of linear analogs of 2-aryl-1,3,4-oxadiazin-5(6H)-one with an additional phenyl ring...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28267984/pyridoxine-resveratrol-hybrids-mannich-base-derivatives-as-novel-dual-inhibitors-of-ache-and-mao-b-with-antioxidant-and-metal-chelating-properties-for-the-treatment-of-alzheimer-s-disease
#18
Xia Yang, Xiaoming Qiang, Yan Li, Li Luo, Rui Xu, Yunxiaozhu Zheng, Zhongcheng Cao, Zhenghuai Tan, Yong Deng
A series of pyridoxine-resveratrol hybrids Mannich base derivatives as multifunctional agents have been designed, synthesized and evaluated for cholinesterase (ChE) and monoamine oxidase (MAO) inhibitory activity. To further explore the multifunctional properties of the new derivatives, their antioxidant activities and metal-chelating properties were also tested. The results showed that most of these compounds could selectively inhibit acetylcholinesterase (AChE) and MAO-B. Among them, compounds 7d and 8b exhibited the highest potency for AChE inhibition with IC50 values of 2...
February 28, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28251489/evaluation-of-the-inhibitory-effects-of-eckol-and-dieckol-isolated-from-edible-brown-alga-eisenia-bicyclis-on-human-monoamine-oxidases-a-and-b
#19
Hyun Ah Jung, Anupom Roy, Jee H Jung, Jae Sue Choi
Eckol and dieckol are important phlorotannins found in edible brown algae including Eisenia bicyclis, Ecklonia stolonifera, and others. Inhibition of monoamine oxidase (MAO) play an important role in the early management of Parkinson's disease (PD). The aim of this study was to determine the effectiveness of eckol and dieckol isolated from the methanolic extract of E. bicyclis against PD by the inhibition of human MAO-A and MAO-B (hMAO-A and hMAO-B). A sensitive enzyme-based chemiluminescent assay and kinetics methods were used to investigate enzyme inhibition and mode of inhibition...
March 1, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28251298/perseveration-in-a-spatial-discrimination-serial-reversal-learning-task-is-differentially-affected-by-mao-a-and-mao-b-inhibition-and-associated-with-reduced-anxiety-and-peripheral-serotonin-levels
#20
Peter Zhukovsky, Johan Alsiö, Bianca Jupp, Jing Xia, Chiara Guiliano, Lucy Jenner, Jessica Griffiths, Errin Riley, Sajeed Ali, Angela C Roberts, Trevor W Robbins, Jeffrey W Dalley
RATIONALE: Impairments in behavioral flexibility lie at the core of anxiety and obsessive-compulsive disorders. Few studies, however, have investigated the neural substrates of natural variation in behavioral flexibility and whether inflexible behavior is linked to anxiety and peripheral markers of stress and monoamine function. OBJECTIVE: The objective of the study was to investigate peripheral and central markers associated with perseverative behavior on a spatial-discrimination serial reversal learning task...
March 2, 2017: Psychopharmacology
keyword
keyword
41397
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"