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https://www.readbyqxmd.com/read/28487125/design-synthesis-and-biological-evaluation-of-3-4-dihydro-2-1h-quinoline-o-alkylamine-derivatives-as-new-multipotent-cholinesterase-monoamine-oxidase-inhibitors-for-the-treatment-of-alzheimer-s-disease
#1
Zhipei Sang, Wanli Pan, Keren Wang, Qinge Ma, Lintao Yu, Wenmin Liu
A new family of multitarget molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase (MAO) A and B, has been synthesized. Novel 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives have been designed using a conjunctive approach that combines the JMC49 and donepezil. The most promising compound TM-33 showed potent and balance inhibitory activities toward ChE and MAO (eeAChE, eqBuChE, hMAO-A and hMAO-B with IC50 values of 0.56μM, 2.3μM, 0...
April 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28474547/new-hmao-a-inhibitors-with-potential-antidepressant-activity-design-synthesis-biological-screening-and-evaluation-of-pharmacological-activity
#2
Begüm Evranos Aksöz, Gülberk Uçar, Sadık Taşkın Taş, Erkan Aksöz, Kemal Yelekçi, Açelya Erikçi, Yıldırım Sara, Alper İskit
A series of new 2-pyrazoline and hydrazone derivatives were synthesized. Their structural elucidation was performed by IR, 1H NMR, 13C NMR, mass spectral data, and elemental analyses. The MAO inhibitory and antidepressant activities of the novel compounds were investigated by in vitro and in vivo screening tests. All compounds inhibited recombinant hMAO-A potently, competetively and reversibly. All of the compounds inhibited hMAO-A more potently than moclobemide, the well known reversible MAO-A inhibitor. Compounds 8a, 8b, 8c, 8d, 8e and 8g inhibited hMAO-A more selectively than moclobemide...
May 3, 2017: Combinatorial Chemistry & High Throughput Screening
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
#3
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
#4
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
#5
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/28454595/expenditure-and-financial-burden-for-the-diagnosis-and-treatment-of-colorectal-cancer-in-china-a-hospital-based-multicenter-cross-sectional-survey
#6
Hui-Yao Huang, Ju-Fang Shi, Lan-Wei Guo, Ya-Na Bai, Xian-Zhen Liao, Guo-Xiang Liu, A-Yan Mao, Jian-Song Ren, Xiao-Jie Sun, Xin-Yu Zhu, Le Wang, Bing-Bing Song, Ling-Bin Du, Lin Zhu, Ji-Yong Gong, Qi Zhou, Yu-Qin Liu, Rong Cao, Ling Mai, Li Lan, Xiao-Hua Sun, Ying Ren, Jin-Yi Zhou, Yuan-Zheng Wang, Xiao Qi, Pei-An Lou, Dian Shi, Ni Li, Kai Zhang, Jie He, Min Dai
BACKGROUND: The increasing prevalence of colorectal cancer (CRC) in China and the paucity of information about relevant expenditure highlight the necessity of better understanding the financial burden and effect of CRC diagnosis and treatment. We performed a survey to quantify the direct medical and non-medical expenditure as well as the resulting financial burden of CRC patients in China. METHODS: We conducted a multicenter, cross-sectional survey in 37 tertiary hospitals in 13 provinces across China between 2012 and 2014...
April 28, 2017: Chinese Journal of Cancer
https://www.readbyqxmd.com/read/28435530/small-molecule-lysyl-oxidase-like-2-loxl2-inhibitors-the-identification-of-an-inhibitor-selective-for-loxl2-over-lox
#7
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/28435523/discovery-of-1-2-3-triazolo-4-5-d-pyrimidine-derivatives-as-novel-lsd1-inhibitors
#8
Zhong-Hua Li, Xue-Qi Liu, Peng-Fei Geng, Feng-Zhi Suo, Jin-Lian Ma, Bin Yu, Tao-Qian Zhao, Zhao-Qing Zhou, Chen-Xi Huang, Yi-Chao Zheng, Hong-Min Liu
Lysine specific demethylase 1 (LSD1) plays a pivotal role in regulating the lysine methylation. The aberrant overexpression of LSD1 has been reported to be involved in the progression of certain human malignant tumors. Abrogation of LSD1 with RNAi or small molecule inhibitors may lead to the inhibition of cancer proliferation and migration. Herein, a series of [1,2,3]triazolo[4,5-d]pyrimidine derivatives were synthesized and evaluated for their LSD1 inhibitory effects. The structure-activity relationship studies (SARs) were conducted by exploring three regions of this scaffold, leading to the discovery of compound 27 as potent LSD1 inhibitor (IC50 = 0...
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
#9
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
#10
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/28418735/polymorphisms-of-comt-c-649g-a-mao-a-c-1460c-t-net-c-1287g-a-genes-and-the-level-of-catecholamines-serotonin-in-patients-with-parkinson-s-disease
#11
Jolanta Florczak-Wyspianska, Agata Rozycka, Lukasz Wolny, Margarita Lianeri, Wojciech Kozubski, Jolanta Dorszewska
The purpose of this study was to determine the concentration of plasma norepinephrine (NE), epinephrine (E), and serotonin (5-HT) in two collections, after a 30-min supine (I) and 5-min upright position (II), and polymorphisms of genes, COMT (c.649G>A), MAO-A (c.1460C>T), and NET (c.1287G>A), in patients with Parkinson's disease (PD) and other degenerative parkinsonism and controls. The study was performed in 49 PD patients, 19 parkinsonism patients, and 48 controls. The level of NE, E, and 5-HT was determined by HPLC/EC...
April 18, 2017: DNA and Cell Biology
https://www.readbyqxmd.com/read/28418429/chemical-constituents-radical-scavenging-activity-and-enzyme-inhibitory-capacity-of-fruits-from-cotoneaster-pannosus-franch
#12
Francisco Les, Víctor López, Giovanni Caprioli, Romilde Iannarelli, Dennis Fiorini, Marzia Innocenti, Maria Bellumori, Filippo Maggi
Cotoneaster pannosus (Rosaceae) is a semievergreen shrub, producing globose dark red pomes, native to China and widely used as an ornamental plant all over the world. Despite its extensive cultivation, little information is available on the chemical composition and biological activities of its fruits. In this work, the analysis of the chemical composition of C. pannosus fruits, in terms of phenolic components, carotenoids and ascorbic acid by HPLC/DAD, HPLC/ESI-MS and MS/MS as well as in terms of macro- and micro-nutrients was performed...
April 18, 2017: Food & Function
https://www.readbyqxmd.com/read/28416295/depressive-symptoms-in-schizophrenia-and-dopamine-and-serotonin-gene-polymorphisms
#13
Vjekoslav Peitl, Mario Štefanović, Dalibor Karlović
Although depressive symptoms seem to be frequent in schizophrenia they have received significantly less attention than other symptom domains. As impaired serotonergic and dopaminergic neurotransmission is implicated in the pathogenesis of depression and schizophrenia this study sought to investigate the putative association between several functional gene polymorphisms (SERT 5-HTTLPR, MAO-A VNTR, COMT Val158Met and DAT VNTR) and schizophrenia. Other objectives of this study were to closely examine schizophrenia symptom domains by performing factor analysis of the two most used instruments in this setting (Positive and negative syndrome scale - PANSS and Calgary depression rating scale - CDSS) and to examine the influence of investigated gene polymorphisms on the schizophrenia symptom domains, focusing on depressive scores...
April 14, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28404874/identification-of-jl1037-as-a-novel-specific-reversible-lysine-specific-demethylase-1-inhibitor-that-induce-apoptosis-and-autophagy-of-aml-cells
#14
Shuang Liu, Wenting Lu, Shouyun Li, Saisai Li, Jia Liu, Yuanyuan Xing, Shuzu Zhang, Joe Zhongxiang Zhou, Haiyan Xing, Yingxi Xu, Qing Rao, Chengjun Deng, Min Wang, Jianxiang Wang
Lysine-specific demethylase 1 (LSD1) has been recognized as a potential therapeutic target for acute myeloid leukemia (AML). Herein, we identified a novel LSD1 inhibitor, JL1037, via Computer Aided Drug Design technology. JL1037 is a potent, selective and reversible LSD1 inhibitor with IC50s of 0.1 μM and >1.5 μM for LSD1 and monoamine oxidases A/B (MAO-A/B), respectively. Treatment of THP-1 and Kasumi-1 cell lines with JL1037 resulted in dose dependent accumulation of H3K4me1 and H3K4me2, the major substrates of LSD1, as well as inhibition of cell proliferation, blockade of cell cycle and induction of apoptosis...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28400844/effects-of-electroacupuncture-on-methamphetamine-induced-behavioral-changes-in-mice
#15
Tsung-Jung Ho, Chiang-Wen Lee, Zi-Yun Lu, Hsien-Yuan Lane, Ming-Horng Tsai, Ing-Kang Ho, Chieh-Liang Huang, Yao-Chang Chiang
Methamphetamine (METH) is a major drug of abuse worldwide, and no efficient therapeutic strategies for treating METH addiction are currently available. Continuous METH use can cause behavioral upregulation or psychosis. The dopaminergic pathways, particularly the neural circuitry from the ventral tegmental area to the nucleus accumbens (NAc), have a critical role in this behavioral stage. Acupuncture has been used for treating diseases in China for more than 2000 years. According to a World Health Organization report, acupuncture can be used to treat several functional disorders, including substance abuse...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28377303/the-monoamine-oxidase-inhibition-properties-of-selected-structural-analogues-of-methylene-blue
#16
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/28365907/does-patchouli-oil-change-blood-platelet-monoamine-oxidase-a-activity-of-adult-mammals
#17
Md Fazlul Karim, Soumyabrata Banerjee, Mrinal K Poddar
Patchouli oil, an essential aroma oil extracted from patchouli leaf during short-term exposure with five and ten drops either inhibited (at 1 or 2 h) or stimulated (at 4 h) the platelet MAO-A activity depending on the dosages of the aroma oil mainly due to inhibition or stimulation of its K m. The long-term 15 consecutive days exposure (with two or five drops) of patchouli oil, on the other hand, maximally stimulated the platelet MAO-A activity with five drops patchouli oil for 1 h exposure, but further continuation of its exposure with same doses (two or five drops) for 30 consecutive days significantly stimulated (with two drops) and inhibited (with five drops) the platelet MAO-A activity due to stimulation and inhibition respectively of its corresponding both K m and V max...
April 1, 2017: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#18
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/28302559/in-vitro-monoamine-oxidase-inhibition-potential-of-alpha-methyltryptamine-analog-new-psychoactive-substances-for-assessing-possible-toxic-risks
#19
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/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
#20
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
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