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https://www.readbyqxmd.com/read/28107736/crystal-structures-binding-interactions-and-adme-evaluation-of-brain-penetrant-n-substituted-indazole-5-carboxamides-as-subnanomolar-selective-monoamine-oxidase-b-and-dual-mao-a-b-inhibitors
#1
Nikolay T Tzvetkov, Hans-Georg Stammler, Beate Neumann, Silvia Hristova, Liudmil Antonov, Marcus Gastreich
The pharmacological and physicochemical analysis of structurally optimized N-alkyl-substituted indazole-5-carboxamides, developed as potential drug and radioligand candidates for the treatment and diagnosis of Parkinson's disease (PD) and other neurological disorders, is reported. Recent efforts have been focused on the development of subnanomolar potent, selective MAO-B (N1-alkyl-substituted compounds 12a-14a and 15) and dual active MAO-A/B (N2-methylated compounds 12b-14b) inhibitors with nanomolar potency towards MAO-B and moderately active against MAO-A enzyme, respectively...
January 11, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28097890/novel-1-2-pyrimidin-2-yl-piperazine-derivatives-as-selective-monoamine-oxidase-mao-a-inhibitors
#2
Betül Kaya, Leyla Yurttaş, Begüm Nurpelin Sağlik, Serkan Levent, Yusuf Özkay, Zafer Asim Kaplancikli
In the present study, a new series of 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-substituted piperazine-1-carbodithioate derivatives (2a-n) were synthesized and screened for their monoamine oxidase A and B inhibitory activity. The structures of compounds were elucidated using spectroscopic methods and some physicochemical properties of new compounds were predicted using Molinspiration and MolSoft programs. Compounds 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-(4-nitrophenyl)piperazine-1-carbodithioate (2j) and 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-benzhydrylpiperazine-1-carbodithioate (2m) exhibited selective MAO-A inhibitory activity with IC50 = 23...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097874/through-scaffold-modification-to-3-5-diaryl-4-5-dihydroisoxazoles-new-potent-and-selective-inhibitors-of-monoamine-oxidase-b
#3
Rita Meleddu, Simona Distinto, Roberto Cirilli, Stefano Alcaro, Matilde Yanez, Maria Luisa Sanna, Angela Corona, Claudia Melis, Giulia Bianco, Peter Matyus, Filippo Cottiglia, Elias Maccioni
3,5-Diaryl-4,5-dihydroisoxazoles were synthesized and evaluated as monoamine oxidase (MAO) enzyme inhibitors and iron chelators. All compounds exhibited selective inhibitory activity towards the B isoform of MAO in the nanomolar concentration range. The best performing compound was preliminarily evaluated for its ability to bind iron II and III cations, indicating that neither iron II nor iron III is coordinated. The best compounds racemic mixtures were separated and single enantiomers inhibitory activity evaluated...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28069007/the-benzopyrone-biochanin-a-as-a-reversible-competitive-and-selective-monoamine-oxidase-b-inhibitor
#4
Najla O Zarmouh, Suresh K Eyunni, Karam F A Soliman
BACKGROUND: Monoamine oxidase-B (MAO-B) inhibitors are widely used in the treatment of Parkinson's disease. They increase vital monoamine neurotransmitters in the brain. However, there is a need for safer natural reversible MAO inhibitors with MAO-B selectivity. Our previous studies showed that Psoralea corylifolia seeds (PCS) extract contains compounds that inhibit monoamine oxidase-B. METHODS: In this study, six of PCS constituents sharing a benzopyrone structure were investigated...
January 10, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28068665/potent-inhibition-of-monoamine-oxidase-b-by-a-piloquinone-from-a-marine-derived-streptomyces-sp-cnq-027
#5
Hyun Woo Lee, Hansol Choi, Sang-Jip Nam, William Fenical, Hoon Kim
Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an IC₅₀ value of 1.21 µM; in addition, it was found to be highly effective against MAO-A, with an IC₅₀ value of 6.47 µM. Compound 1 was selective, but not extremely so, for MAO-B compared to MAO-A, with a selectivity index value of 5...
January 9, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28057462/monoamine-oxidase-inhibitory-activity-in-tobacco-particulate-matter-are-harman-and-norharman-the-only-physiologically-relevant-inhibitors
#6
Penelope Truman, Peter Grounds, Katharine A Brennan
Monoamine oxidase inhibition is significant in smokers, but it is still unclear how the inhibition that is seen in the brains and bodies of smokers is brought about. Our aim was to test the contribution of the harman and norharman in tobacco smoke to MAO-A inhibition from tobacco smoke preparations, as part of a re-examination of harman and norharman as the cause of the inhibition of MAO-A inhibition in the brain. Tobacco smoke particulate matter and cigarette smoke particulate matter were prepared and the amounts of harman and norharman measured...
January 3, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/28052533/what-a-difference-a-methyl-group-makes-the-selectivity-of-monoamine-oxidase-b-towards-histamine-and-n-methylhistamine
#7
Aleksandra Maršavelski, Robert Vianello
Monoamine oxidase (MAO) enzymes catalyze the degradation of a very broad range of biogenic and dietary amines including many neurotransmitters in the brain, whose imbalance is extensively linked with the biochemical pathology of various neurological disorders. Although sharing around 70% sequence identity, both MAO A and B isoforms differ in substrate affinities and inhibitor sensitivities. Inhibitors that act on MAO A are used to treat depression, due to their ability to raise serotonin concentrations, while MAO B inhibitors decrease dopamine degradation and improve motor control in patients with Parkinson disease...
January 3, 2017: Chemistry: a European Journal
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/28012831/selective-inhibition-of-mao-a-activity-results-in-an-antidepressant-like-action-of-2-benzoyl-4-iodoselenophene-in-mice
#9
Daniela Velasquez, Caroline Quines, Renan Pistóia, Gilson Zeni, Cristina W Nogueira
Depression is a leading cause of disability worldwide. For this reason, the aim of this study was to investigate the possible antidepressant-like activity of 2-benzoyl-4-iodoselenophene (C17H11IOSe), a selenophene compound, in two well-consolidated behavioral assays for screening antidepressant activity (forced swimming test and tail suspension test) in mice. In order to investigate the mechanism of action of C17H11IOSe, it was investigated the activities of cerebral enzymes: monoamine oxidase MAO A and B and Na(+), K(+) ATPase, and if an inhibitor of serotonin synthesis, p-chlorophenylalanine (pCPA) (100mg/kg) blocks the antidepressant-like effect of C17H11IOSe...
December 21, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/28012396/antidepressant-like-effects-of-hydrolysable-tannins-of-terminalia-catappa-leaf-extract-via-modulation-of-hippocampal-plasticity-and-regulation-of-monoamine-neurotransmitters-subjected-to-chronic-mild-stress-cms
#10
Y Chandrasekhar, E M Ramya, K Navya, G Phani Kumar, K R Anilakumar
Terminalia catappa L. belonging to Combretaceae family is a folk medicine, known for its multiple pharmacological properties, but the neuro-modulatory effect of TC against chronic mild stress was seldom explored. The present study was designed to elucidate potential antidepressant-like effect of Terminalia cattapa (leaf) hydro-alcoholic extract (TC) by using CMS model for a period of 7 weeks. Identification of hydrolysable tannins was done by using LC-MS. After the CMS exposure, mice groups were administered with imipramine (IMP, 10mg/kg, i...
December 21, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27998471/-economic-burden-of-cancer-in-china-during-1996-2014-a-systematic-review
#11
J F Shi, C L Shi, X P Yue, H Y Huang, L Wang, J Li, P A Lou, A Y Mao, M Dai
Objective: To explore the current status of research on economic burden of cancer in China from 1996 to 2014. Methods: The key words including cancer, economic burden, expenditure, cost were used to retrieve the literatures published in CNKI and Wanfang (the two most commonly used databases for literature in Chinese) and PubMed during 1996-2014. A total of 91 studies were included after several exclusionary procedures. Information on subjects and data source, methodology, main results were structurally abstracted...
December 23, 2016: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
https://www.readbyqxmd.com/read/27994633/electroacupuncture-restores-5-ht-system-deficit-in-chronic-mild-stress-induced-depressed-rats
#12
Dongmei Duan, Ya Tu, Xiuyan Yang, Ping Liu
Objective. The current study is designed to investigate the antidepressant efficacy of electroacupuncture (EA) treatment by evaluating its effect on the synthesis, metabolism, reuptake, and receptors of 5-hydroxytryptamine (5-HT), so as to clarify the molecular mechanisms of EA for antidepression. Materials and Methods. Solitary combined with the chronic unpredictable mild stress (CUMS) was used to establish the rat model with depression. The depressed rats were supplied with EA treatment for 4 weeks, and the behavior change and the following indices including 5-HT, 5-hydroxyindoleacetic acid (5-HIAA), monoamine oxidase A (MAO-A), tryptophan hydroxylase (TPH), 5-HT transporter (SERT), 5-HT1A, and 5-HT2A in hippocampus and prefrontal cortex were examined...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27984078/anti-inflammatory-and-protective-effects-of-mt-031-a-novel-multitarget-mao-a-and-ache-buche-inhibitor-in-scopolamine-mouse-model-and-inflammatory-cells
#13
Wei Liu, Alon Rabinovich, Yuval Nash, Dan Frenkel, Yuqiang Wang, Moussa B H Youdim, Orly Weinreb
Previous study demonstrated that the novel multitarget compound, MT-031 preserved in one molecule entity the beneficial properties of its parent drugs, rasagiline and rivastigmine, and exerted high dual potencies of monoamine oxidase-A (MAO-A) and cholinesterase (ChE) inhibition in acute-treated mice and neuroprotective effects against H2O2-induced neurotoxicity in human neuroblastoma SH-SY5Y cells. The present study aimed to further investigate the anti-inflammatory and protective effects of MT-031 in scopolamine mouse model and inflammatory cell cultures...
October 28, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27981510/aberrant-cpg-methylation-mediates-abnormal-transcription-of-mao-a-induced-by-acute-and-chronic-l-3-4-dihydroxyphenylalanine-administration-in-sh-sy5y-neuronal-cells
#14
Zhaofei Yang, Xuan Wang, Jian Yang, Min Sun, Yong Wang, Xiaomin Wang
L-3,4-dihydroxyphenylalanine (L-dopa) remains the most effective drug for therapy of Parkinson's disease (PD); however, long-term use of it causes serious side effects. L-dopa-induced dyskinesia (LID) has consistently been related to L-dopa-derived excessive dopamine release, but the mechanisms have not been addressed very clear. Monoamine oxidase A (MAO-A) is one of the key enzymes in dopamine metabolism and therefore may be involved in L-dopa-induced side effects. And, epigenetic modification controls MAO-A gene transcription...
December 15, 2016: Neurotoxicity Research
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
#15
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/27968842/quality-of-life-and-health-utility-scores-for-common-cancers-in-china-a-multicentre-cross-sectional-survey
#16
Ju-Fang Shi, Hui-Yao Huang, Lan-Wei Guo, Dian Shi, Xiu-Ying Gu, Han Liang, Le Wang, Jian-Song Ren, Ya-Na Bai, A-Yan Mao, Guo-Xiang Liu, Xian-Zhen Liao, Kai Zhang, Jie He, Min Dai
BACKGROUND: The measurement of quality-adjusted life-years (QALYs) forms a key component of cost-utility evaluation in cancer intervention; however, detailed data for utility weights by cancer type and health status are still scarce both in China and other regions. The aim of this study was to systematically evaluate utility scores in relation to the most common six cancers in China in 2012 (lung, breast, colorectal, oesophageal, liver, and stomach cancer). METHODS: As a part of a Screening Program in Urban China (CanSPUC) supported by the central government of China, we undertook a cross-sectional survey in 13 provinces across China from 2013 to 2014...
October 2016: Lancet
https://www.readbyqxmd.com/read/27968822/expenditure-and-financial-burden-for-common-cancers-in-china-a-hospital-based-multicentre-cross-sectional-study
#17
Hui-Yao Huang, Ju-Fang Shi, Lan-Wei Guo, Xin-Yu Zhu, Le Wang, Xian-Zhen Liao, Guo-Xiang Liu, Ya-Na Bai, A-Yan Mao, Jian-Song Ren, Xiao-Jie Sun, Kai Zhang, Jie He, Min Dai
BACKGROUND: Comprehensive health economic evaluation, a key component of the Cancer Screening Program in Urban China (CanSPUC), was expected to support government policy-making on screening initiatives for common cancers (lung, breast, colorectal, oesophageal, liver, and stomach cancer) in urban China. Estimation of expenditure for cancer diagnosis and treatment from a societal perspective was an essential component. The aim of this study was to estimate direct medical and non-medical expenditure and to discern the resultant financial burden...
October 2016: Lancet
https://www.readbyqxmd.com/read/27926950/c6-and-c7-substituted-3-4-dihydro-2-1h-quinolinones-as-inhibitors-of-monoamine-oxidase
#18
L Meiring, J Petzer, A Petzer
Purpose Monoamine oxidase (MAO) inhibitors are considered to be useful therapeutic agents and isoform specific inhibitors are employed for the treatment of depression and Parkinson's disease. MAO inhibitors are also under investigation for the treatment of disorders ranging from Alzheimer's disease, prostate cancer and certain cardiomyopathies. While a number of irreversible MAO inhibitors are available in the clinic, reversible inhibitors, particularly of the MAO-B isoform are still being developed. Based on our interest in discovering reversible inhibitors with specificity for MAO-B, we have recently reported that, among a series of 10 3,4-dihydro-2(1H)-quinolinone derivatives, are high potency MAO-B inhibitors, with a number of homologues displaying good selectivities for MAO-B over the MAO-A isoform...
December 7, 2016: Drug Research
https://www.readbyqxmd.com/read/27909009/association-of-protein-distribution-and-gene-expression-revealed-by-pet-and-post-mortem-quantification-in-the-serotonergic-system-of-the-human-brain
#19
A Komorowski, G M James, C Philippe, G Gryglewski, A Bauer, M Hienert, M Spies, A Kautzky, T Vanicek, A Hahn, T Traub-Weidinger, D Winkler, W Wadsak, M Mitterhauser, M Hacker, S Kasper, R Lanzenberger
Regional differences in posttranscriptional mechanisms may influence in vivo protein densities. The association of positron emission tomography (PET) imaging data from 112 healthy controls and gene expression values from the Allen Human Brain Atlas, based on post-mortem brains, was investigated for key serotonergic proteins. PET binding values and gene expression intensities were correlated for the main inhibitory (5-HT1A) and excitatory (5-HT2A) serotonin receptor, the serotonin transporter (SERT) as well as monoamine oxidase-A (MAO-A), using Spearman's correlation coefficients (rs) in a voxel-wise and region-wise analysis...
November 30, 2016: Cerebral Cortex
https://www.readbyqxmd.com/read/27900600/antidepressant-like-effect-of-isorhynchophylline-in-mice
#20
Yan-Fang Xian, Ding Fan, Siu-Po Ip, Qing-Qiu Mao, Zhi-Xiu Lin
Isorhynchophylline (IRN), an oxindole alkaloid, has been identified as the main active ingredient responsible for the biological activities of Uncaria rhynchophylla (Miq) Miq ex Havil. (Rubiaceae). Previous studies in our laboratory have revealed that IRN possesses potent neuroprotective effects in different models of Alzheimer's disease. However, the antidepressant-like effects of IRN are remained unclear. The present study aims to evaluate the antidepressant-like effects of IRN. The antidepressant-like effects of IRN was determined by using animal models of depression including forced swimming and tail suspension tests...
November 30, 2016: Neurochemical Research
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