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https://www.readbyqxmd.com/read/29159774/pharmacokinetics-pharmacodynamics-and-safety-of-rasagiline-transdermal-patch-a-preliminary-study-in-healthy-chinese-subjects
#1
Wenjia Zhou, Chengzhe Lv, Quanying Zhang, Shunlin Zong, Meng Wang
BACKGROUND AND OBJECTIVES: Rasagiline tablet is an oral MAO-B inhibitor applied in early or advanced Parkinson's disease (PD). However, when patients with PD cannot take their usual oral medications, a rasagiline transdermal patch can be used as a way to offer continuous rasagiline while avoiding plasma concentration peaks and troughs. The objectives of this study were to investigate the pharmacokinetics, pharmacodynamics, and safety of the rasagiline transdermal patch in healthy Chinese subjects...
November 20, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29140741/comparative-in-vitro-study-of-11-c-methionine-and-11-c-deuterodeprenyl-uptake-in-three-human-glioma-cell-lines
#2
Elena Vasilskis, Ingrid Kreimerman, Silvia Olivera, Eduardo Savio, Henry Engler
AIM: To compare the uptake of (11)C-deuterodeprenyl ((11)C-DED) and (11)C-methionine ((11)C-MET) in three human glioma cell lines and study the relationship with glial fibrillary acid protein (GFAP) and monoamine oxidase B (MAO B) expression. (11)C-DED is used in positron emission tomography imaging as a marker of astrocytosis in various central nervous system pathologies. It binds irreversibly to MAO B, a glial dimeric enzyme with increased activity in some neurological pathologies. MATERIALS AND METHODS: Binding and internalization studies of (11)C-MET and (11)C-DED were performed in astrocytoma grade III, glioblastoma grade IV, and radio-resistant glioblastoma grade IV cells...
November 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29138643/interactions-of-desmethoxyyangonin-a-secondary-metabolite-from-renealmia-alpinia-with-human-monoamine-oxidase-a-and-oxidase-b
#3
Narayan D Chaurasiya, Francisco León, Yuanqing Ding, Isabel Gómez-Betancur, Dora Benjumea, Larry A Walker, Stephen J Cutler, Babu L Tekwani
Renealmia alpinia (Zingiberaceae), a medicinal plant of tropical rainforests, is used to treat snakebites and other injuries and also as a febrifuge, analgesic, antiemetic, antiulcer, and anticonvulsant. The dichloromethane extract of R. alpinia leaves showed potent inhibition of human monoamine oxidases- (MAOs-) A and B. Phytochemical studies yielded six known compounds, including pinostrobin 1, 4'-methyl ether sakuranetin 2, sakuranetin 3, pinostrobin chalcone 4, yashabushidiol A 5, and desmethoxyyangonin 6...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29130466/-safinamide-from-daily-clinical-practice-first-clinical-steps
#4
J Pagonabarraga, J Kulisevsky
INTRODUCTION: The management of motor complications in Parkinson's disease (PD) is still limited. Safinamide, a new drug that has MAO-B inhibition and antiglutamatergic effects through inhibition of sodium channels, has shown efficacy for the treatment of fluctuations at doses of 50-100 mg/day. PATIENTS AND METHODS: From daily clinical practice, we describe the efficacy and tolerability of safinamide at three months in PD patients with motor complications. Efficacy was assessed by the Clinical Global Impression of Change scale and change in 'off' time during the daytime...
November 16, 2017: Revista de Neurologia
https://www.readbyqxmd.com/read/29128806/emotional-disorders-induced-by-hemopressin-and-rvd-hemopressin-%C3%AE-administration-in-rats
#5
Sheila Leone, Lucia Recinella, Annalisa Chiavaroli, Sara Martinotti, Claudio Ferrante, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Szabolcs Dvorácskó, Csaba Tömböly, Luciano De Petrocellis, Michele Vacca, Luigi Brunetti, Giustino Orlando
BACKGROUND: The endocannabinoid (eCB) system plays an important role in regulating emotional disorders, and is involved, directly or indirectly, in psychiatric diseases, such as anxiety and depression. Hemopressin, a hemoglobin α chain-derived peptide, and RVD-hemopressin(α), a N-terminally extended form of hemopressin, act as antagonist/inverse agonist and negative allosteric modulator of the cannabinoid 1 (CB1) receptor, respectively. METHODS: Considering the possible involvement of these peptides on emotional behaviour, the aim of our study was to investigate the behavioural effects of a single intraperitoneal (ip) injection of hemopressin (0...
June 23, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29127552/mao-b-inhibitors-do-not-block-in-vivo-flortaucipir-18-f-av-1451-binding
#6
Allan K Hansen, David J Brooks, Per Borghammer
PURPOSE: Recent evidence suggests that the tau radiotracer [(18)F]THK-5351 displays high affinity for the monoamine oxidase type B (MAO-B) enzyme. Utilizing another tau-tracer, flortaucipir ([(18)F]AV-1451), we previously reported that non-demented Parkinson's disease patients show off-target binding in subcortical structures, but no appreciable cortical uptake. However, 59 % of these patients were receiving MAO-B inhibitors at the time of their scan. Here, we retrospectively investigated if MAO-B inhibitors in clinical doses affect flortaucipir binding...
November 10, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/29126727/design-synthesis-and-biochemical-evaluation-of-novel-multi-target-inhibitors-as-potential-anti-parkinson-agents
#7
Simone Carradori, Francesco Ortuso, Anél Petzer, Donatella Bagetta, Celeste De Monte, Daniela Secci, Daniela De Vita, Paolo Guglielmi, Gokhan Zengin, Abdurrahman Aktumsek, Stefano Alcaro, Jacobus P Petzer
New 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of neurodegenerative disorders such as Parkinson's disease. Rational molecular design, target recognition and predicted pharmacokinetic properties have been evaluated by means of molecular modelling. Based on these properties, compounds were synthesized and evaluated in vitro as MAO-B and AChE inhibitors, and compared to the activities at their corresponding isozymes, monoamine oxidase A (MAO-A) and butyrylcholinesterase (BuChE), respectively...
October 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29126721/synthesis-monoamine-oxidase-inhibition-activity-and-molecular-docking-studies-of-novel-4-hydroxy-n-benzylidene-or-1-phenylethylidene-2-h-methyl-benzyl-1-2-benzothiazine-3-carbohydrazide-1-1-dioxides
#8
Furqan Ahmad Saddique, Sumera Zaib, Saquib Jalil, Sana Aslam, Matloob Ahmad, Sadia Sultan, Humera Naz, Mazhar Iqbal, Jamshed Iqbal
Three series of 4-hydroxy-N(')-[benzylidene/1-phenylethylidene]-2-H/methyl/benzyl-1,2-benzothiazine-3-carbohydrazide 1,1-dioxides (9-11)a-l were synthesized and unraveled to be highly potent dual inhibitors of monoamine oxidases (MAO-A and MAO-B). All the examined compounds demonstrated IC50 values in lower micro-molar range for both MAO-A as well as MAO-B. The most active MAO-A inhibitor was 4-hydroxy-N'-(1-phenylethylidene)-2H-benzo[e][1,2]thiazine-3-carbohydrazide 1,1-dioxide (9i) with an IC50 value of 0...
October 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29114238/long-term-monitoring-gait-analysis-using-a-wearable-device-in-daily-lives-of-patients-with-parkinson-s-disease-the-efficacy-of-selegiline-hydrochloride-for-gait-disturbance
#9
Mutsumi Iijima, Hiroshi Mitoma, Shinichiro Uchiyama, Kazuo Kitagawa
Objective: The aim of this study was to assess quantitatively the gait disorders in the daily lives of patients with Parkinson's disease (PD) using with a newly developed portable gait rhythmogram (PGR), which has a trunk-mounted acceleration sensor and automatic gait-detection algorithm. Methods: Using the PGR, we recorded the daily walking profiles of 14 PD patients before and after the addition or increase in dose of an MAO-B inhibitor (selegiline, average dose: 4...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/29098902/design-synthesis-and-pharmacological-evaluation-of-2-amino-5-nitrothiazole-derived-semicarbazones-as-dual-inhibitors-of-monoamine-oxidase-and-cholinesterase-effect-of-the-size-of-aryl-binding-site
#10
Rati K P Tripathi, Vishnu M Sasi, Sukesh K Gupta, Sairam Krishnamurthy, Senthil R Ayyannan
A series of 2-amino-5-nitrothiazole derived semicarbazones were designed, synthesised and investigated for MAO and ChE inhibition properties. Most of the compounds showed preferential inhibition towards MAO-B. Compound 4, (1-(1-(4-Bromophenyl)ethylidene)-4-(5-nitrothiazol-2-yl)semicarbazide) emerged as lead candidate (IC50 = 0.212 µM, SI = 331.04) against MAO-B; whereas compounds 21 1-(5-Bromo-2-oxoindolin-3-ylidene)-4-(5-nitrothiazol-2-yl)semicarbazide (IC50 = 0.264 µM) and 17 1-((4-Chlorophenyl) (phenyl)methylene)-4-(5-nitrothiazol-2-yl)semicarbazide (IC50 = 0...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29093288/synthesis-of-amide-and-ester-derivatives-of-cinnamic-acid-and-its-analogs-evaluation-of-their-free-radical-scavenging-and-monoamine-oxidase-and-cholinesterase-inhibitory-activities
#11
Koichi Takao, Kazuhiro Toda, Takayuki Saito, Yoshiaki Sugita
A series of cinnamic acid derivatives, amides (1-12) and esters (13-22), were synthesized, and structure-activity relationships for antioxidant activity, and monoamine oxidases (MAO) A and B, acetylcholinesterase, and butyrylcholinesterase (BChE) inhibitory activities were analyzed. Among the synthesized compounds, compounds 1-10, 12-18, and rosmarinic acid (23), which contained catechol, o-methoxyphenol or 5-hydroxyindole moieties, showed potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29065322/sulfonyl-hydrazones-derived-from-3-formylchromone-as-non-selective-inhibitors-of-mao-a-and-mao-b-synthesis-molecular-modelling-and-in-silico-adme-evaluation
#12
Syed Mobasher Ali Abid, Hafiza Amna Younus, Mariya Al-Rashida, Zunaira Arshad, Tooba Maryum, Mazhar Amjad Gilani, Abdulrahman I Alharthi, Jamshed Iqbal
A series of sulfonyl hydrazones derived from 3-formylchromone was synthesized and discovered to be effective, non-selective inhibitors of monoamine oxidases (MAO-A and MAO-B). The compounds are easily (synthetically) accessible in high yields, by simple condensation of 4-methylbenzenesulfonohydrazide with different (un)substituted 3-formylchromones. All compounds had IC50 values in lower micro-molar range (IC50 = 0.33-7.14 μM for MAO-A, and 1.12-3.56 μM for MAO-B). The most active MAO-B inhibitor was N'-[(E)-(6-fluoro-4-oxo-4H-chromen-3-yl)methylidene]-4-methylbenzenesulfonohydrazide (3e) with IC50 value of 1...
October 4, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29050969/a-novel-selective-mao-b-inhibitor-with-neuroprotective-and-anti-parkinsonian-properties
#13
Hugh H Chan, Man Kit Tse, Saravana Kumar, Lang Zhuo
We previously reported that 1,3-bisbenzylimidazolium (DBZIM) bromide was neuroprotective for the dopaminergic system in Parkinson's disease (PD) models of rodent, however the underlying mechanism was unclear. We currently further confirmed that DBZIM ameliorated the Parkinsonian motor deficit and protected the nigrostriatal tract from the neurotoxicity of 1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine (2'-CH3-MPTP) in C57Bl/6 mice. The dopaminergic degeneration in the substantia nigra par compacta (SNc) and striatum was analyzed by immunohistochemistry while the monoamine oxidase B (MAO-B) inhibition effect of DBZIM was determined by enzyme kinetics...
October 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29044007/depressive-symptoms-monoamines-levels-mao-b-activity-and-effect-of-treatment-in-a-subset-of-depressed-individuals-from-government-sector-hospital-at-karachi
#14
Farah Zeb, Sabira Naqvi, Razaur Rahman, Ahsana Dar Farooq
Depression is one of the leading causes of disability in developing countries including Pakistan. This study was designed to assess the frequency and severity of depressive symptoms, monoamines and their metabolite levels, MAO-B activities before and after treatment with antidepressants in a sub-set of Karachi population in Pakistan. Drug naive depressed subjects were evaluated before and after treatment with selective serotonin reuptake inhibitors. Symptoms of depressed mood and anxiety psychic (90%) were more frequent whereas, suicidal thoughts (~50%) and feelings of guilt (~30%) were less common...
July 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29033233/design-synthesis-and-biological-evaluation-of-2-acetyl-5-o-amino-alkyl-phenol-derivatives-as-multifunctional-agents-for-the-treatment-of-alzheimer-s-disease
#15
Zhipei Sang, Keren Wang, Huifang Wang, Huijuan Wang, Qianwen Ma, Xue Han, Mengyao Ye, Lintao Yu, Wenmin Liu
A series of 2-acetyl-5-O-(amino-alkyl)phenol derivatives was designed, synthesized and evaluated as multi-function inhibitors for the treatment of Alzheimer's disease (AD). The results revealed that compound TM-3 indicated selective AChE inhibitory potency (eeAChE, IC50 = 0.69 μM, selective index (SI) = 32.7). Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-3 could simultaneously bind to the catalytic active site and peripheral anionic site of AChE. And TM-3 was also a highly selective MAO-B inhibitor (IC50 = 6...
November 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29033232/design-synthesis-and-biological-evaluation-of-phthalimide-alkylamine-derivatives-as-balanced-multifunctional-cholinesterase-and-monoamine-oxidase-b-inhibitors-for-the-treatment-of-alzheimer-s-disease
#16
Zhipei Sang, Keren Wang, Huifang Wang, Lintao Yu, Huijuan Wang, Qianwen Ma, Mengyao Ye, Xue Han, Wenmin Liu
A series of novel phthalimide-alkylamine derivatives were synthesized and evaluated as multi-functions inhibitors for the treatment of Alzheimer's disease (AD). The results showed that compound TM-9 could be regarded as a balanced multi-targets active molecule. It exhibited potent and balanced inhibitory activities against ChE and MAO-B (huAChE, huBuChE, and huMAO-B with IC50 values of 1.2μM, 3.8μM and 2.6 μM, respectively) with low selectivity. Both kinetic analysis of AChE inhibition and molecular modeling study suggested that TM-9 binds simultaneously to the catalytic active site and peripheral anionic site of AChE...
November 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29031059/tying-up-tranylcypromine-novel-selective-histone-lysine-specific-demethylase-1-lsd1-inhibitors
#17
Yue-Yang Ji, Sen-Dong Lin, Yu-Jie Wang, Ming-Bo Su, Wei Zhang, Hendra Gunosewoyo, Fan Yang, Jia Li, Jie Tang, Yu-Bo Zhou, Li-Fang Yu
Aberrant expression of lysine specific histone demethylase 1 (LSD1) has been increasingly associated with numerous cancer cells and several proof-of-concept studies are strongly suggestive of its potential as a druggable target. Tranylcypromine (TCP) is an antidepressant originally known to target the monoamine oxidases A and B (MAO-A and MAO-B), which are structurally related to LSD1. A number of TCP derivatives have been identified as potent LSD1 inhibitors, with a handful of them currently being tested in clinical trials...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29027345/a-strategy-for-specific-fluorescence-imaging-of-monoamine-oxidase%C3%A2-a-in-living-cells
#18
Xiaofeng Wu, Wen Shi, Xiaohua Li, Huimin Ma
Monoamine oxidase (MAO) has two isoforms, MAO-A and MAO-B, which show different functions, and thus selective fluorescence imaging is important for biological studies. Currently, however, specific detection of MAO-A remains a great challenge. Herein, we report a new strategy for specific imaging of MAO-A through the design of fluorogenic probes combining the characteristic structure of an inhibitor of the target enzyme along with propylamine as a recognition moiety. The high specificity of our representative probe is demonstrated by imaging MAO-A in different live cells such as SH-SY5Y (high levels of MAO-A) and HepG2 (high levels of MAO-B), and further validated by western blot analyses...
October 12, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28952032/neuroprotective-strategies-to-prevent-and-treat-parkinson-s-disease-based-on-its-pathophysiological-mechanism
#19
REVIEW
Yujeong Lee, Min-Sun Kim, Jaewon Lee
Parkinson's disease (PD) is the second most common progressive neurodegenerative disease after Alzheimer's disease. PD exhibits clinical symptoms that include tremors, rigidity, and bradykinesia. Many drugs are available to treat PD, such as, L-dopa, COMT inhibitor, MAO-B inhibitor, and dopamine agonists, but these drugs simply compensate for dopamine loss in PD, and therefore, cannot completely suppress its symptoms or progression. Although the causes of PD are not clearly understood, common pathophysiological pathways, such as, oxidative stress, mitochondrial dysfunction, and neuroinflammation are considered to be etiological factors, and thus, many treatments and interventions have been developed to target these pathophysiological factors...
September 26, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28945218/tnf%C3%AE-yap-p65-hk2-axis-mediates-breast-cancer-cell-migration
#20
Y Gao, Y Yang, F Yuan, J Huang, W Xu, B Mao, Z Yuan, W Bi
Clinical and experimental evidence indicates that macrophages could promote solid-tumor progression and metastasis. However, the mechanisms underlying this process remain unclear. Here we show that yes-associated protein 1 (YAP1), a transcriptional regulator that controls tissue growth and regeneration, has an important role in tumor necrosis factor α (TNF α)-induced breast cancer migration. Mechanistically, macrophage conditioned medium (CM) or TNFα triggers IκB kinases (IKKs)-mediated YAP phosphorylation and activation in breast cancer cells...
September 25, 2017: Oncogenesis
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