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https://www.readbyqxmd.com/read/28110399/safinamide-a-review-in-parkinson-s-disease
#1
Hannah A Blair, Sohita Dhillon
Safinamide (Xadago(®)) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. In the EU, safinamide is approved for the treatment of mid- to late-stage fluctuating Parkinson's disease (PD) as add-on therapy to a stable dose of levodopa alone or in combination with other PD medications. Safinamide 50-100 mg/day administered as a fixed or flexible dose significantly increased daily 'on' time without dyskinesia (primary endpoint) in patients with mid- to late-stage PD with motor fluctuations in 24-week, placebo-controlled clinical trials...
January 21, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28109809/potent-inhibition-of-monoamine-oxidase-a-by-decursin-from-angelica-gigas-nakai-and-by-wogonin-from-scutellaria-baicalensis-georgi
#2
Hyun Woo Lee, Hyung Won Ryu, Myung-Gyun Kang, Daeui Park, Hanna Lee, Heung Mook Shin, Sei-Ryang Oh, Hoon Kim
During the ongoing search for new monoamine oxidase (MAO) inhibitors, five coumarin derivatives and eight flavonoids were isolated from the roots of Angelica gigas Nakai and Scutellaria baicalensis Georgi, respectively. Of the phytochemicals, decursin (4) was found to potently and selectively inhibit human MAO-A (IC50=1.89μM). The IC50 value of 4 for MAO-A belonged to the lowest group in herbal sources and was similar to that of toloxatone (1.78μM), a marketed drug. Wogonin (11) effectively inhibited MAO-A and MAO-B (IC50=6...
January 18, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28108387/inhibition-of-monoamine-oxidase-b-by-selegiline-reduces-cigarette-smoke-induced-oxidative-stress-and-inflammation-in-airway-epithelial-cells
#3
Yuting Cui, Kenneth W K Liu, Yingmin Liang, Mary S M Ip, Judith C W Mak
Chronic obstructive pulmonary disease (COPD) is caused by the build-up of oxidative stress-induced damages due to cigarette smoking, but how monoamine oxidase (MAO)-B signaling is involved remains unclear. This study aims to establish the involvement of MAO-B signaling pathways in cigarette smoke medium (CSM)-induced oxidative stress and inflammation in human airway epithelial cells (AECs). CSM treatment increased MAO-B activity, ROS levels and IL-8 release in AECs. Pretreatment with MAO-B selective inhibitor selegiline reversed the CSM-induced changes in MAO-B activity, ROS levels and IL-8 release in a dose-dependent manner...
January 17, 2017: Toxicology Letters
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
#4
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/28104804/the-n-terminus-specifies-the-switch-between-transport-modes-of-the-human-serotonin-transporter
#5
Carina Kern, Fatma Asli Erdem, Ali El-Kasaby, Walter Sandtner, Michael Freissmuth, Sonja Sucic
The serotonin transporter (SERT) and other monoamine transporters operate in either a forward transport mode, where the transporter undergoes a full transport cycle, or an exchange mode, where the transporter seesaws through half-cycles. Amphetamines trigger the exchange-mode leading to substrate efflux. This efflux was proposed to rely on the N-terminus, which was suggested to adopt different conformations in the inward-, outward-facing and amphetamine-bound states. This prediction was verified by tryptic digestion of SERT-expressing membranes: in the absence of Na+, the N-terminus was rapidly digested...
January 19, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28103426/analytical-characterization-and-pharmacological-evaluation-of-the-new-psychoactive-substance-4-fluoromethylphenidate-4%C3%A2-f-mph-and-differentiation-between-the-%C3%A2-threo-and-%C3%A2-erythro-diastereomers
#6
Gavin McLaughlin, Noreen Morris, Pierce V Kavanagh, John D Power, Geraldine Dowling, Brendan Twamley, John O'Brien, Gary Hessman, Brian Murphy, Donna Walther, John S Partilla, Michael H Baumann, Simon D Brandt
Misuse of (±)-threo-methylphenidate (methyl-2-phenyl-2-(piperidin-2-yl)acetate; Ritalin®, MPH) has long been acknowledged, but the appearance of MPH analogs in the form of 'research chemicals' has only emerged in more recent years. 4-Fluoromethylphenidate (4 F-MPH) is one of these recent examples and this study presents the identification and analytical characterization of two powdered 4 F-MPH products that were obtained from an online vendor in 2015. Interestingly, the products appeared to have originated from two distinct batches given that one product consisted of (±)-threo-4 F-MPH isomers whereas the second sample consisted of a mixture of (±)-threo and (±)-erythro 4 F-MPH...
January 19, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28101368/polymorphisms-in-the-canine-monoamine-oxidase-a-maoa-gene-identification-and-variation-among-five-broad-dog-breed-groups
#7
James Sacco, Andrew Ruplin, Paul Skonieczny, Michael Ohman
BACKGROUND: In humans, reduced activity of the enzyme monoamine oxidase type A (MAOA) due to genetic polymorphisms within the MAOA gene leads to increased brain neurotransmitter levels associated with aggression. In order to study MAOA genetic diversity in dogs, we designed a preliminary study whose objectives were to identify novel alleles in functionally important regions of the canine MAOA gene, and to investigate whether the frequencies of these polymorphisms varied between five broad breed groups (ancient, herding, mastiff, modern European, and mountain)...
2017: Canine Genetics and Epidemiology
https://www.readbyqxmd.com/read/28097890/novel-1-2-pyrimidin-2-yl-piperazine-derivatives-as-selective-monoamine-oxidase-mao-a-inhibitors
#8
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
#9
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/28095073/preclinical-and-potential-applications-of-common-western-herbal-supplements-as-complementary-treatment-in-parkinson-s-disease
#10
Luke A Morgan, Oliver Grundmann
Parkinson's disease (PD) is a neurological disorder with a complex pathological etiology, which is not fully understood. Progression of PD may be the result of a buildup of iron in the substantia nigra, microglia-mediated neuroinflammation, dysfunctional mitochondria, or abnormal protein handling. Dopamine is the main neurotransmitter affected, but as the disease progresses, a decrease in all the brain's biogenic amines occurs. Current medication used in the treatment of PD aims to prevent the breakdown of dopamine or increase dopaminergic neurotransmission in the central nervous system...
January 17, 2017: Journal of Dietary Supplements
https://www.readbyqxmd.com/read/28094812/putative-presynaptic-dopamine-dysregulation-in-schizophrenia-is-supported-by-molecular-evidence-from-post-mortem-human-midbrain
#11
T D Purves-Tyson, S J Owens, D A Rothmond, G M Halliday, K L Double, J Stevens, T McCrossin, C Shannon Weickert
The dopamine hypothesis of schizophrenia posits that increased subcortical dopamine underpins psychosis. In vivo imaging studies indicate an increased presynaptic dopamine synthesis capacity in striatal terminals and cell bodies in the midbrain in schizophrenia; however, measures of the dopamine-synthesising enzyme, tyrosine hydroxylase (TH), have not identified consistent changes. We hypothesise that dopamine dysregulation in schizophrenia could result from changes in expression of dopamine synthesis enzymes, receptors, transporters or catabolic enzymes...
January 17, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28093976/chemoinformatics-profiling-of-the-chromone-nucleus-as-a-mao-b-a2aar-dual-binding-scaffold
#12
Maykel Cruz-Monteagudo, Fernanda Borges, M Natália D S Cordeiroc, Aliuska Morales Helguerad, Eduardo Tejerab, Cesar Paz-Y-Miñob, Aminael Sánchez-Rodrígueze, Yunier Perera-Sardiñaf, Yunierkis Perez-Castillo
BACKGROUND: In the context of the current drug discovery efforts to find disease modifying therapies for Parkinson´s disease (PD) the current single target strategy has proved inefficient. Consequently, the search for multi-potent agents is attracting more and more attention due to the multiple pathogenetic factors implicated in PD. Multiple evidences points to the dual inhibition of the monoamine oxidase B (MAO-B), as well as adenosine A2A receptor (A2AAR) blockade, as a promising approach to prevent the neurodegeneration involved in PD...
January 16, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28090585/circadian-forced-desynchrony-of-the-master-clock-leads-to-phenotypic-manifestation-of-depression-in-rats
#13
Miriam Ben-Hamo, Tracy A Larson, Leanne S Duge, Carl Sikkema, Charles W Wilkinson, Horacio O de la Iglesia, Mónica M C González
In mammals, a master circadian clock within the suprachiasmatic nucleus (SCN) of the hypothalamus maintains the phase coherence among a wide array of behavioral and physiological circadian rhythms. Affective disorders are typically associated with disruption of this fine-tuned "internal synchronization," but whether this internal misalignment is part of the physiopathology of mood disorders is not clear. To date, depressive-like behavior in animal models has been induced by methods that fail to specifically target the SCN regulation of internal synchronization as the mode to generate depression...
November 2016: ENeuro
https://www.readbyqxmd.com/read/28089688/functional-identification-of-plasma-membrane-monoamine-transporter-pmat-slc29a4-as-an-atenolol-transporter-sensitive-to-flavonoids-contained-in-apple-juice
#14
Yoshihisa Mimura, Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Hiroaki Yuasa
The intestinal absorption of atenolol has recently been reported to be reduced by simultaneous ingestion of fruit juices, such as apple juice. This finding implies a possibility that an unidentified carrier-mediated transport system, which could be interfered by some components of those juices, might be involved in atenolol absorption. In an attempt to explore that possibility, we successfully identified plasma membrane monoamine transporter (PMAT/SLC29A4) as a transporter that can operate for cellular atenolol uptake in the intestine, using Madin-Darby canine kidney II cells stably expressing PMAT...
January 12, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28080034/the-mechanism-of-the-flavoprotein-6-hydroxy-l-nicotine-oxidase-ph-and-solvent-isotope-effects-and-identification-of-key-active-site-residues
#15
Paul F Fitzpatrick, Fatemeh Chadegani, Shengnan Zhang, Vi Dougherty
The flavoenzyme L-6-hydroxynicotine oxidase (LHNO) is a member of the monoamine oxidase family that catalyzes the oxidation of (S)-6-hydroxynicotine to 6-hydroxypseudooxynicotine during microbial catabolism of nicotine. While the enzyme has long been understood to catalyze oxidation of carbon-carbon bond, it has recently been shown to catalyze oxidation of a carbon-nitrogen bond (Fitzpatrick et al., Biochemistry 55, 697-703). The effects of pH and mutagenesis of active site residues have now been utilized to study the mechanism and the roles of active site residues...
January 12, 2017: Biochemistry
https://www.readbyqxmd.com/read/28078250/effects-of-mimosa-pudica-l-leaves-extract-on-anxiety-depression-and-memory
#16
Ganesh Patro, Subrat Kumar Bhattamisra, Bijay Kumar Mohanty
OBJECTIVE: The present study was carried out to investigate the neuropharmacological activities of ethyl acetate extract of Mimosa pudica (EAMP) leaves on anxiety, depression and memory in a mouse model. MATERIALS AND METHODS: Anti-anxiety potential of EAMP was evaluated by elevated plus maze (EPM), light-dark box (LDB) and social interaction (SI) tests in mice.Anti-depressant potential of EAMP was evaluated by forced swimming (FST), tail suspension (TST), and open field tests (OFT)...
November 2016: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28069864/hydralazine-is-involved-in-tele-methylhistamine-metabolism-by-inhibiting-monoamine-oxidase-b-in-pregnancy-associated-hypertensive-mice
#17
Shohei Kawasaki, Koichiro Kako, Yusuke Nagashima, Akihiko Kanou, Junji Ishida, Akiyoshi Fukamizu
Hypertensive disorders of pregnancy globally affect 6-8% of gestation and remain a major cause of both foetal and maternal morbidity and mortality. However, the antihypertensive medications for the patients of this disease are strictly limited due to the teratogenic potentials. Here, we found that tele-methylhistamine (tMH) increased in response to the administration of hydralazine (Hdz), a vasodilative agent, in the pregnancy-associated hypertensive (PAH) mice. Hdz abrogated the degradation of tMH catalyzed by monoamine oxidase B (MAO-B) in vitro These results suggested that Hdz inhibited the MAO-B activity and consequently tMH increased in the maternal circulation of PAH mice...
January 7, 2017: Journal of Biochemistry
https://www.readbyqxmd.com/read/28069535/thyronamines-and-analogues-translational-research-on-thyronergic-amines-the-route-from-rediscovery-of-thyronamines-to-the-bedside
#18
Grazia Chiellini, Lorenza Bellusci, Martina Sabatini, Riccardo Zucchi
Thyronamines are a novel class of endogenous signaling compounds, structurally related to thyroid hormones (THs). Specific thyronamines, particularly 3-iodothyronamine (T1AM), stimulate with nanomolar affinity trace amine-associated receptor 1 (TAAR1), a G protein-coupled membrane receptor, and may also interact with other TAAR subtypes (particularly TAAR5), adrenergic receptors (particularly α2 receptors), amine transporters, and mitochondrial proteins. In addition to its structural similarities with THs, T1AM also contains the arylethylamine scaffold as in monoamine neurotransmitters, implicating an intriguing role for T1AM as both a neuromodulator and a hormone-like molecule constituting a part of thyroid hormone signaling...
January 6, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28069007/the-benzopyrone-biochanin-a-as-a-reversible-competitive-and-selective-monoamine-oxidase-b-inhibitor
#19
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
#20
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
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