keyword
MENU ▼
Read by QxMD icon Read
search

Selegiline

keyword
https://www.readbyqxmd.com/read/29309800/partial-reversal-of-the-effort-related-motivational-effects-of-tetrabenazine-with-the-mao-b-inhibitor-deprenyl-selegiline-implications-for-treating-motivational-dysfunctions
#1
Hector Contreras-Mora, Megan A Rowland, Samantha E Yohn, Merce Correa, John D Salamone
People with depression and Parkinsonism frequently show effort-related motivational symptoms, such as anergia, psychomotor retardation, and fatigue. Tasks that assess effort-related choice are being used as animal models of these motivational symptoms. The present studies characterized the ability of monoamine oxidase (MAO) inhibitors with varying selectivity profiles to reverse the low effort bias induced by the monoamine storage inhibitor tetrabenazine. Tetrabenazine produces depressive symptoms in humans, and because of its selective inhibition of VMAT-2, it preferentially depletes DA at low doses...
January 5, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29279995/type-a-and-b-monoamine-oxidases-distinctly-modulate-signal-transduction-pathway-and-gene-expression-to-regulate-brain-function-and-survival-of-neurons
#2
REVIEW
Makoto Naoi, Wakako Maruyama, Masayo Shamoto-Nagai
Type A and B monoamine oxidases (MAO-A, -B) mediate and modulate intracellular signal pathways for survival or death of neuronal cells. MAO-A is associated with development of neuronal architecture, synaptic activity, and onset of psychiatric disorders, including depression, and antisocial aggressive impulsive behaviors. MAO-B produces hydrogen peroxide and plays a vital role in neuronal loss of neurodegenerative disorders, such as Parkinson's and Alzheimer's diseases. This review presents a novel role of MAO-A and B, their substrates and inhibitors, and hydrogen peroxide in brain function and neuronal survival and death...
December 26, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29250969/-the-role-of-selective-monoamine-oxidase-b-inhibitors-in-the-therapeutic-strategy-of-parkinson-s-disease-in-the-neurology-clinics-of-tirgu-mures-county-emergency-clinical-hospital
#3
József Attila Szász, Viorelia Constantin, Péter Alpár Fazakas, Eszter Blényesi, Levente Gábor Grieb, Antal Balla, Mónika Sárig, Kinga Szegedi, Eszter Noémi Bartha, Szabolcs Szatmári
INTRODUCTION: Selective monoamine oxidase B inhibitors have an accurate place in therapeutical strategy of Parkinsons's disease. In the early stages of the disease, especially in younger patients with milder symptoms, the introduction of levodopa substitution could be efficacious in delaying; in advanced stages they are mainly used to treat motor complications, as an adjunct to levodopa. AIM: The evaluation of therapeutical strategies used in the neurology clinics of Tirgu Mures County Emergency Clinical Hospital in order to define the role of monoamine oxidase B inhibitors...
December 2017: Orvosi Hetilap
https://www.readbyqxmd.com/read/29221756/characterization-of-the-binding-site-for-d-deprenyl-in-human-inflamed-synovial-membrane
#4
Anna Lesniak, Mikko Aarnio, Shanti Diwakarla, Thomas Norberg, Fred Nyberg, Torsten Gordh
AIMS: d-Deprenyl when used as a positron emission tomography tracer visualizes peripheral inflammation. The major aim of the current study was to identify and investigate the properties of the binding target for d-deprenyl in synovial membrane explants from arthritic patients. MAIN METHODS: Thirty patients diagnosed with arthritis or osteoarthritis were enrolled into the study. Homologous and competitive radioligand binding assays utilizing [3H]d-deprenyl were performed to investigate the biochemical characteristics of the binding site and assess differences in the binding profile in synovial membranes exhibiting varying levels of inflammation...
December 5, 2017: Life Sciences
https://www.readbyqxmd.com/read/29198609/synthesis-and-evaluation-of-biaryl-derivatives-for-structural-characterization-of-selective-monoamine-oxidase-b-inhibitors-toward-parkinson-s-disease-therapy
#5
Seul Ki Yeon, Ji Won Choi, Jong-Hyun Park, Ye Rim Lee, Hyeon Jeong Kim, Su Jeong Shin, Bo Ko Jang, Siwon Kim, Yong-Sun Bahn, Gyoonhee Han, Yong Sup Lee, Ae Nim Pae, Ki Duk Park
Benzyloxyphenyl moiety is a common structure of highly potent, selective and reversible inhibitors of monoamine oxidase B (MAO-B), safinamide and sembragiline. We synthesized 4-(benzyloxy)phenyl and biphenyl-4-yl derivatives including halogen substituents on the terminal aryl unit. In addition, we modified the carbon linker between amine group and the biaryl linked unit. Among synthesized compounds, 12c exhibited the most potent and selective MAO-B inhibitory effect (hMAO-B IC50: 8.9 nM; >10,000-fold selectivity over MAO-A) as a competitive inhibitor...
November 24, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29175589/design-synthesis-monoamine-oxidase-inhibition-and-docking-studies-of-new-dithiocarbamate-derivatives-bearing-benzylamine-moiety
#6
Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Yusuf Özkay, Beril İnci, Zafer Asım Kaplancıklı
A new series of thirteen 2-[(4-fluorophenyl)(4-nitrobenzyl)amino]-2-oxoethyl-1-substituted-carbodithioate derivatives (4a-4m) were synthesized and tested for their human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitory potential by an in vitro fluorometric method. Most of the compounds have found to be selective towards MAO-B than MAO-A. Compound 4j that carrying 4-nitrophenyl piperazine moiety, was detected as the most active agent amongst all compounds with the IC50 value of 0.097 ± 0.003 µM for MAO-B while that of selegiline was 0...
November 20, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29133700/wearing-off-a-complex-phenomenon-often-poorly-recognized-in-parkinson-s-disease-a-study-with-the-woq-19-questionnaire
#7
Michele Pistacchi, Manuela Gioulis, Flavio Sanson, Sandro Z Marsala
BACKGROUND: 'Wearing off' refers to the phenomenology of movement disorders in Parkinson's disease (PD) that appears early and is much commoner than generally believed. It may be present in the form of either motor symptoms or non-motor symptoms. AIM: To investigate the utility of wearing-off questionnaire (WOQ-19, Italian version) in the outpatient clinical practice to assess the suitability of different combinations of treatment, in various stages of PD. METHODS: 73 consecutive patients (58% male and 42% female) suffering from PD were recruited through the Santorso Hospital and San Martino Hospital from September 2012 to March 2014...
November 2017: Neurology India
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
#8
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/29054367/monoamine-oxidase-b-inhibitor-protects-degenerating-spinal-neurons-enhances-nerve-regeneration-and-functional-recovery-in-sciatic-nerve-crush-injury-model
#9
Al-Shimali M Hussain, Waleed M Renno, Hanaa L Sadek, Noura M Kayali, Aseel Al-Salem, Muddanna S Rao, Khalid M Khan
Monoamine oxidase-B (MAOB), a flavin adenine dinucleotide (FAD), is an enzyme which catalyzes the oxidation of amines. MAOB is proposed to play a major role in the pathogenesis of neurodegeneration through the production of reactive oxygen species (ROS) and neurotoxins. The present study was designed to outline the effects of the MAOB inhibitor (MAOB-I) on neuroprotection of spinal neurons, regeneration of sciatic nerve fibers, and recovery of sensory-motor functions in the sciatic nerve crush injury model...
October 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29050969/a-novel-selective-mao-b-inhibitor-with-neuroprotective-and-anti-parkinsonian-properties
#10
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/29033831/accumulation-of-123-i-ioflupane-is-a-useful-marker-of-the-efficacy-of-selegiline-monotherapy-in-drug-na%C3%A3-ve-parkinson-s-disease
#11
Hidetomo Murakami, Tetsuhito Nohara, Masanobu Uchiyama, Yoshiyuki Owan, Akinori Futamura, Azusa Shiromaru, Setsuro Tsukada, Yu Saito, Takeshi Kuroda, Satoshi Yano, Seiichiro Ishigaki, Hirotaka Katoh, Jiro Munechika, Yoshimitsu Ohgiya, Takehiko Gokan, Kenjiro Ono
Background: Selegiline enhances the patient's endogenous dopamine by inhibiting dopamine metabolism. The efficacy of selegiline monotherapy for drug-naïve Parkinson's disease (PD) patients may depend on the degree of dopaminergic neuronal degeneration. (123)I-Ioflupane single photon emission computed tomography (SPECT) and (123)I-meta-iodobenzylguanidine (MIBG) myocardial scintigraphy are diagnostic methods to assess the pharmacological and pathological changes in PD. Objective: We examined the utility of these imaging methods to predict the efficacy of selegiline monotherapy for motor symptoms in drug-naïve PD patients...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/28875405/appraisal-of-transdermal-water-in-oil-nanoemulgel-of-selegiline-hcl-for-the-effective-management-of-parkinson-s-disease-pharmacodynamic-pharmacokinetic-and-biochemical-investigations
#12
Sonal Setya, Tushar Madaan, Mohammad Tariq, B K Razdan, Sushama Talegaonkar
In the present study, the potential of transdermal nanoemulsion gel of selegiline hydrochloride for the treatment of Parkinson's disease was investigated. Water-in-oil nanoemulsions were developed by comparing low- and high-energy methods and were subjected to thermodynamic stability tests, in vitro permeation, and characterization studies. In vitro studies indicated that components of nanoemulsion acted as permeation enhancers with highest flux of 3.531 ± 1.94 μg/cm(2)/h from nanoemulsion SB6 containing 0...
September 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28857772/a-randomized-double-blind-placebo-controlled-phase-iii-trial-of-selegiline-monotherapy-for-early-parkinson-disease
#13
Yoshikuni Mizuno, Nobutaka Hattori, Tomoyoshi Kondo, Masahiro Nomoto, Hideki Origasa, Ryosuke Takahashi, Mitsutoshi Yamamoto, Nobuo Yanagisawa
BACKGROUND: In Japan, selegiline has been approved for combination therapy with levodopa for Parkinson disease (PD). We conducted a trial of selegiline monotherapy for early PD. METHODS: In this 12-week controlled phase III trial, a total of 292 subjects were randomized to receive placebo (n = 146) (full analysis set 140) or selegiline (n = 146) (full analysis set 139). The primary outcome measure was the change in the Unified Parkinson Disease Rating Scale part I + II + III total score from baseline to the final visit...
September 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28840582/n-acetylcysteine-prevents-the-increase-in-spontaneous-oxidation-of-dopamine-during-monoamine-oxidase-inhibition-in-pc12-cells
#14
David S Goldstein, Yunden Jinsmaa, Patti Sullivan, Yehonatan Sharabi
The catecholaldehyde hypothesis for the pathogenesis of Parkinson's disease proposes that the deaminated dopamine metabolite 3,4-dihydroxyphenylacetaldehyde (DOPAL) is toxic to nigrostriatal dopaminergic neurons. Inhibiting monoamine oxidase (MAO) should therefore slow the disease progression; however, MAO inhibition increases spontaneous oxidation of dopamine, as indicated by increased 5-S-cysteinyl-dopamine (Cys-DA) levels, and the oxidation products may also be toxic. This study examined whether N-acetylcysteine (NAC), a precursor of the anti-oxidant glutathione, attenuates the increase in Cys-DA production during MAO inhibition...
November 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28831499/erratum-to-efficacy-of-rasagiline-and-selegiline-in-parkinson-s-disease-a-head-to-head-3-year-retrospective-case-control-study
#15
Emanuele Cereda, Roberto Cilia, Margherita Canesi, Silvana Tesei, Claudio Bruno Mariani, Anna Lena Zecchinelli, Gianni Pezzoli
No abstract text is available yet for this article.
September 2017: Journal of Neurology
https://www.readbyqxmd.com/read/28774283/effectiveness-of-spinal-cord-stimulation-for-painful-camptocormia-with-pisa-syndrome-in-parkinson-s-disease-a-case-report
#16
Hisanao Akiyama, Saki Nukui, Masashi Akamatu, Yasuhiro Hasegawa, Osamu Nishikido, Soichiro Inoue
BACKGROUND: Spinal cord stimulation (SCS) has recently been reported to be effective for truncal postural abnormalities such as camptocormia and Pisa syndrome in Parkinson's disease. In this case report, we describe a case of a woman with Parkinson's disease in whom SCS was effective for painful camptocormia with Pisa syndrome. CASE PRESENTATION: A 65-year-old woman was admitted to our hospital because of painful camptocormia. She had noticed resting tremor in the left upper limb and aprosody at 48 years of age...
August 3, 2017: BMC Neurology
https://www.readbyqxmd.com/read/28738644/biosensor-for-the-characterisation-of-hmao-b-inhibitors-and-the-quantification-of-selegiline
#17
Maximilian Aigner, Patricia Preissegger, Kurt Kalcher, Eda Mehmeti, Peter Macheroux, Dale Edmondson, Astrid Ortner
A novel human monoamine oxidase B (hMAO B) based biosensor for inhibitory measurements was developed. It allows both the characterisation of the type of enzyme inhibition and the sensitive and simple determination of inhibitors like selegiline hydrochloride. The sensor consists of a screen printed carbon working electrode modified with 20% manganese dioxide (MnO2) and the enzyme hMAO B, which was immobilised on the electrode via a dialysis membrane (regenerated cellulose, molecular weight cut-off 14000). Inhibition of hMAO B is evaluated by adding different concentrations of the inhibitor selegiline hydrochloride to the enzyme and applying a defined amount of the hMAO B substrate phenylethylamine (PEA)...
November 1, 2017: Talanta
https://www.readbyqxmd.com/read/28737446/quantitative-in-vitro-phenotyping-and-prediction-of-drug-interaction-potential-of-cyp2b6-substrates-as-victims
#18
Raghava Choudary Palacharla, Ramakrishna Nirogi, Venkatesham Uthukam, Arunkumar Manoharan, Ranjith Kumar Ponnamaneni, Ilayaraja Kalaikadhiban
1. Determination of fm, CYP for a compound is critical to assess the potential risk of a drug candidate as a victim of DDI. Several compounds are identified as CYP2B6 substrates but the fm, CYP2B6 values are not determined quantitatively 2. Two methods of reaction phenotyping, the chemical inhibition method, and metabolism in rCYP enzymes, were used to determine the relative contributions of the enzymes. Chemical inhibition method was also conducted in the presence of BSA (0.5% w/v) 3. The results confirm with the earlier studies concerning the identity of the CYP2B6 enzyme...
July 24, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28682134/brain-targeted-delivery-of-mucoadhesive-thermosensitive-nasal-gel-of-selegiline-hydrochloride-for-treatment-of-parkinson-s-disease
#19
Vinay Sridhar, Sarika Wairkar, Ram Gaud, Amrita Bajaj, Pramod Meshram
Selegiline hydrochloride (SL), is an Anti-Parkinson's agent, has low oral bioavailability due to its high first pass metabolism and scarce oral absorption. In the present study, SL mucoadhesive nasal thermosensitive gel (SNT-gel) was prepared to enhance the bioavailability and subsequently, its concentration in the brain. The SNT-gel was prepared using Poloxamer 407-Chitosan combination and optimized formulation was further evaluated for physicochemical parameters. The comparative pharmacodynamic studies including behavioral studies, biochemical testing and histopathology of the brain was carried out in rats for SNT-gel, SL-nasal solution and SL Marketed Tablets...
July 6, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28649132/reassessment-of-subacute-mptp-treated-mice-as-animal-model-of-parkinson-s-disease
#20
Qiu-Shuang Zhang, Yang Heng, Zheng Mou, Ju-Yang Huang, Yu-He Yuan, Nai-Hong Chen
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model remains the most commonly used animal model of Parkinson's disease (PD). There are three MPTP-treatment schemes: acute, subacute and chronic. Considering the advantages of the period and similarity to PD, the subacute model was often chosen to assess the validity of new candidates, but the changes caused by the subacute MPTP treatment and the appropriate positive control for this model remain to be further confirmed. The aim of this study was: to estimate the value of the subacute MPTP mouse model in aspects of behavioral performance, biochemical changes and pathological abnormalities, and to find effective positive drugs...
October 2017: Acta Pharmacologica Sinica
keyword
keyword
12445
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"