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Dopamine reuptake

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https://www.readbyqxmd.com/read/28644892/r-modafinil-exerts-weak-effects-on-spatial-memory-acquisition-and-dentate-gyrus-synaptic-plasticity
#1
Bharanidharan Shanmugasundaram, Yogesh D Aher, Jana Aradska, Marija Ilic, Daniel Daba Feyissa, Predrag Kalaba, Nilima Y Aher, Vladimir Dragacevic, Babak Saber Marouf, Thierry Langer, Harald H Sitte, Harald Hoeger, Gert Lubec, Volker Korz
Modafinil is a wake promoting drug approved for clinical use and also has cognitive enhancing properties. Its enantiomer R-Modafinil (R-MO) is not well studied in regard to cognitive enhancing properties. Hence we studied its effect in a spatial memory paradigm and its possible effects on dentate gyrus long-term potentiation (DG-LTP). Clinically relevant doses of R-MO, vehicle dimethyl sulfoxide (DMSO) or saline were administered for three days during the hole-board test and in in vivo DG-LTP. Synaptic levels of dopamine receptors D1R, D2R, dopamine transporter (DAT), and its phosphorylated form (ph-DAT) in DG tissue 4 h after LTP induction were quantified by western blot analysis...
2017: PloS One
https://www.readbyqxmd.com/read/28629964/a-novel-heterocyclic-compound-improves-working-memory-in-the-radial-arm-maze-and-modulates-the-dopamine-receptor-d1r-in-frontal-cortex-of-the-sprague-dawley-rat
#2
Ahmed M Hussein, Yogesh D Aher, Predrag Kalaba, Nilima Y Aher, Vladimir Dragačević, Bojana Radoman, Marija Ilic, Johann Leban, Tetyana Beryozkina, Abdel Baset M A Ahmed, Ernst Urban, Thierry Langer, Gert Lubec
A series of compounds have been shown to enhance cognitive function via the dopaminergic system and indeed the search for more active and less toxic compounds is continuing. It was therefore the aim of the study to synthetise and test a novel heterocyclic compound for cognitive enhancement in a paradigm for working memory. Specific and effective dopamine re-uptake inhibition (DAT (IC50=4,1 ± 0,8μM) made us test this compound in a radial arm maze (RAM) in the rat. CE-125 (4-((benzhydrylsulfinyl)methyl)-2-cyclopropylthiazole), was tested for dopamine (DAT), serotonin and norepinephrine re-uptake inhibition by a well-established system...
June 16, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28625719/atypical-dopamine-transporter-inhibitors-r-modafinil-and-jhw-007-differentially-affect-d2-autoreceptor-neurotransmission-and-the-firing-rate-of-midbrain-dopamine-neurons
#3
Alicia J Avelar, J Cao, Amy Hauck Newman, Michael J Beckstead
Abuse of psychostimulants like cocaine that inhibit dopamine (DA) reuptake through the dopamine transporter (DAT) represents a major public health issue, however FDA-approved pharmacotherapies have yet to be developed. Recently a class of ligands termed "atypical DAT inhibitors" has gained attention due to their range of effectiveness in increasing extracellular dopamine (DA) levels without demonstrating significant abuse liability. These compounds not only hold promise as therapeutic agents to treat stimulant use disorders but also as experimental tools to improve our understanding of DAT function...
June 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28619473/cocaine-adulteration
#4
REVIEW
Oliver Kudlacek, Tina Hofmaier, Anton Luf, Felix P Mayer, Thomas Stockner, Constanze Nagy, Marion Holy, Michael Freissmuth, Rainer Schmid, Harald H Sitte
Cocaine is a naturally occurring and illicitly used psychostimulant drug, which exerts its activity at monoaminergic neurotransmitter transporters. These transporters mediate the reuptake of the monoamines dopamine, serotonin and norepinephrine and are blocked by cocaine. The increase of monoamines in the extracellular space is the phenomenon underlying the drug effects that cocaine users seek. Currently, it is one of the most important illicit drugs on the European market. However, this increase in monoamines is also the underlying cause for the development of addiction and a number of severe side effects...
June 12, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28605373/modeling-fast-scan-cyclic-voltammetry-data-from-electrically-stimulated-dopamine-neurotransmission-data-using-qnsim1-0
#5
Rashed Harun, Christine M Grassi, Miranda J Munoz, Amy K Wagner
Central dopaminergic (DAergic) pathways have an important role in a wide range of functions, such as attention, motivation, and movement. Dopamine (DA) is implicated in diseases and disorders including attention deficit hyperactivity disorder, Parkinson's disease, and traumatic brain injury. Thus, DA neurotransmission and the methods to study it are of intense scientific interest. In vivo fast-scan cyclic voltammetry (FSCV) is a method that allows for selectively monitoring DA concentration changes with fine temporal and spatial resolution...
June 5, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28596833/absorption-distribution-metabolism-and-excretion-of-14-c-dasotraline-in-humans
#6
Yu-Luan Chen, Estela Skende, Jing Lin, Yijun Yi, Peter L Wang, Sarah Wills, H Scott Wilkinson, Kenneth S Koblan, Seth C Hopkins
Dasotraline is a dopamine and norepinephrine reuptake inhibitor, and the early clinical trials show a slow absorption and long elimination half-life. To investigate the absorption, distribution, metabolism, and excretion of dasotraline in humans, a single dose of [(14)C]-dasotraline was administered to eight healthy male adult volunteers. At 35 days, 90.7% of the dosed radioactivity was recovered in the urine (68.3%) and feces (22.4%). The major metabolic pathways involved were: (1) amine oxidation to form oxime M41 and sequential sulfation to form M42 or glucuronidation to form M43; (2) N-hydroxylation and sequential glucuronidation to form M35; (3) oxidative deamination to form (S)-tetralone; (4) mono-oxidation of (S)-tetralone and sequential glucuronidation to form M31A and M32; and (5) N-acetylation to form (1R,4S)-acetamide M102...
February 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28582390/polymorphisms-in-dopaminergic-system-genes-association-with-criminal-behavior-and-self-reported-aggression-in-violent-prison-inmates-from-pakistan
#7
Muhammad Imran Qadeer, Ali Amar, J John Mann, Shahida Hasnain
Genetic factors contribute to antisocial and criminal behavior. Dopamine transporter DAT-1 (SLC6A3) and DRD2 gene for the dopamine-2 receptor are dopaminergic system genes that regulate dopamine reuptake and signaling, and may be part of the pathogenesis of psychiatric disorders including antisocial behaviors and traits. No previous studies have analyzed DAT-1 and DRD2 polymorphisms in convicted murderers, particularly from Indian subcontinent. In this study we investigated the association of 40 bp VNTR polymorphism of DAT-1 and Taq1 variant of DRD2 gene (rs1800479) with criminal behavior and self-reported aggression in 729 subjects, including 370 men in Pakistani prisons convicted of first degree murder(s) and 359 control men without any history of violence or criminal tendency...
2017: PloS One
https://www.readbyqxmd.com/read/28579325/a-peptide-disrupting-the-d2r-dat-interaction-protects-against-dopamine-neurotoxicity
#8
Ping Su, Fang Liu
Dopamine reuptake from extracellular space to cytosol leads to accumulation of dopamine, which triggers neurotoxicity in dopaminergic neurons. Previous studies have shown that both dopamine D2 receptor (D2R) and dopamine transporter (DAT) are involved in dopamine neurotoxicity. However, blockade of either D2R or DAT causes side effects due to antagonism of other physiological functions of these two proteins. We previously found that DAT can form a protein complex with D2R and its cell surface expression is facilitated via D2R-DAT interaction, which regulates dopamine reuptake and intracellular dopamine levels...
June 1, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28577135/a-review-of-adjunctive-cns-medications-used-for-the-treatment-of-post-surgical-pain
#9
REVIEW
Ajit Rai, Howard Meng, Aliza Weinrib, Marina Englesakis, Dinesh Kumbhare, Liza Grosman-Rimon, Joel Katz, Hance Clarke
Inadequate post-operative pain management can have significant impacts on patients' quality of life. Effective management of acute pain after surgery is important for early mobilization and discharge from hospital, patient satisfaction, and overall well-being. Utilizing multimodal analgesic strategies has become the mainstay of acute post-operative pain management. A comprehensive search was performed, assessing the published or otherwise publically available literature on different central nervous system (CNS) drugs [excluding opioids, non-steroidal anti-inflammatory drugs (NSAIDs), and acetaminophen] and their uses to treat acute post-surgical pain...
June 2, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28571709/phospho-specific-antibodies-targeting-the-amino-terminus-of-the-human-dopamine-transporter
#10
Caline S Karam, Namita Sen, Jonathan A Javitch
The dopamine transporter (DAT), which mediates the inactivation of released dopamine through its reuptake, is the primary molecular target for the actions of psychostimulants. An increasing number of studies support an essential role for phosphorylation of serines (Ser) in the distal amino (N) terminus of DAT in regulating its function. Still, the molecular details of the regulation of phosphorylation and its impact on function are not fully understood. To address this, we have developed and characterized two distinct phospho-antibodies that recognize human DAT when it is phosphorylated at Ser7 or Ser12...
May 30, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28562526/efficacy-of-antidepressive-medication-for-depression-in-parkinson-disease-a-network-meta-analysis
#11
Chuanjun Zhuo, Rong Xue, Lanlan Luo, Feng Ji, Hongjun Tian, Hongru Qu, Xiaodong Lin, Ronghuan Jiang, Ran Tao
BACKGROUND: Parkinson disease (PD) was considered as the 2nd most prevalent neurodegenerative disorder after Alzheimer disease, while depression is a prevailing nonmotor symptom of PD. Typically used antidepression medication includes tricyclic antidepressants (TCA), selective serotonin reuptake inhibitors (SSRI), serotonin and norepinephrine reuptake inhibitors (SNRI), monoamine-oxidase inhibitors (MAOI), and dopamine agonists (DA). Our study aimed at evaluating the efficacy of antidepressive medications for depression of PD...
June 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28522087/mazindol-a-risk-factor-for-pulmonary-arterial-hypertension
#12
Eric Konofal, Cherine Benzouid, Christophe Delclaux, Michel Lecendreux, Elizabeth Hussey
Mazindol is an imidazo-isoindole derivative, a tricyclic compound and a non-amphetamine central nervous system stimulant that blocks dopamine and norepinephrine reuptake. Mazindol was withdrawn from the US and European markets in 1999 for reasons unrelated to its efficacy or safety around a time when other anorexic drugs were found to be associated with the development of pulmonary arterial hypertension (PAH). Despite the use of mazindol for decades, reports of PAH due to mazindol intake have been extremely rare...
June 2017: Sleep Medicine
https://www.readbyqxmd.com/read/28494748/the-novelty-of-bupropion-as-a-dopaminergic-antidepressant-for-the-treatment-of-adult-attention-deficit-hyperactive-disorder
#13
Kanit Tha Deang, Hatta Sidi, Hazli Zakaria, Raja Lope Adam, Srijit Das, Nurul Hazwani Hatta, Muhammad Hatta, Kok Wei Wee
Attention deficit hyperactive disorder (ADHD), a hyperactivity disorder that is prevalent among children may continue as an adulthood attention deficit. To date, treating an individual with an adult ADHD may be an arduous task as it involved numerous challenges, such as a need for high index of suspicion to diagnose this medical condition. Many psychiatric disorders masquerade as ADHD and delayed the necessary assessment and proper treatment for the debilitating medical condition. Adult ADHD would also be misdiagnosed (or under diagnosed) due to the facts that this medical condition is being masked by his or her high level of intellectuality achievement...
May 11, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28492455/reevaluating-antidepressant-selection-in-patients-with-bruxism-and-temporomandibular-joint-disorder
#14
Royce Rajan, Ye-Ming Sun
Temporomandibular joint disorder (TMD) is a broad pain disorder that refers to several conditions affecting the temporomandibular joint of the jaw and the muscles of mastication. As with most pain disorders, a high prevalence of depression and anxiety is associated with TMD. Research has shown that selective serotonin reuptake inhibitors (SSRIs), the first-line drug therapy for major depressive disorder, may not be suitable for TMD patients because SSRIs can induce teeth-grinding, otherwise known as bruxism...
May 2017: Journal of Psychiatric Practice
https://www.readbyqxmd.com/read/28488009/linking-stress-catecholamine-autotoxicity-and-allostatic-load-with-neurodegenerative-diseases-a-focused-review-in-memory-of-richard-kvetnansky
#15
REVIEW
David S Goldstein, Irwin J Kopin
In this Focused Review, we provide an update about evolving concepts that may link chronic stress and catecholamine autotoxicity with neurodegenerative diseases such as Parkinson's disease. Richard Kvetnansky's contributions to the field of stress and catecholamine systems inspired some of the ideas presented here. We propose that coordination of catecholaminergic systems mediates adjustments maintaining health and that senescence-related disintegration of these systems leads to disorders of regulation and to neurodegenerative diseases such as Parkinson's disease...
May 9, 2017: Cellular and Molecular Neurobiology
https://www.readbyqxmd.com/read/28487792/ssri-facilitated-crack-dancing
#16
Ravi Doobay, Lili Sun, Amish Shah, Pardeep Masuta, Zachary Shepherd
Choreoathetoid movement secondary to cocaine use is a well-documented phenomenon better known as "crack dancing." It consists of uncontrolled writhing movements secondary to excess dopamine from cocaine use. We present a 32-year-old male who had been using cocaine for many years and was recently started on paroxetine, a selective serotonin reuptake inhibitor (SSRI) for worsening depression four weeks before presentation. He had been doing cocaine every 2 weeks for the last three years and had never "crack danced" before this episode...
2017: Case Reports in Neurological Medicine
https://www.readbyqxmd.com/read/28457819/mechanisms-underlying-alterations-in-norepinephrine-levels-in-the-locus-coeruleus-of-ovariectomized-rats-modulation-by-estradiol-valerate-and-black-cohosh
#17
Jing Zhang, Wenpei Bai, Wenjuan Wang, Hai Jiang, Biao Jin, Yao Liu, Shuya Liu, Ke Wang, Jing Jia, Lihua Qin
Hot flushes are common in menopause. Norepinephrine (NE), primarily synthesized in the locus coeruleus (LC), plays a major role in central thermoregulation. Furthermore, we previously observed decreased dopamine beta hydroxylase (DβH), a key enzyme in NE synthesis, in LC neurons following ovariectomy. In this study, we explore the mechanisms underlying decreased NE levels in the LC (LC-NE) in ovariectomized (OVX) rats, and the modulating effects of estradiol valerate (E2) and black cohosh (ICR). We used high-performance liquid chromatography to detect LC-NE in SHAM, OVX, OVX-E2, and OVX-ICR groups...
April 27, 2017: Neuroscience
https://www.readbyqxmd.com/read/28452866/effects-of-dopamine-and-norepinephrine-on-exercise-induced-oculomotor-fatigue
#18
Charlotte J W Connell, Benjamin Thompson, Jason Turuwhenua, Alexa Srzich, Nicholas Gant
INTRODUCTION: Fatigue-induced impairments in the control of eye movements are detectable via reduced eye movement velocity following a bout of prolonged, strenuous exercise. Slower eye movements caused by neural fatigue within the oculomotor system can be prevented by caffeine and upregulation of central catecholamines may be responsible for this effect. This study explored the individual contribution of dopamine and norepinephrine to fatigue-related impairments in oculomotor control...
April 28, 2017: Medicine and Science in Sports and Exercise
https://www.readbyqxmd.com/read/28445595/ventricular-fibrillation-cardiac-arrest-produces-a-chronic-striatal-hyperdopaminergic-state-that-is-worsened-by-methylphenidate-treatment
#19
Gerald J Nora, Rashed Harun, David F Fine, Daniel Hutchison, Adam C Grobart, Jason P Stezoski, Miranda Munoz, Patrick M Kochanek, Rehana K Leak, Tomas Drabek, Amy K Wagner
Cardiac arrest survival rates have improved with modern resuscitation techniques, but many survivors experience impairments associated with hypoxic-ischemic brain injury. Currently, little is understood about chronic changes in striatal dopamine (DA) systems after hypoxic-ischemic brain injury. Given the common empiric clinical use of DA enhancing agents in neurorehabilitation, investigation evaluating dopaminergic alterations after cardiac arrest (CA) is necessary to optimize rehabilitation approaches. We hypothesized that striatal DA neurotransmission would be altered chronically after ventricular fibrillation cardiac arrest (VF-CA)...
April 26, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28442937/simultaneous-administration-of-fluoxetine-and-simvastatin-ameliorates-lipid-profile-improves-brain-level-of-neurotransmitters-and-increases-bioavailability-of-simvastatin
#20
Abdulrahman K Al-Asmari, Zabih Ullah, Aqeel Salman Al Masoudi, Ishtiaque Ahmad
Simvastatin (STT), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, is widely prescribed for dyslipidemia, whereas fluoxetine (FLX) is the first-choice drug for the treatment of depression and anxiety. A recent report suggests that selective serotonin reuptake inhibitors can interact with the cytochrome P450 3A4 substrate, and another one suggests that STT enhances the antidepressant activity of FLX. However, the data are inconclusive. The present study was designed to explore the pharmacokinetic and pharmacodynamic consequences of coadministration of STT and FLX in experimental animals...
2017: Journal of Experimental Pharmacology
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