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Dopamine reuptake

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https://www.readbyqxmd.com/read/28734204/molecular-dynamics-of-conformation-specific-dopamine-transporter-inhibitor-complexes
#1
Bernandie Jean, Christopher K Surratt, Jeffry D Madura
The recreational psychostimulant cocaine inhibits dopamine reuptake from the synapse, resulting in excessive stimulation of postsynaptic dopamine receptors in brain areas associated with reward and addiction. Cocaine binds to and stabilizes the outward- (extracellular-) facing conformation of the dopamine transporter (DAT) protein, while the low abuse potential DAT inhibitor benztropine prefers the inward- (cytoplasmic-) facing conformation. A correlation has been previously postulated between psychostimulant abuse potential and preference for the outward-facing DAT conformation...
July 11, 2017: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/28731336/triple-reuptake-inhibitors-as-potential-therapeutics-for-depression-and-other-disorders-design-paradigm-and-developmental-challenges
#2
Murugaiah A M Subbaiah
Although first-line antidepressants offer therapeutic benefit, about 35% of depressed patients are not adequately treated, creating a large unmet medical need. These medicines mostly enhance the synaptic levels of serotonin and/or norepinephrine. Evidence from preclinical and clinical studies implicate dopamine hypofunction in the pathophysiology of depression. Triple reuptake inhibitors (TRIs), which elevate dopamine in addition to serotonin and norepinephrine, may demonstrate greater efficacy, with the reversal of anhedonia and improved tolerability...
July 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28720013/the-5-ht1b-serotonin-receptor-regulates-methylphenidate-induced-gene-expression-in-the-striatum-differential-effects-on-immediate-early-genes
#3
David Alter, Joel A Beverley, Ronak Patel, Carlos A Bolaños-Guzmán, Heinz Steiner
Drug combinations that include a psychostimulant such as methylphenidate (Ritalin) and a selective serotonin reuptake inhibitor such as fluoxetine are indicated in several medical conditions. Co-exposure to these drugs also occurs with "cognitive enhancer" use by individuals treated with selective serotonin reuptake inhibitors. Methylphenidate, a dopamine reuptake inhibitor, by itself produces some addiction-related gene regulation in the striatum. We have demonstrated that co-administration of selective serotonin reuptake inhibitors potentiates these methylphenidate-induced molecular effects, thus producing a more "cocaine-like" profile...
July 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28714693/stochastic-simulation-of-dopamine-neuromodulation-for-implementation-of-fluorescent-neurochemical-probes-in-the-striatal-extracellular-space
#4
Abraham Beyene, Ian McFarlane, Rebecca Pinals, Markita P Landry
Imaging the dynamic behavior of neuromodulatory neurotransmitters in the extracelluar space arising from individual quantal releases would constitute a major advance in neurochemical imaging. Spatial and temporal resolution of these highly stochastic neuromodulatory events requires concurrent advances in the chemical development of optical nanosensors selective for neuromodulators in concert with advances in imaging methodologies to capture millisecond neurotransmitter release. Herein, we develop and implement a stochastic model to describe dopamine dynamics in the extracellular space (ECS) of the brain dorsal striatum to guide the design and implementation of fluorescent neurochemical probes that record neurotransmitter dynamics in the ECS...
July 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28707591/new-generation-non-ssri-antidepressants-therapeutic-drug-monitoring-and-pharmacological-interactions-part-1-snris-smss-saris
#5
Roberto Mandrioli, Michele Protti, Laura Mercolini
BACKGROUND: New-generation antidepressants (NGAs) are the latest additions to the clinician's arsenal in the fight against depression. After the introduction of selective serotonin reuptake inhibitors (SSRIs), a plethora of other groups followed, identified by their main mechanisms of activity: serotonin and norepinephrine reuptake inhibitors (SNRI); serotonin modulators and stimulators (SMS); serotonin antagonists and reuptake inhibitors (SARI); noradrenergic and selective serotonergic antidepressants (NaSSA); norepinephrine reuptake inhibitors (NeRI); serotonin, norepinephrine and dopamine reuptake inhibitors (SNDRI) or triple reuptake inhibitors (TRI); and melatonin and serotonin agonists (MaSA)...
July 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28694090/milnacipran-affects-mouse-impulsive-aggressive-and-depressive-like-behaviors-in-a-distinct-dose-dependent-manner
#6
Iku Tsutsui-Kimura, Yu Ohmura, Takayuki Yoshida, Mitsuhiro Yoshioka
Serotonin/noradrenaline reuptake inhibitors (SNRIs) are widely used for the treatment for major depressive disorder, but these drugs induce several side effects including increased aggression and impulsivity, which are risk factors for substance abuse, criminal involvement, and suicide. To address this issue, milnacipran (0, 3, 10, or 30 mg/kg), an SNRI and antidepressant, was intraperitoneally administered to mice prior to the 3-choice serial reaction time task, resident-intruder test, and forced swimming test to measure impulsive, aggressive, and depressive-like behaviors, respectively...
June 27, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28655626/differential-effects-of-perinatal-exposure-to-antidepressants-on-learning-and-memory-acoustic-startle-anxiety-and-open-field-activity-in-sprague-dawley-rats
#7
Jenna L N Sprowles, Jillian R Hufgard, Arnold Gutierrez, Rebecca A Bailey, Sarah A Jablonski, Michael T Williams, Charles V Vorhees
Most antidepressants inhibit monoamine reuptake. Selective serotonin (5-HT) reuptake inhibitors (SSRIs) act on the 5-HT transporter (SERT) whereas norepinephrine-dopamine reuptake inhibitors (NDRIs) act on the norepinephrine and dopamine transporters. Epidemiological reports link SSRI use during pregnancy to an increased prevalence of autism spectrum disorder (ASD). We previously showed that perinatal exposure to the SSRI citalopram (CIT) results in rodent offspring that exhibit a number of behaviors consistent with an ASD-like phenotype...
June 24, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28655495/tranylcypromine-in-mind-part-i-review-of-pharmacology
#8
REVIEW
Sven Ulrich, Roland Ricken, Mazda Adli
It has been over 50 years since a review has focused exclusively on the monoamine oxidase (MAO) inhibitor tranylcypromine (TCP). A new review has therefore been conducted for TCP in two parts which are written to be read preferably in close conjunction: Part I - pharmacodynamics, pharmacokinetics, drug interactions, toxicology; and Part II - clinical studies with meta-analysis of controlled studies in depression, practice of TCP treatment, place in therapy. Pharmacological data of this review part I characterize TCP as an irreversible and nonselective MAO-A/B inhibitor at low therapeutic doses of 20mg/day with supplementary norepinephrine reuptake inhibition at higher doses of 40-60mg/day...
June 24, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28644892/r-modafinil-exerts-weak-effects-on-spatial-memory-acquisition-and-dentate-gyrus-synaptic-plasticity
#9
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
#10
Ahmed M Hussein, Yogesh D Aher, Predrag Kalaba, Nilima Y Aher, Vladimir Dragačević, Bojana Radoman, Marija Ilić, 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
#11
Alicia J Avelar, Jianjing 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 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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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...
July 2017: CNS Drugs
https://www.readbyqxmd.com/read/28571709/phospho-specific-antibodies-targeting-the-amino-terminus-of-the-human-dopamine-transporter
#18
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
#19
REVIEW
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
#20
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
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