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https://www.readbyqxmd.com/read/29216407/an-open-label-positron-emission-tomography-pet-study-to-evaluate-serotonin-transporter-occupancy-following-escalating-dosing-regimens-of-r-o-desmethylvenlafaxine-and-racemic-o-desmethylvenlafaxine
#1
W Gordon Frankle, Brigitte Robertson, Gary Maier, Jennifer Paris, Deanna Asmonga, Maureen May, Michael L Himes, N Scott Mason, Chester A Mathis, Rajesh Narendran
INTRODUCTION: SEP-227162 [R(-)-O-desmethylvenlafaxine] is an enantiomer of the venlafaxine metabolite O-desmethylvenlafaxine (ODV, Pristiq™, Wyeth). This study compared the serotonin transporter occupancy achieved by SEP-227162 and ODV, at daily doses of 25mg, 50mg, 100mg and 150mg using [11 C]DASB positron emission tomography (PET). METHODS: Sixteen healthy male subjects participated in one of four dose groups (N = 4 per group) during which they were administered two doses of the study drug (SEP-227162 or ODV)...
December 7, 2017: Synapse
https://www.readbyqxmd.com/read/29153425/fluoroethoxy-1-4-diphenethylpiperidine-and-piperazine-derivatives-potent-and-selective-inhibitors-of-3-h-dopamine-uptake-at-the-vesicular-monoamine-transporter-2
#2
Emily R Hankosky, Shyam R Joolakanti, Justin R Nickell, Venumadhav Janganati, Linda P Dwoskin, Peter A Crooks
A small library of fluoroethoxy-1,4-diphenethyl piperidine and fluoroethoxy-1,4-diphenethyl piperazine derivatives were designed, synthesized and evaluated for their ability to inhibit [(3)H]dopamine (DA) uptake at the vesicular monoamine transporter-2 (VMAT2) and dopamine transporter (DAT), [(3)H]serotonin (5-HT) uptake at the serotonin transporter (SERT), and [(3)H]dofetilide binding at the human-ether-a-go-go-related gene (hERG) channel. The majority of the compounds exhibited potent inhibition of [(3)H]DA uptake at VMAT2, Ki changes in the nanomolar range (Ki = 0...
October 20, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29145140/fluoxetine-modulates-the-transcription-of-genes-involved-in-serotonin-dopamine-and-adrenergic-signalling-in-zebrafish-embryos
#3
V Cunha, P Rodrigues, M M Santos, P Moradas-Ferreira, M Ferreira
Neurotransmitters pathways in fish and mammals are phylogenetically conserved. Therefore, the environmental presence of psychopharmaceuticals, such as fluoxetine (FLU), are likely to interact with fish serotonergic, dopaminergic and adrenergic systems, affecting their response and associated biological functions. Hence, the present work aimed at evaluating the effects of FLU in the transcription of genes involved in serotonin, dopamine and adrenergic transporters and receptors signalling in early stages of Danio rerio development...
January 2018: Chemosphere
https://www.readbyqxmd.com/read/29091968/computational-and-biological-evidences-on-the-serotonergic-involvement-of-setacn-antidepressant-like-effect-in-mice
#4
Mariana G Fronza, Lucimar M Pinto Brod, Angela Maria Casaril, Manoela Sacramento, Diego Alves, Lucielli Savegnago
A series of phenylselanyl-1H-1,2,3-triazole-4-carbonitriles with different substituents were screened for their binding affinity with serotonin transporter (SERT) and dopamine transporter (DAT) by docking molecular. 5-(4methoxyphenyl)-1-(2-(phenylselanyl)phenyl)-1H-1,2,3-triazole-4-carbonitrile (SeTACN) exhibited the best conformation with SERT even higher than fluoxetine and serotonin, suggesting a competitive inhibition. SeTACN demonstrated additional affinity to other serotonergic receptors involved in antidepressant effects: 5HT1a, 5HT2a and 5HT3...
2017: PloS One
https://www.readbyqxmd.com/read/29081351/integrating-biological-treatment-mechanisms-into-randomized-clinical-trials-design-of-progress-prolonged-exposure-and-sertraline-trial
#5
Sheila A M Rauch, Naomi M Simon, H Myra Kim, Ron Acierno, Anthony P King, Sonya B Norman, Margaret R Venners, Katherine Porter, K Luan Phan, Peter W Tuerk, Carolyn Allard, Israel Liberzon, Barbara O Rothbaum, Brian Martis, Murray B Stein, Charles W Hoge
Increased emphasis on mechanisms of treatment effectiveness, biomarker predictors, and objective indicators of treatment response has sparked interest in integrated, translational treatment outcomes trials. The PROlonGed ExpoSure and Sertraline Trial (PROGrESS) is one such randomized controlled trial (RCT) focused on a key question in clinical management of posttraumatic stress disorder (PTSD) - the comparative and combined effectiveness of medication and psychotherapy. PROGrESS employs a state of the art trial design to examine psychotherapy and medication effects across three conditions: 1) Prolonged Exposure (PE) plus pill placebo, 2) Sertraline (SERT) plus Enhanced Medication Management (EMM), and 3) Combined treatment (PE/SERT)...
October 29, 2017: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/29032583/third-generation-ventricular-assist-device-mid-term-outcomes-of-the-heartware-hvad-in-pediatric-patients
#6
Mustafa Pac, Sinan Sabit Kocabeyoglu, Umit Kervan, Dogan Emre Sert, Serhat Koca, Ibrahim Ece, Feyza Aysenur Pac
The HeartWare HVAD is a small, third generation continuous flow pump that is intracorporeally placed for support of a failing ventricle in adult patients. This device is small in size when compared to other left ventricular assist devices and can therefore be used in smaller sized pediatric patients. We present our initial experience using the HVAD as a bridge to heart transplantation in the pediatric population. We performed a retrospective, single center, nonrandomized review of 17 pediatric patients who underwent HVAD implantation between June 2013 and March 2016...
October 15, 2017: Artificial Organs
https://www.readbyqxmd.com/read/29030421/serotonin-transporter-gene-polymorphisms-may-be-associated-with-poststroke-neurological-recovery-after-escitalopram-use
#7
Eun-Jae Lee, Mi-Sun Oh, Jong S Kim, Dae-Il Chang, Jong-Ho Park, Jae-Kwan Cha, Ji Hoe Heo, Sung-Il Sohn, Dong-Eog Kim, Hahn Young Kim, Jei Kim, Woo-Keun Seo, Jun Lee, Sang-Won Park, Yun Joong Kim, Byung-Chul Lee
OBJECTIVE: Selective serotonin reuptake inhibitors (SSRIs) putatively improve neurological recovery after stroke. We aimed to investigate whether serotonin transporter (SERT) gene polymorphisms are related to the responsiveness to SSRIs in the poststroke neurological recovery. METHODS: This was a post hoc analysis of the EMOTION study (ClinicalTrials.gov NCT01278498), a randomised, placebo-controlled, double-blind trial examining the efficacy of escitalopram on emotional and neurological disturbances after acute stroke...
October 13, 2017: Journal of Neurology, Neurosurgery, and Psychiatry
https://www.readbyqxmd.com/read/28935840/test-retest-reliability-of-the-sert-imaging-agent-11-c-homadam-in-healthy-humans
#8
Vikram Adhikarla, Boadie W Dunlop, Nachwa Jarkas, Mark Goodman, Helen Mayberg, Michael J Owens, Jonathon A Nye
The aim of this study was to measure the test-retest reliability of (11)C-N,N-dimethyl-2-(2'-amino-4'-hydroxymethylphenylthio)benzylamine ([(11)C]HOMADAM) imaging of serotonin transporter (SERT) density in healthy control subjects. Methods: Two female and two male volunteers participated in the study and underwent three [(11)C]HOMADAM Positron Emission Tomography (PET) scans each of 90 min in duration. Time-activity curves were derived from SERT rich structures and fit to two models: 1) a simplified reference tissue model (SRTM) and 2) a multi-linear graphical model (MRTM)...
September 21, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28861307/preliminary-feasibility-study-of-a-new-method-of-hypothermia-in-an-experimental-canine-model
#9
İbrahim Ünal Sert, Murat Akand, Özcan Kılıç, Nuri Yavru, Ersan Bulut
OBJECTIVE: To build up a new microcontroller thermoelectric system to achieve renal hypothermia. MATERIAL AND METHODS: Renal hypothermia system was tested under in vivo conditions in the kidneys of ten Mongrel dogs. Ambient temperature was evaluated using two different microcontrollers. In order to ensure hypothermia in the renal parenchyma, selection can be made among 4 modules and sensors which detect the temperature of the area. The temperature range of the system was adjusted between -50°C and +50°C...
September 2017: Turkish Journal of Urology
https://www.readbyqxmd.com/read/28815595/sigma-1-receptor-ligands-inhibit-catecholamine-secretion-from-adrenal-chromaffin-cells-due-to-block-of-nicotinic-acetylcholine-receptors
#10
Rebecca L Brindley, Mary Beth Bauer, Nolan D Hartley, Kyle J Horning, Kevin P M Currie
Adrenal chromaffin cells (ACCs) are the neuroendocrine arm of the sympathetic nervous system and key mediators of the physiological stress response. Acetylcholine (ACh) released from preganglionic splanchnic nerves activates nicotinic acetylcholine receptors (nAChRs) on chromaffin cells causing membrane depolarization, opening voltage-gated Ca(2+) channels (VGCC), and exocytosis of catecholamines and neuropeptides. The serotonin transporter is expressed in ACCs and interacts with 5-HT1A receptors to control secretion...
October 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28796292/exposure-to-low-environmental-concentrations-of-manganese-lead-and-cadmium-alters-the-serotonin-system-of-blue-mussels
#11
Marc Fraser, Marlène Fortier, Delphine Foucher, Pierre-Hervé Roumier, Pauline Brousseau, Michel Fournier, Céline Surette, Cathy Vaillancourt
Serotonin plays a crucial role in mussel survival and reproduction. Although the serotonin system can be affected by metals, the effects of environmental concentrations of metals such as manganese (Mn), lead (Pd), and cadmium (Cd) have never been studied in blue mussels. The present study aimed to determine the effects of exposure to Mn, Pb, or Cd on serotonin levels, monoamine oxidase (MAO) activity, and serotonin transporter (SERT) levels in the blue mussel Mytilus edulis. Mussels were exposed in vivo to increasing and environmentally relevant doses of Mn (10-1000 nM; 0...
August 10, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28795234/demographic-and-clinical-characteristics-of-patients-with-serum-sickness-like-reaction
#12
Alaaddin Yorulmaz, Fatih Akın, Ahmet Sert, Mehmet Akif Ağır, Rıza Yılmaz, Şükrü Arslan
In this study, we aimed to review the demographic, clinical, and laboratory characteristics of patients who were followed up and treated with the diagnosis of serum sickness-like reactions (SSLR) in our pediatric rheumatology clinic retrospectively and emphasize the importance of early diagnosis and treatment. The files of 29 patients who were hospitalized in the pediatric rheumatology clinic between September 2016 and March 2017 with the diagnosis of type 3 hypersensitivity reaction were reviewed retrospectively...
August 9, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28790887/mir-16-and-fluoxetine-both-reverse-autophagic-and-apoptotic-change-in-chronic-unpredictable-mild-stress-model-rats
#13
Yang Yang, Zhiying Hu, Xiaoxue Du, Henry Davies, Xue Huo, Marong Fang
In the clinic selective serotonin reuptake inhibitors (SSRIs), like Fluoxetine, remain the primary treatment for major depression. It has been suggested that miR-16 regulates serotonin transporters (SERT) via raphe nuclei and hippocampal responses to antidepressants. However, the underlying mechanism and regulatory pathways are still obtuse. Here, a chronic unpredicted mild stress (CUMS) depression model in rats was established, and then raphe nuclei miR-16 and intragastric Fluoxetine injections were administered for a duration of 3 weeks...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28774871/enteric-serotonin-and-oxytocin-endogenous-regulation-of-severity-in-a-murine-model-of-necrotizing-enterocolitis
#14
Kara Gross Margolis, Jennifer Vittorio, Maria Talavera, Karen Gluck, Zhishan Li, Alina Iuga, Korey Stevanovic, Virginia Saurman, Narek Israelyan, Martha G Welch, Michael D Gershon
Necrotizing enterocolitis (NEC), a gastrointestinal inflammatory disease of unknown etiology, causes a great deal of morbidity and mortality in premature infants. The liver as well as the gut may be affected in NEC. We tested the hypothesis that signaling molecules, which are endogenous to the bowel, regulate the severity of experimental NEC in mice. Specifically, we postulated that mucosal serotonin (5-HT), which is proinflammatory, would increase the severity of NEC and that oxytocin (OT), which is present in enteric neurons and is anti-inflammatory, would oppose NEC...
August 3, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28763213/novel-3-1-2-3-6-tetrahydropyridin-4-yl-1h-indole-based-multifunctional-ligands-with-antipsychotic-like-mood-modulating-and-procognitive-activity
#15
Adam Bucki, Monika Marcinkowska, Joanna Śniecikowska, Krzysztof Więckowski, Maciej Pawłowski, Monika Głuch-Lutwin, Anna Gryboś, Agata Siwek, Karolina Pytka, Magdalena Jastrzębska-Więsek, Anna Partyka, Anna Wesołowska, Paweł Mierzejewski, Marcin Kołaczkowski
The most troublesome aspects of behavioral and psychological symptoms of dementia (BPSD) are nowadays addressed by antidepressant, anxiolytic, and antipsychotic drugs, often administered off-label. Considering their modest effectiveness in dementia patients, the increased risk of adverse events and cognitive decline, there is an unmet need for well-tolerated and effective therapy of BPSD. We designed and synthesized multifunctional ligands characterized in vitro as high-affinity partial agonists of D2R, antagonists of 5-HT6R, and blockers of SERT...
September 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28673772/methyl-4-phenylpyridinium-mpp-differentially-affects-monoamine-release-and-re-uptake-in-murine-embryonic-stem-cell-derived-dopaminergic-and-serotonergic-neurons
#16
Yasmina Martí, Friederike Matthaeus, Thorsten Lau, Patrick Schloss
1-Methyl-4-phenyl-1,2,5,6-tetrahydropyridine (MPTP) is known to selectively damage dopaminergic (DA) cells in the substantia nigra and to produce symptoms which are alike to those observed in Parkinson's disease (PD). Based on the similarity between MPTP-induced neurotoxicity and PD-related neuropathology, application of MPTP or its metabolite methyl-4-phenylpyridinium (MPP+) was successfully established in experimental rodent models to study PD-related neurodegenerative events. MPP+ is taken up by the dopamine transporter (DAT) into DA neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain...
June 30, 2017: Molecular and Cellular Neurosciences
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
#17
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...
October 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28644875/estimation-of-the-optimal-dosing-regimen-of-escitalopram-in-dogs-a-dose-occupancy-study-with-11c-dasb
#18
Olivia Taylor, Nick Van Laeken, Ingeborgh Polis, Robrecht Dockx, Lise Vlerick, Andre Dobbeleir, Ingeborg Goethals, Jimmy Saunders, Nele Sadones, Chris Baeken, Filip De Vos, Kathelijne Peremans
Although the favourable characteristics of escitalopram as being the most selective serotonin reuptake inhibitor and having an increased therapeutic efficacy via binding on an additional allosteric binding site of the serotonin transporter, its dosing regimen has not yet been optimized for its use in dogs. This study aimed to estimate the optimal dosing frequency and the required dose for achieving 80% occupancy of the serotonin transporters in the basal ganglia. The dosing frequency was investigated by determining the elimination half-life after a four day oral pre-treatment period with 0...
2017: PloS One
https://www.readbyqxmd.com/read/28611606/long-term-sertraline-intake-reverses-the-behavioral-changes-induced-by-prenatal-stress-in-rats-in-a-sex-dependent-way
#19
Inês Pereira-Figueiredo, Orlando Castellano, Adelaida S Riolobos, Graça Ferreira-Dias, Dolores E López, Consuelo Sancho
Early life stress is a major factor underlying the vulnerability to respond to stressful events later in life. The present study attempted to evaluate the role of prenatal stress affecting the development of stress-related disorders and their reversion by postnatal exposure to Sertraline (SERT), a front-line medication for medication for posttraumatic stress disorder (PTSD) in humans. To achieve this, adult male and female prenatally stressed (PS) or unstressed (Controls) offspring rats, following oral chronic treatment with SERT (5 mg/kg/day; from 1 month to 4 months old), or not, were studied prior to and after a traumatic event...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28594090/design-and-synthesis-of-1-2-4-triazolo-3-2-b-1-3-5-thiadiazine-derivatives-as-a-novel-template-for-analgesic-anti-inflammatory-activity
#20
Seyma Sert-Ozgur, Banu C Tel, Elif I Somuncuoglu, Inci Kazkayasi, Mevlut Ertan, Birsen Tozkoparan
Previously, we demonstrated that certain heterocyclic compounds derived from 3-substituted-1,2,4-triazole-5-thiones had promising analgesic/anti-inflammatory activities together with low ulcerogenic properties. Therefore, we sought to design and synthesize new derivatives of triazol-5-thiones-fused heterocycles. In the present study, a series of novel bis-Mannich bases, namely 2,6-disubstituted-6,7-dihydro-5H-1,2,4-triazolo[3,2-b]-1,3,5-thiadiazines (1a-d, 2a-c, and 3a-d), were synthesized and characterized to assess their possible anti-inflammatory/analgesic properties...
June 8, 2017: Archiv der Pharmazie
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