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https://www.readbyqxmd.com/read/28644875/estimation-of-the-optimal-dosing-regimen-of-escitalopram-in-dogs-a-dose-occupancy-study-with-11c-dasb
#1
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
#2
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
#3
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
https://www.readbyqxmd.com/read/28529483/identification-of-a-novel-allosteric-inhibitory-site-on-tryptophan-hydroxylase-1-enabling-unprecedented-selectivity-over-all-related-hydroxylases
#4
Mike Petrassi, Rob Barber, Celine Be, Sarah Beach, Brian Cox, Anne-Marie D'Souza, Nick Duggan, Martin Hussey, Roy Fox, Peter Hunt, Gabor Jarai, Takatoshi Kosaka, Paul Oakley, Viral Patel, Neil Press, David Rowlands, Clemens Scheufler, Oliver Schmidt, Honnappa Srinivas, Mary Turner, Rob Turner, John Westwick, Alison Wolfreys, Nuzhat Pathan, Simon Watson, Matthew Thomas
Pulmonary arterial hypertension (PAH) has demonstrated multi-serotonin receptor dependent pathologies, characterized by increased tone (5-HT1B receptor) and complex lesions (SERT, 5-HT1B, 5-HT2B receptors) of the pulmonary vasculature together with right ventricular hypertrophy, ischemia and fibrosis (5-HT2B receptor). Selective inhibitors of individual signaling elements - SERT, 5-HT2A, 5HT2B, and combined 5-HT2A/B receptors, have all been tested clinically and failed. Thus, inhibition of tryptophan hydroxylase 1 (TPH1), the rate limiting step in 5-HT synthesis, has been suggested as a more broad, and thereby more effective, mode of 5-HT inhibition...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28508340/comparative-effects-of-sertraline-haloperidol-or-olanzapine-treatments-on-ketamine-induced-changes-in-mouse-behaviours
#5
O J Onaolapo, T B Paul, A Y Onaolapo
Effects of sertraline, haloperidol or olanzapine administration on ketamine-induced behaviours in mice were examined. The aim was to ascertain the degree of reversal of such behaviours by sertraline, and compare its effectiveness to haloperidol and olanzapine. Ten-week old mice (N = 120) were equally divided into main groups; 1 (open-field, radial-arm maze and elevated plus maze {EPM} tests), and 2 (social interaction test). Mice in each main group were assigned into six groups of ten (n = 10) each. Group 1 received intraperitoneal (i...
May 15, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28491024/the-serotonin-transporter-and-early-life-stress-translational-perspectives
#6
REVIEW
Danielle J Houwing, Bauke Buwalda, Eddy A van der Zee, Sietse F de Boer, Jocelien D A Olivier
The interaction between the serotonin transporter (SERT) linked polymorphic region (5-HTTLPR) and adverse early life stressing (ELS) events is associated with enhanced stress susceptibility and risk to develop mental disorders like major depression, anxiety, and aggressiveness. In particular, human short allele carriers are at increased risk. This 5-HTTLPR polymorphism is absent in the rodent SERT gene, but heterozygous SERT knockout rodents (SERT(+/-)) show several similarities to the human S-allele carrier, therefore creating an animal model of the human situation...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28467588/the-effect-of-2-different-surgical-methods-on-intracompartmental-pressure-value-in-tibial-shaft-fracture-an-experimental-study-in-a-rabbit-model
#7
Cemil Ertürk, Mehmet Akif Altay, Nuray Altay, İbrahim Avşin Öztürk, İslam Baykara, Cemil Sert, Uğur Erdem Işıkan
BACKGROUND: Intracompartmental pressure (ICP) monitoring is a widely used modality, particularly after intramedullary nailing of tibial shaft fractures. It was hypothesized that ICP value in fracture fixed with Ilizarov circular fixator (ICF) might be lower than in fracture fixed with intramedullary pin (IMP). The present study is a comparison of ICP value in tibial fractures in a rabbit model fixed with ICF and IMP. METHODS: Twenty male New Zealand White rabbits were randomly divided into 2 groups of equal size: ICF group (Group 1) and IMP group (Group 2)...
March 2017: Ulusal Travma Ve Acil Cerrahi Dergisi, Turkish Journal of Trauma & Emergency Surgery: TJTES
https://www.readbyqxmd.com/read/28458330/gender-differences-in-serotonin-signaling-in-patients-with-diarrhea-predominant-irritable-bowel-syndrome
#8
Ryo Katsumata, Akiko Shiotani, Takahisa Murao, Manabu Ishii, Minoru Fujita, Hiroshi Matsumoto, Ken Haruma
Objective Gender differences, including differences in the prevalence, subtypes and the effectiveness of treatment, are generally recognized in irritable bowel syndrome (IBS). Although serotonin type 3 receptor (5-HT3R) antagonists appear to be more effective in women with diarrhea predominant IBS (IBS-D) than they are in men, the mechanisms underlying these effects remain unclear. The aim of the present was to investigate the gender differences in 5-HT signaling. Methods The subjects were selected from outpatients with IBS-D and healthy controls...
2017: Internal Medicine
https://www.readbyqxmd.com/read/28454981/neuropharmacological-characterization-of-the-new-psychoactive-substance-methoxetamine
#9
Laura Hondebrink, Emma E J Kasteel, Anke M Tukker, Fiona M J Wijnolts, Anouk H A Verboven, Remco H S Westerink
The use of new psychoactive substances (NPS) is steadily increasing. One commonly used NPS is methoxetamine (MXE), a ketamine analogue. Several adverse effects have been reported following MXE exposure, while only limited data are available on its neuropharmacological modes of action. We investigated the effects of MXE and ketamine on several endpoints using multiple in vitro models. These included rat primary cortical cells, human SH-SY5Y cells, human induced pluripotent stem cell (hiPSC)-derived iCell(®) Neurons, DopaNeurons and astrocyte co-cultures, and human embryonic kidney (HEK293) cells...
April 25, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28405636/when-transporters-fail-to-be-transported-how-to-rescue-folding-deficient-slc6-transporters
#10
Sonja Sucic, Ameya Kasture, H M Mazhar Asjad, Carina Kern, Ali El-Kasaby, Michael Freissmuth
The human dopamine transporter (hDAT) belongs to the solute carrier 6 (SLC6) gene family. Point mutations in hDAT (SLC6A3) have been linked to a syndrome of dopamine transporter deficiency or infantile dystonia/parkinsonism. The mutations impair DAT folding, causing retention of variant DATs in the endoplasmic reticulum and subsequently impair transport activity. The folding trajectory of DAT itself is not understood, though many insights have been gained from studies of folding-deficient mutants of the closely related serotonin transporter (SERT); i...
December 30, 2016: Journal of Neurology & Neuromedicine
https://www.readbyqxmd.com/read/28404997/novel-fitc-labeled-igy-antibody-fluorescence-imaging-toxoplasma-gondii-in-vitro
#11
Mehtap Sert, Rabia Cakir Koc, Yasemin Budama Kilinc
Toxoplasmosis is caused by T. gondii and can create serious health problems in humans and also worldwide economic harm. Because of the clinical and veterinary importance of toxoplasmosis, its timely and accurate diagnosis has a major impact on disease-fighting strategies. T. gondii surface antigen 1 (SAG1), an immunodominant-specific antigen, is often used as a diagnostic tool. Therefore, the aim of this study was the optimization of novel fluorescein isothiocyanate (FITC) labeling of the SAG1-specific IgY antibody to show the potential for immunofluorescence imaging of T...
April 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28404880/serotonergic-system-antagonists-target-breast-tumor-initiating-cells-and-synergize-with-chemotherapy-to-shrink-human-breast-tumor-xenografts
#12
William D Gwynne, Robin M Hallett, Adele Girgis-Gabardo, Bojana Bojovic, Anna Dvorkin-Gheva, Craig Aarts, Kay Dias, Anita Bane, John A Hassell
Breast tumors comprise an infrequent tumor cell population, termed breast tumor initiating cells (BTIC), which sustain tumor growth, seed metastases and resist cytotoxic therapies. Hence therapies are needed to target BTIC to provide more durable breast cancer remissions than are currently achieved. We previously reported that serotonergic system antagonists abrogated the activity of mouse BTIC resident in the mammary tumors of a HER2-overexpressing model of breast cancer. Here we report that antagonists of serotonin (5-hydroxytryptamine; 5-HT) biosynthesis and activity, including US Federal Food and Drug Administration (FDA)-approved antidepressants, targeted BTIC resident in numerous breast tumor cell lines regardless of their clinical or molecular subtype...
May 9, 2017: Oncotarget
https://www.readbyqxmd.com/read/28396142/atypical-binding-at-dopamine-and-serotonin-transporters-contribute-to-the-discriminative-stimulus-effects-of-mephedrone
#13
Alyssa F DeLarge, Laura L Erwin, Peter J Winsauer
Mephedrone (4-methylmethcathinone), a constituent of the recreational substances known as "bath salts", is a synthetic cathinone that can produce auditory and visual hallucinations, as well as problematic cardiovascular effects. This study compared the discriminative stimulus effects of mephedrone (0.32-10 mg/kg) with other prototypical drugs of abuse: cocaine (0.56-32 mg/kg), d-amphetamine (0.18-3.2 mg/kg), ketamine (1.8-18 mg/kg), phencyclidine (PCP, 1-5.6 mg/kg), heroin (1-10 mg/kg), 2,5-dimethoxy-4-iodoamphetamine (R-DOI, 0...
June 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28342338/antidepressants-and-risk-of-cataract-development-a-population-based-nested-case-control-study
#14
Po-Han Chou, Che-Sheng Chu, Yi-Huei Chen, Min-Yen Hsu, Min-Wei Huang, Tsuo-Hung Lan, Ching-Heng Lin
BACKGROUND: Previous studies demonstrated increased risk of cataract development among users of selective serotonin reuptake inhibitors (SSRIs). However, it remains unknown whether this risk also prevails with the use of other types of antidepressants. The aim of this study was to investigate whether use of antidepressants is associated with an increased risk of cataract development. Moreover, the relationship between binding affinities of serotonin transporter (SERT) of antidepressant and the risk of cataracts is examined...
June 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28331735/metaplastic-breast-carcinoma-analysis-of-clinical-and-pathologic-characteristics-a-case-series
#15
Semra Salimoğlu, İsmail Sert, Mustafa Emiroğlu, Cem Karaali, Dilek Kuzukıran, Yasemin Akyüz Kırmızı, Gülden Diniz, Cengiz Aydın
OBJECTIVE: Metaplastic breast cancer (MBC) is a rare type of breast cancer that is considered to be clinically aggressive. The clinical significance and prognostic risk factors of MBC are limited. This study comprises a retrospective analysis of the clinical and pathologic findings of a series of patients treated for MBC. MATERIALS AND METHODS: The files of 657 patients who underwent surgery because of breast cancer at our clinic were examined and the data found on 11 patients who were diagnosed as having MBC were analyzed...
April 2016: Journal of Breast Health (2013)
https://www.readbyqxmd.com/read/28284954/peri-adolescent-asthma-symptoms-cause-adult-anxiety-related-behavior-and-neurobiological-processes-in-mice
#16
Jasmine I Caulfield, Michael J Caruso, Kerry C Michael, Rebecca A Bourne, Nicole R Chirichella, Laura C Klein, Timothy Craig, Robert H Bonneau, Avery August, Sonia A Cavigelli
Human and animal studies have shown that physical challenges and stressors during adolescence can have significant influences on behavioral and neurobiological development associated with internalizing disorders such as anxiety and depression. Given the prevalence of asthma during adolescence and increased rates of internalizing disorders in humans with asthma, we used a mouse model to test if and which symptoms of adolescent allergic asthma (airway inflammation or labored breathing) cause adult anxiety- and depression-related behavior and brain function...
March 8, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28266501/the-novel-modafinil-analog-jjc8-016-as-a-potential-cocaine-abuse-pharmacotherapeutic
#17
Hai-Ying Zhang, Guo-Hua Bi, Hong-Ju Yang, Yi He, Gilbert Xue, Jiajing Cao, Gianluigi Tanda, Eliot L Gardner, Amy Hauck Newman, Zheng-Xiong Xi
(±)Modafinil ((±)MOD) and its R-enantiomer (R-modafinil; R-MOD) have been investigated for their potential as treatments for psychostimulant addiction. We recently reported a series of (±)MOD analogs, of which JJC8-016 (N-(2-((bis(4-fluorophenyl)methyl)thio)ethyl)-3-phenylpropan-1-amine) was selected for further development. JJC8-016 and R-MOD were evaluated for binding across ~70 receptors, transporters, and enzymes. Although at a concentration of 10 μM, there were many hits for JJC8-016, binding affinities in the range of its DAT affinity were only observed at the serotonin transporter (SERT), dopamine D2-like, and sigma1 receptors...
March 29, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28220701/deconstructed-analogs-of-bupropion-reveal-structural-requirements-for-transporter-inhibition-versus-substrate-induced-neurotransmitter-release
#18
Abdelrahman R Shalabi, Donna Walther, Michael H Baumann, Richard A Glennon
Bupropion (1), an α-aminophenone uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET), is a widely prescribed antidepressant and smoking cessation aid. Cathinone (2), a structurally simpler α-aminophenone, is a substrate-type releasing agent at the same transporters and a recognized drug of abuse. Our goal was to identify the structural features of α-aminophenones that govern the mechanistic transition from uptake inhibition to substrate-induced release. Deconstructed analogs of 1 were synthesized and compared for their ability to interact with DAT, NET, and the serotonin transporter (SERT) using in vitro assay methods...
February 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28220069/effects-of-selective-serotonin-reuptake-inhibitors-on-interregional-relation-of-serotonin-transporter-availability-in-major-depression
#19
Gregory M James, Pia Baldinger-Melich, Cecile Philippe, Georg S Kranz, Thomas Vanicek, Andreas Hahn, Gregor Gryglewski, Marius Hienert, Marie Spies, Tatjana Traub-Weidinger, Markus Mitterhauser, Wolfgang Wadsak, Marcus Hacker, Siegfried Kasper, Rupert Lanzenberger
Selective serotonin reuptake inhibitors (SSRIs) modulate serotonergic neurotransmission by blocking reuptake of serotonin from the extracellular space. Up to now, it remains unclear how SSRIs achieve their antidepressant effect. However, task-based and resting state functional magnetic resonance imaging studies, have demonstrated connectivity changes between brain regions. Here, we use positron emission tomography (PET) to quantify SSRI's main target, the serotonin transporter (SERT), and assess treatment-induced molecular changes in the interregional relation of SERT binding potential (BPND)...
2017: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/28198447/the-tnf-%C3%AE-antagonist-etanercept-reverses-age-related-decreases-in-colonic-sert-expression-and-faecal-output-in-mice
#20
Bhavik Anil Patel, Sara Fidalgo, Chunfang Wang, Leena Parmar, Kasonde Mandona, Annabelle Panossian, Melanie S Flint, Richard N Ranson, M Jill Saffrey, Mark S Yeoman
Treatment for chronic constipation in older people is challenging and the condition has a major impact on quality of life. A lack of understanding about the causes of this condition has hampered the development of effective treatments. 5-HT is an important pro-kinetic agent in the colon. We examined whether alterations in colonic 5-HT signalling underlie age-related changes in faecal output in mice and whether these changes were due to an increase in TNF-α. Components of the 5-HT signalling system (5-HT, 5-HIAA, SERT) and TNF-α expression were examined in the distal colon of 3, 12, 18 and 24-month old mice and faecal output and water content monitored under control conditions and following the administration of etanercept (TNF-α inhibitor; 1 mg Kg(-1))...
February 15, 2017: Scientific Reports
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