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https://www.readbyqxmd.com/read/28815595/sigma-1-receptor-ligands-inhibit-catecholamine-secretion-from-adrenal-chromaffin-cells-due-to-block-of-nicotinic-acetylcholine-receptors
#1
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 (SERT) is expressed in ACCs and interacts with 5-HT1A receptors to control secretion...
August 16, 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
#2
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 serotonin system can be affected by metals, the effects of environmental concentration of metals, such as manganese (Mn), lead (Pd), and cadmium (Cd), have never been studied in blue mussels. This study aims to determine the effects of exposure to Mn, Pb or Cd on serotonin levels, monoamine oxidase (MAO) activity, and serotonin transporter (SERT) 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
#3
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
#4
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
#5
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
#6
Adam Bucki, Monika Marcinkowska, Joanna Śniecikowska, Krzysztof Więckowski, Maciej H 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...
August 1, 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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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