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Serotonin transporter

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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/28811134/a-new-chemotype-inhibitor-for-the-human-organic-cation-transporter-3-hoct3
#2
Xiaolei Pan, Kavita A Iyer, Hebing Liu, Douglas H Sweet, Małgorzata Dukat
Human organic cation transporters (OCTs) represent an understudied neurotransmitter uptake mechanism for which no selective agents have yet been identified. Several neurotransmitters (e.g. serotonin, norepinephrine) are low-affinity substrates for these transporters, but possess higher affinity for other transporters (e.g. the serotonin or norepinephrine transporters; SERT and NET, respectively). We have identified a new class of OCT inhibitors with a phenylguanidine structural scaffold. Here, we examine the actions of a series of such compounds and report preliminary structure-activity relationships (SARs) - the first dedicated SAR study of OCT3 action...
August 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28807575/triple-reuptake-inhibitors-design-synthesis-and-structure-activity-relationship-of-benzylpiperidine-tetrazoles
#3
Suresh Paudel, Xiao Min, Srijan Acharya, Daulat Bikram Khadka, Goo Yoon, Kyeong-Man Kim, Seung Hoon Cheon
Monoamine transporters are important targets in the treatment of various central nervous disorders. Several limitations of traditional reuptake inhibitors, like delayed onset of action, insomnia, and sexual dysfunction, have compelled the search for safer, more effective compounds. In this study, we have sought to identify novel monoamine reuptake inhibitors. Based upon the docking study of compounds that we had reported previously, aromatic rings (A1) were modified to generate a novel series of benzylpiperidine-tetrazoles...
July 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28805431/disentangling-the-effects-of-serotonin-on-risk-perception-s-carriers-of-5-httlpr-are-primarily-concerned-with-the-magnitude-of-the-outcomes-not-the-uncertainty
#4
Philip Millroth, Peter Juslin, Elias Eriksson, Thomas Agren
Serotonin signaling is vital for reward processing, and hence, also for decision-making. The serotonin transporter gene linked polymorphic region (5-HTTLPR) has been connected to decision making, suggesting that short-allele carriers (s) are more risk averse than long-allele homozygotes (ll). However, previous research has not identified if this occurs because s-carriers (i) are more sensitive to the uncertainty of the outcomes or (ii) are more sensitive to the magnitude of the outcomes. This issue was disentangled using a willingness-to-pay task, where the participants evaluated prospects involving certain gains, uncertain gains, and ambiguous gains...
August 14, 2017: Behavioral Neuroscience
https://www.readbyqxmd.com/read/28802938/impulse-control-and-related-disorders-in-parkinson-s-disease
#5
Daniel Weintraub, Daniel O Claassen
Impulse control disorders (ICDs), such as compulsive gambling, buying, sexual, and eating behaviors, are a serious and increasingly recognized complication in Parkinson's disease (PD), occurring in up to 20% of PD patients over the course of their illness. Related behaviors include punding (stereotyped, repetitive, purposeless behaviors), dopamine dysregulation syndrome (DDS) (compulsive medication overuse), and hobbyism (e.g., compulsive internet use, artistic endeavors, and writing). These disorders have a significant impact on quality of life and function, strain interpersonal relationships, and worsen caregiver burden, and are associated with significant psychiatric comorbidity...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28800511/the-serotonin-transporter-promoter-variant-5-httlpr-and-childhood-adversity-are-associated-with-the-personality-trait-openness-to-experience
#6
Md Shafiqur Rahman, Peter Guban, Mei Wang, Philippe A Melas, Yvonne Forsell, Catharina Lavebratt
There is evidence supporting an association between the serotonin-transporter-linked polymorphic region (5-HTTLPR) and the Five Factor Model (FFM) of human personality. 5-HTTLPR has also been found to interact with stressful life events to increase risk of psychopathology. In the present study, by taking into account stressful life events in the form of childhood adversity, we examined the association between 5-HTTLPR and FFM traits using an adult Swedish cohort (N = 3112). We found that 5-HTTLPR was significantly associated with openness (to experience)...
July 31, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28797691/antidepressant-like-activity-of-venlafaxine-and-clonidine-in-mice-exposed-to-single-prolonged-stress-a-model-of-post-traumatic-stress-disorder-pharmacodynamic-and-molecular-docking-studies
#7
Natalia Malikowska, Łukasz Fijałkowski, Alicja Nowaczyk, Piotr Popik, Kinga Sałat
BACKGROUND: Post-traumatic stress disorder (PTSD) is a growing issue worldwide characterized by stress and anxiety in response to re-experiencing traumatic events which strongly impair patient's quality of life and social functions. Available antidepressant and anxiolytic drugs are not efficacious in the majority of treated individuals. This necessitates a significant medical demand to develop novel therapeutic strategies for PTSD. EXPERIMENTAL APPROACH: Animal model of PTSD was induced using a mouse single prolonged stress protocol (mSPS)...
August 7, 2017: Brain Research
https://www.readbyqxmd.com/read/28796292/exposure-to-low-environmental-concentrations-of-manganese-lead-and-cadmium-alters-the-serotonin-system-of-blue-mussels
#8
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/28793232/interaction-effect-between-5-httlpr-and-htr1a-rs6295-polymorphisms-on-the-frontoparietal-network
#9
Haixia Long, Bing Liu, Chao Wang, Xiaolong Zhang, Jin Li, Chunshui Yu, Tianzi Jiang
Previous studies have shown a close relationship between the serotonin system and working memory, but the neural mechanism for the role of the serotonin system on the working memory is unclear. The frontoparietal network is involved in working memory and is associated with the serotonin system. Therefore, this study investigated the interaction effect of the serotonin transporter-linked polymorphic region (5-HTTLPR) and the polymorphism in the serotonin 1A receptor gene (rs6295) on the frontoparietal network obtained from the independent component analysis in a large, young Chinese sample population...
August 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/28790927/the-role-of-sulfide-oxidation-impairment-in-the-pathogenesis-of-primary-coq-deficiency
#10
REVIEW
Catarina M Quinzii, Marta Luna-Sanchez, Marcello Ziosi, Agustin Hidalgo-Gutierrez, Giulio Kleiner, Luis C Lopez
Coenzyme Q (CoQ) is a lipid present in all cell membranes. One of the multiple metabolic functions of CoQ is to transport electrons in the reaction catalyzed by sulfide:quinone oxidoreductase (SQOR), the first enzyme of the oxidation pathway of sulfides (hydrogen sulfide, H2S). Early evidence of a defect in the metabolism of H2S in primary CoQ deficiency came from yeast studies in Schizosaccharomyces pombe strains defective for dps1 and ppt1 (homologs of PDSS1 and COQ2, respectively), which have H2S accumulation...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28790887/mir-16-and-fluoxetine-both-reverse-autophagic-and-apoptotic-change-in-chronic-unpredictable-mild-stress-model-rats
#11
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/28790021/deficient-striatal-adaptation-in-aminergic-and-glutamatergic-neurotransmission-is-associated-with-tardive-dyskinesia-in-non-human-primates-exposed-to-antipsychotic-drugs
#12
Catherine Lévesque, Giovanni Hernandez, Souha Mahmoudi, Frédéric Calon, Fabrizio Gasparini, Baltazar Gomez-Mancilla, Pierre J Blanchet, Daniel Lévesque
Tardive dyskinesia (TD) is a potentially disabling condition encompassing all delayed, persistent, and often irreversible abnormal involuntary movements arising in a fraction of subjects during long-term exposure to centrally acting dopamine receptor-blocking agents such as antipsychotic drugs and metoclopramide. However, the pathogenesis of TD has proved complex and remains elusive. To investigate the mechanism underlying the development of TD, we have chronically exposed 17 Cebus apella monkeys to typical (11) or atypical (6) antipsychotic drugs...
August 5, 2017: Neuroscience
https://www.readbyqxmd.com/read/28781163/polypharmacology-of-conformationally-locked-methanocarba-nucleosides
#13
REVIEW
Kenneth A Jacobson, Dilip K Tosh, Kiran S Toti, Antonella Ciancetta
A single molecular scaffold can be adapted to interact with diverse targets, either separately or simultaneously. Nucleosides and nucleotides in which ribose is substituted with bicyclo[3.1.0]hexane are an example of a versatile drug-like scaffold for increasing selectivity at their classical targets: kinases, polymerases, adenosine and P2 receptors. Also, by applying structure-based functional group manipulations, rigidified adenosine derivatives can be repurposed to satisfy pharmacophoric requirements of various GPCRs, ion channels, enzymes and transporters, initially detected as off-target activities...
August 3, 2017: Drug Discovery Today
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/28774778/frontiers-in-endocrine-disruption-impacts-of-organotin-on-the-hypothalamus-pituitary-thyroid-axis
#15
REVIEW
Ana Paula Santos-Silva, Marcelle Novaes Andrade, Paula Pereira-Rodrigues, Francisca Diana Paiva-Melo, Paula Soares, Jones Bernardes Graceli, Glaecir Roseni Mundstock Dias, Andrea Claudia Freitas Ferreira, Denise Pires de Carvalho, Leandro Miranda-Alves
Endocrine disruptors (EDs), chemical substances widely used in industry and ubiquitously distributed in the environment, are able to interfere with the synthesis, release, transport, metabolism, receptor binding, action, or elimination of endogenous hormones. EDs affect homeostasis mainly by acting on nuclear and nonnuclear steroid receptors but also on serotonin, dopamine, norepinephrine and orphan receptors in addition to thyroid hormone receptors. Tributyltin (TBT), an ED widely used as a pesticide and biocide in antifouling paints, has well-documented actions that include inhibiting aromatase and affecting the nuclear receptors PPARγ and RXR...
July 31, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28774705/serotonin-transporter-gene-promoter-methylation-in-peripheral-cells-in-healthy-adults-neural-correlates-and-tissue-specificity
#16
Elmira Ismaylova, Jessica Di Sante, Moshe Szyf, Zsofia Nemoda, Wei-Jo Yu, Florence B Pomares, Gustavo Turecki, Gabriella Gobbi, Frank Vitaro, Richard E Tremblay, Linda Booij
Early adversity can influence gene expression via epigenetic mechanisms, including DNA methylation. Peripheral tissues are essential in psychiatric epigenetics, as methylation generally cannot be assessed in the living human brain. Several magnetic resonance imaging (MRI) studies show associations of peripheral serotonin transporter gene (SLC6A4) methylation with function and/or structure of frontal-limbic circuits and brain's resting-state. Commonly used samples are derived from blood, saliva or buccal cells...
July 31, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28771712/organization-of-alpha-transducin-immunoreactive-system-in-the-brain-and-retina-of-larval-and-young-adult-sea-lamprey-petromyzon-marinus-and-their-relationship-with-other-neural-systems
#17
Antón Barreiro-Iglesias, Blanca Fernández-López, Daniel Sobrido-Cameán, Ramón Anadón
We employed an anti-transducin antibody (Gαt-S), in combination with other markers, to characterize the Gαt-S-immunoreactive (ir) system in the CNS of the sea lamprey, Petromyzon marinus. Gαt-S immunoreactivity was observed in some neuronal populations and numerous fibers distributed throughout the brain. Double Gαt-S- and opsin-ir neurons (putative photoreceptors) are distributed in the hypothalamus (postoptic commissure nucleus, dorsal and ventral hypothalamus) and caudal diencephalon, confirming results of García-Fernández et al...
August 2, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28769770/regulatory-mechanisms-controlling-maturation-of-serotonin-neuron-identity-and-function
#18
William C Spencer, Evan S Deneris
The brain serotonin (5-hydroxytryptamine; 5-HT) system has been extensively studied for its role in normal physiology and behavior, as well as, neuropsychiatric disorders. The broad influence of 5-HT on brain function, is in part due to the vast connectivity pattern of 5-HT-producing neurons throughout the CNS. 5-HT neurons are born and terminally specified midway through embryogenesis, then enter a protracted period of maturation, where they functionally integrate into CNS circuitry and then are maintained throughout life...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28767225/new-trends-and-current-status-of%C3%A2-pet-and-spect-radioligands-for-neuronal%C3%A2-5-ht%C3%A2-receptors-5-htrs-and-serotonin-transporter-sert
#19
Puja Panwar Hazari, Ankita Pandey, Shubhra Chaturvedi, Anil Kumar Mishra
The critical role of serotonin (5-hydroxytryptamine; 5-HT) and its receptors (5-HTRs) in the pathophysiology of various neuropsychiatric and neurodegenerative disorders render them attractive diagnostic/therapeutic targets for brain disorders. Therefore, in vivo assessment of binding of 5-HT receptor ligands under a multitude of physiologic and pathologic scenario may support the more accurate identification of disease and its progression, patient's response to therapy, and the screening of novel therapeutic strategies...
August 2, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28766852/serotonin-transporter-promoter-polymorphism-modulates-the-ability-to-control-food-intake-effect-on-total-weight-loss
#20
Gemma Bonnet, Purificación Gómez-Abellán, Beatriz Vera, Juan Francisco Sánchez-Romera, Antonio M Hernández-Martínez, Silvia Sookoian, Carlos Jose Pirola, Marta Garaulet
SCOPE: The biggest challenge for losing weight is the ability to control the amount of food eaten; the tendency to overeat is called disinhibition. Our aims were to determine whether a) the SLC6A4-promoter variant (5-HTTLPR) relates to disinhibition; b) this association could affect total weight-loss during a behavioral/dietary treatment for obesity. METHODS AND RESULTS: 2961 subjects attended voluntarily five weight-loss clinics; a subsample (n = 624) was recruited for SLC6A4 genotyping...
August 2, 2017: Molecular Nutrition & Food Research
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