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https://www.readbyqxmd.com/read/28802861/contrasting-effects-of-vortioxetine-and-paroxetine-on-pineal-gland-biochemistry-in-a-tryptophan-depletion-model-of-depression-in-female-rats
#1
M Franklin, N Hlavacova, Y Li, I Bermudez, A Csanova, C Sanchez, D Jezova
We studied the effects of the multi-modal antidepressant, vortioxetine and the SSRI, paroxetine on pineal melatonin and monoamine synthesis in a sub-chronic tryptophan (TRP) depletion model of depression based on a low TRP diet. Female Sprague-Dawley rats were randomised to groups a) control, b) low TRP diet, c) low TRP diet+paroxetine and d) low TRP diet+vortioxetine. Vortioxetine was administered via the diet (0.76mg/kg of food weight) and paroxetine via drinking water (10mg/kg/day) for 14days. Both drugs resulted in SERT occupancies >90%...
August 9, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28801295/-foshouningshen-decoction-improves-sleeping-via-the-serotonergic-system-in-a-rat-model-of-insomnia
#2
Jie-Cong Huang, Wei Xie, Ning Deng, Wen-Lin Liang, Dong-Rong Hu, Yu Hong, Yang Zhou
OBJECTIVE: To evaluate the sedative and hypnotic effects of Foshouningshen decoction (FSNSD) and study its effects on expressions of 5-hydroxy tryptamine (5-HT) and 5-HT1A receptor (5-HT1AR) in the hippocampus in a rat model of insomnia. METHODS: Male KM mice were divided into control group, estazolam (0.4 mg/kg daily) group, and low-, moderate-, and high-dose FSNSD groups (daily dose of 12, 24, and 48 g/kg, respectively). After corresponding treatments for 1 week, the mice underwent sleep-inducing test with subthreshold and threshold doses of sodium pentobarbital...
August 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28796998/microrna-dependent-control-of-serotonin-induced-pulmonary-arterial-contraction
#3
Diana Dahan, Tran Thi Hien, Philip Tannenberg, Mari Ekman, Catarina Rippe, Thomas Boettger, Thomas Braun, Karin Tran-Lundmark, Phan-Kiet Tran, Karl Swärd, Sebastian Albinsson
BACKGROUND: Serotonin (5-HT) is considered to play a role in pulmonary arterial hypertension by regulating vascular remodeling and smooth muscle contractility. Here, arteries from mice with inducible and smooth muscle-specific deletion of Dicer were used to address mechanisms by which microRNAs control 5-HT-induced contraction. METHODS: Mice were used 5 weeks after Dicer deletion, and pulmonary artery contractility was analyzed by wire myography. RESULTS: No change was seen in right ventricular systolic pressure following dicer deletion, but systemic blood pressure was reduced...
August 11, 2017: Journal of Vascular Research
https://www.readbyqxmd.com/read/28792478/marine-inspired-2-5-halo-1h-indol-3-yl-n-n-dimethylethanamines-as-modulators-of-serotonin-receptors-an-example-illustrating-the-power-of-bromine-as-part-of-the-uniquely-marine-chemical-space
#4
Mohamed A Ibrahim, Abir T El-Alfy, Kelly Ezel, Mohamed O Radwan, Abbas G Shilabin, Anna J Kochanowska-Karamyan, Howaida I Abd-Alla, Masami Otsuka, Mark T Hamann
In previous studies, we have isolated several marine indole alkaloids and evaluated them in the forced swim test (FST) and locomotor activity test, revealing their potential as antidepressant and sedative drug leads. Amongst the reported metabolites to display such activities was 5-bromo-N,N-dimethyltryptamine. Owing to the importance of the judicious introduction of halogens into drug candidates, we synthesized two series built on a 2-(1H-indol-3-yl)-N,N-dimethylethanamine scaffold with different halogen substitutions...
August 9, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28782490/unmet-needs-in-schizophrenia
#5
Maurizio Pompili, Herbert Y Meltzer
The objectives of this article are to describe current trends in the treatment of schizophrenia and the most interesting new approaches to optimizing outcome and fostering the development of new schizophrenia treatments. RESULTS: Increasing utilization of diverse types of atypical antipsychotic drugs (AAPDs), e.g. clozapine-type serotonin (5-HT)2A and weak dopamine (DA) D2 antagonist, amisulpride, a D2/D3/5-HT7 antagonist, and cariprazine, a D3 partial agonist with additional neurotransmitter targets, is occurring as their advantages in efficacy, especially for cognitive impairment and mood symptoms, and side effects is becoming appreciated...
August 3, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28777821/anatomy-and-behavioral-function-of-serotonin-receptors-in-drosophila-melanogaster-larvae
#6
Annina Huser, Melanie Eschment, Nazli Güllü, Katharina A N Collins, Kathrin Böpple, Lyubov Pankevych, Emilia Rolsing, Andreas S Thum
The biogenic amine serotonin (5-HT) is an important neuroactive molecule in the central nervous system of the majority of animal phyla. 5-HT binds to specific G protein-coupled and ligand-gated ion receptors to regulate particular aspects of animal behavior. In Drosophila, as in many other insects this includes the regulation of locomotion and feeding. Due to its genetic amenability and neuronal simplicity the Drosophila larva has turned into a useful model for studying the anatomical and molecular basis of chemosensory behaviors...
2017: PloS One
https://www.readbyqxmd.com/read/28774871/enteric-serotonin-and-oxytocin-endogenous-regulation-of-severity-in-a-murine-model-of-necrotizing-enterocolitis
#7
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/28771848/5-ht-modulates-the-rat-mesenteric-vasopressor-outflow-by-5-ht1d-sympatholytic-receptors
#8
José-Ángel García-Pedraza, Mónica García-Domingo, Miriam Gómez-Roso, Alicia Rodríguez-Barbero, María-Luisa Martín, Asunción Morán
5-hydroxytryptamine (5-HT) modulates noradrenergic activity in different cardiovascular territories, but its effect on the mesenteric vasopressor outflow has not yet been clarified. This study investigated the in vivo serotonergic influence, characterizing 5-HT receptors implicated, in sympathetic innervation of mesenteric vasculature. Wistar rats were anaesthetised and prepared for the in situ autoperfused rat mesentery, monitoring systemic blood pressure (SBP), heart rate (HR) and mesenteric perfusion pressure (MPP)...
August 3, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28769809/apixaban-enhances-vasodilatation-mediated-by-protease-activated-receptor-2-in-isolated-rat-arteries
#9
Ambra Villari, Giovanni Giurdanella, Claudio Bucolo, Filippo Drago, Salvatore Salomone
Apixaban (APX) is a direct inhibitor of factor X (FXa) approved for prophylaxis and treatment of deep venous thrombosis and atrial fibrillation. Because FXa activates protease-activated receptor 2 (PAR-2) in endothelium and vascular smooth muscle, inhibition of FXa by APX may affect vasomotor function. The effect of APX was assessed in vitro, by wire myography, in rat mesenteric resistance arteries (MRAs) and basilar arteries challenged with vasoconstrictors [phenylephrine (PE); 5-hydroxytryptamine (5-HT)], vasodilators [acetylcholine (ACh); sodium nitroprusside (SNP)] or with the PAR-2 peptide agonist SLIGRL...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28768570/primary-cytoreductive-surgery-and-adjuvant-hormonal-monotherapy-in-women-with-advanced-low-grade-serous-ovarian-carcinoma-reducing-overtreatment-without-compromising-survival
#10
Amanda N Fader, Jennifer Bergstrom, Amelia Jernigan, Edward J Tanner, Kara Long Roche, Rebecca L Stone, Kimberly L Levinson, Stephanie Ricci, Stephanie Wethingon, Tian-Li Wang, Ie-Ming Shih, Bin Yang, Gloria Zhang, Deborah K Armstrong, Stephanie Gaillard, Chad Michener, Robert DeBernardo, Peter G Rose
OBJECTIVES: Women with advanced-stage, low-grade serous ovarian carcinoma (LGSC) have low chemotherapy response rates and poor overall survival. Most LGSC tumors overexpress hormone receptors, which represent a potential treatment target. Our study objective was to determine the outcomes of patients with advanced-stage LGSC treated with primary cytoreductive surgery (CRS) and hormone therapy (HT). METHODS: A retrospective study was performed at two academic cancer centers...
July 30, 2017: Gynecologic Oncology
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
#11
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/28766214/factors-influencing-use-of-hormone-therapy-for-ductal-carcinoma-in-situ-a-national-cancer-database-study
#12
Toan T Nguyen, Tanya L Hoskin, Courtney N Day, Elizabeth B Habermann, Matthew P Goetz, Judy C Boughey
BACKGROUND: Adjuvant hormonal therapy (HT) reduces breast cancer recurrence risk in estrogen receptor-positive (ER+) ductal carcinoma in situ (DCIS). We assessed national practice patterns and influence of surgery and pathology on HT use in DCIS. METHODS: Data on DCIS patients diagnosed from 2004 to 2014 were extracted from the National Cancer Database, and patients were classified according to ER status and whether HT was received. Factors associated with HT use were assessed using Chi square tests for univariate analysis and logistic regression for multivariate analysis...
August 1, 2017: Annals of Surgical Oncology
https://www.readbyqxmd.com/read/28761080/serotonin-inputs-to-the-dorsal-bnst-modulate-anxiety-in-a-5-ht1a-receptor-dependent-manner
#13
A L Garcia-Garcia, S Canetta, J M Stujenske, N S Burghardt, M S Ansorge, A Dranovsky, E D Leonardo
Serotonin (5-HT) neurons project from the raphe nuclei throughout the brain where they act to maintain homeostasis. Here, we study 5-HT inputs into the bed nucleus of the stria terminalis (BNST), a major subdivision of the extended amygdala that has been proposed to regulate responses to anxiogenic environments in humans and rodents. While the dorsal part of the BNST (dBNST) receives dense 5-HT innervation, whether and how 5-HT in the dBNST normally modulates anxiety remains unclear. Using optogenetics, we demonstrate that activation of 5-HT terminals in the dBNST reduces anxiety in a highly anxiogenic environment...
August 1, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28758583/new-trends-in-the-treatment-of-schizophrenia
#14
Herbert Y Meltzer
The objectives of this article are to describe current trends in the treatment of schizophrenia and the most interesting new approaches to optimizing outcome and fostering the development of new schizophrenia treatments. RESULTS: Increasing utilization of diverse types of atypical antipsychotic drugs (AAPDs), e.g. clozapine-type serotonin (5-HT)2A and weak dopamine (DA) D2 antagonist, amisulpride, a D2/D3/5-HT7 antagonist, and cariprazine, a D3 partial agonist with additional neurotransmitter targets, is occurring as their advantages in efficacy, especially for cognitive impairment and mood symptoms, and side effects is becoming appreciated...
July 28, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28757154/the-central-serotonin2b-receptor-as-a-new-pharmacological-target-for-the-treatment-of-dopamine-related-neuropsychiatric-disorders-rationale-and-current-status-of-research
#15
REVIEW
Céline Devroye, Adeline Cathala, Pier Vincenzo Piazza, Umberto Spampinato
The serotonin2B receptor (5-HT2BR), which was first cloned and characterized in the rat stomach fundus, is the most recent addition to the 5-HT2R family. While its involvement in the regulation of gastrointestinal, vascular, pulmonary and cardiac physiology has been widely investigated, its functional role within the central nervous system (CNS) has received much less attention. Nevertheless, when considering the data available in the literature with regards to the regulatory control exerted by the central 5-HT2BR on dopamine (DA) and serotonin (5-HT) neuron activity, a very interesting picture emerges and highlights the key role of these receptors for future therapeutic strategies of DA-related neuropsychiatric disorders...
July 27, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28752054/serotonergic-modulation-of-the-activity-of-glp-1-producing-neurons-in-the-nucleus-of-the-solitary-tract-in-mouse
#16
Marie K Holt, Ida J Llewellyn-Smith, Frank Reimann, Fiona M Gribble, Stefan Trapp
OBJECTIVE: Glucagon-like peptide-1 (GLP-1) and 5-HT are potent regulators of food intake within the brain. GLP-1 is expressed by preproglucagon (PPG) neurons in the nucleus tractus solitarius (NTS). We have previously shown that PPG neurons innervate 5-HT neurons in the ventral brainstem. Here, we investigate whether PPG neurons receive serotonergic input and respond to 5-HT. METHODS: We employed immunohistochemistry to reveal serotonergic innervation of PPG neurons...
August 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28751862/utp-gated-signaling-pathways-of-5-ht-release-from-bon-cells-as-a-model-of-human-enterochromaffin-cells
#17
Andromeda Liñán-Rico, Fernando Ochoa-Cortes, Alix Zuleta-Alarcon, Mazin Alhaj, Esmerina Tili, Josh Enneking, Alan Harzman, Iveta Grants, Sergio Bergese, Fievos L Christofi
Background: Enterochromaffin cells (EC) synthesize and release 5-HT and ATP to trigger or modulate gut neural reflexes and transmit information about visceral/pain sensation. Alterations in 5-HT signaling mechanisms may contribute to the pathogenesis of IBD or IBS, but the pharmacologic or molecular mechanisms modulating Ca(2+)-dependent 5-HT release are not understood. Previous studies indicated that purinergic signaling via ATP and ADP is an important mechanism in modulation of 5-HT release. However, EC cells also respond to UTP and UDP suggesting uridine triphosphate receptor and signaling pathways are involved as well...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28750135/ameliorative-effect-of-chlorpromazine-hydrochloride-on-visceral-hypersensitivity-in-rats-possible-involvement-of-5-ht2a-receptor
#18
Teita Asano, Ken-Ichiro Tanaka, Arisa Tada, Hikaru Shimamura, Rikako Tanaka, Hiroki Maruoka, Tohru Mizushima, Mitsuko Takenaga
BACKGROUND AND PURPOSE: Visceral hypersensitivity is responsible for pathogenesis of irritable bowel syndrome (IBS). Therefore, its prevention can help avoid abdominal pain and discomfort in IBS. To find candidate drugs for visceral hypersensitivity, we screened existing medicines for their ability to prevent visceral sensitivity induced by colorectal distension (CRD) in rats and identified chlorpromazine, a typical antipsychotic drug, as a candidate compound. In this study, we investigated the effect of chlorpromazine on visceral hypersensitivity...
July 27, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28749698/the-safety-and-efficacy-of-the-5-ht-1f-receptor-agonist-lasmiditan-in-the-acute-treatment-of-migraine
#19
Bianca Raffaelli, Heike Israel, Lars Neeb, Uwe Reuter
Migraine is among the most disabling disorders worldwide, with a significant therapeutic need. Triptans are drugs of choice in the acute attack treatment, but they are contraindicated in patients with vascular conditions due to their potential vasoconstrictive properties. Further limitations include side effects, inconsistency in therapeutic action and possible non-response. Lasmiditan, a highly selective 5-HT1F receptor agonist, is a novel acute anti-migraine substance devoid of vasoconstriction. Areas covered: This article reviews the clinical efficacy and safety of oral and intravenous lasmiditan as a possible acute migraine treatment...
July 27, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28745513/modulating-the-serotonin-receptor-spectrum-of-pulicatin-natural-products
#20
Zhenjian Lin, Misty D Smith, Gisela P Concepcion, Margo G Haygood, Baldomero M Olivera, Alan Light, Eric W Schmidt
Serotonin (5-HT) receptors are important in health and disease, but the existence of 14 subtypes necessitates selective ligands. Previously, the pulicatins were identified as ligands that specifically bound to the subtype 5-HT2B in the 500 nM to 10 μM range and that exhibited in vitro effects on cultured mouse neurons. Here, we examined the structure-activity relationship of 30 synthetic and natural pulicatin derivatives using binding, receptor functionality, and in vivo assays. The results reveal the 2-arylthiazoline scaffold as a tunable serotonin receptor-targeting pharmacophore...
July 26, 2017: Journal of Natural Products
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