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Serotonin receptor subtype

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https://www.readbyqxmd.com/read/28544903/estrogen-receptor-%C3%AE-deficiency-impairs-bdnf-5-ht2a-signaling-in-the-hippocampus-of-female-brain-a-possible-mechanism-for-menopausal-depression
#1
Anindit Chhibber, Sarah K Woody, M A Karim Rumi, Michael J Soares, Liqin Zhao
Depression currently affects 350 million people worldwide and 19 million Americans each year. Women are 2.5 times more likely to experience major depression than men, with some women appearing to be at a heightened risk during the menopausal transition. Estrogen signaling has been implicated in the pathophysiology of mood disorders including depression; however, the underlying mechanisms are poorly understood. In this study, the role of estrogen receptor (ER) subtypes, ERα and ERβ, in the regulation of brain-derived neurotrophic factor (BDNF) and serotonin (5-HT) signaling was investigated; two pathways that have been hypothesized to be interrelated in the etiology of depression...
May 18, 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28483714/purposeless-oral-activity-induced-by-meta-chlorophenylpiperazine-m-cpp-undefined-tic-like-behaviors
#2
Deborah S Kreiss, Philippe De Deurwaerdère
BACKGROUND: The pathophysiological hypothesis underlying tic disorders in Tourette syndrome (TS) is that basal ganglia are not capable of properly filtering cortical information, leading patients with difficulties in inhibiting unwanted behaviors or impulses. One of the main challenges for furthering such a hypothesis is to find appropriate animal models summarizing some aspects of the disease. METHODS: It has been established for more than 25 years in rodents that the prototypical serotonin (5-HT) agonist meta-chlorophenylpiperazine (m-CPP) elicits purposeless oral movements including chewing behavior...
May 5, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/28483393/activation-of-5-ht7-receptors-reverses-nmda-r-dependent-ltd-by-activating-pka-in-medial-vestibular-neurons
#3
Yan-Hai Li, Lei Han, Kenneth Lap-Kei Wu, Ying-Shing Chan
The medial vestibular nucleus (MVN) is a major output station for neurons that project to the vestibulo-spinal pathway. MVN neurons show capacity for long-term depression (LTD) during the juvenile period. We investigated LTD of MVN neurons using whole-cell patch-clamp recordings. High frequency stimulation (HFS) robustly induced LTD in 90% of type B neurons in the MVN, while only 10% of type A neurons were responsive, indicating that type B neurons are the major contributors to LTD in the MVN. The neuromodulator serotonin (5-HT) is known to modulate LTD in neural circuits of the cerebral cortex and the hippocampus...
May 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28459524/growing-evidence-for-heterogeneous-synaptic-localization-of-5-ht2a-receptors
#4
Carine Bécamel, Coralie Berthoux, Alexander Barre, Philippe Marin
The serotonin 2A (5-HT2A) receptor subtype continues to attract attention as a target for numerous psychoactive drugs including psychedelic hallucinogens, antidepressants, anxiolytics, and atypical antipsychotics. 5-HT2A receptors are a principal G protein-coupled receptor subtype mediating the excitatory effects of serotonin. Nonetheless, pre- vs postsynaptic localization of 5HT2A receptors, relative to glutamatergic synapses, has remained controversial. Here, we discuss recent findings highlighting the existence and roles of presynaptic 5-HT2A receptors in regulating glutamatergic transmission and cognition...
May 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28458330/gender-differences-in-serotonin-signaling-in-patients-with-diarrhea-predominant-irritable-bowel-syndrome
#5
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/28414989/role-of-cortical-alpha-2-adrenoceptors-in-alcohol-withdrawal-induced-depression-and-tricyclic-antidepressants
#6
Bruk Getachew, Sheketha R Hauser, Antonei B Csoka, Robert E Taylor, Yousef Tizabi
INTRODUCTION: Although a role for alpha-2 adrenoceptors (alpha-2 ARs) in alcohol use disorder (AUD) and depression is suggested, very little information on a direct interaction between alcohol and these receptors is available. METHODS: In this study adult female Wistar and Wistar-Kyoto (WKY) rats, a putative animal model of depression, were exposed to alcohol vapor 3h daily for 10days (blood alcohol concentration ∼150mg%) followed by daily injection of 10mg/kg of imipramine (IMP, a selective norepinephrine NE/serotonin reuptake inhibitor) or nomifensine (NOMI, a selective NE/dopamine reuptake inhibitor)...
April 4, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28404880/serotonergic-system-antagonists-target-breast-tumor-initiating-cells-and-synergize-with-chemotherapy-to-shrink-human-breast-tumor-xenografts
#7
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/28361518/ketanserin-and-naftopidil-enhance-the-potentiating-effect-of-alpha-methyl-serotonin-on-the-neurally-induced-contraction-of-human-isolated-urinary-bladder-muscle-strips
#8
Tsuyoshi Hattori, Philippe Lluel, Céline Rouget, Moèz Rekik, Mitsuharu Yoshiyama
PURPOSE: The aim of this study was to assess the potential involvement of a specific subtype of 5-hydroxytryptamine (5-HT), 5HT2 receptors in neurally-induced contractions of the human detrusor. METHODS: Contractile responses to electrical field stimulation (EFS) were examined in human isolated urinary bladder muscle strips. The potentiation of EFS-induced detrusor contraction was examined by adding cumulative concentrations of a 5-HT and 5-HT2 receptor agonist, α-methyl-serotonin (α-Me-5-HT) (1nM-100μM) in the presence or absence of a 5-HT2 antagonist, ketanserin (5-HT2A>5-HT2C) or naftopidil (5-HT2B>5-HT2A) (0...
March 24, 2017: International Neurourology Journal
https://www.readbyqxmd.com/read/28322152/serotonin-receptor-binding-characteristics-of-geissoschizine-methyl-ether-an-indole-alkaloid-in-uncaria-hook
#9
Yasushi Ikarashi, Kyoji Sekiguchi, Kazushige Mizoguchi
Geissoschizine methyl ether (GM) is one of the indole alkaloids in Uncaria hook, and an active ingredient of yokukansan (YKS) that improves behavioral and psychological symptoms of dementia (BPSD) in patients with several types of dementia. The pharmacological action of GM has been related to various serotonin (5-HT) receptor subtypes. Here we describe previous findings and our own data to review the binding characteristics of GM to the 5-HT receptor subtypes. Competitive receptor-binding assays showed that GM bound the following 5-HT receptor subtypes: 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4, 5-HT5A, 5-HT6, and 5-HT7...
March 20, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28258217/heterodimers-of-serotonin-receptor-subtypes-2-are-driven-by-5-ht2c-protomers
#10
Imane Moutkine, Emily Quentin, Bruno P Guiard, Luc Maroteaux, Stephane Doly
The serotonin receptor subtypes 2 comprise 5-HT2A, 5-HT2B, and 5-HT2C, which are Gαq-coupled receptors and display distinct pharmacological properties. Although co-expressed in some brain regions and involved in various neurological disorders, their functional interactions have not yet been studied. We report that 5-HT2 receptors can form homo- and heterodimers when expressed alone or co-expressed in transfected cells. Co-immunoprecipitation and bioluminescence resonance energy transfer studies confirmed that 5-HT2C receptors interact with either 5-HT2A or 5-HT2B receptors...
April 14, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28240194/brain-and-gut-crf-signaling-biological-actions-and-role-in-the-gastrointestinal-tract
#11
Yvette Taché, Mulugeta Million, Muriel Larauche, Pu-Qing Yuan
Corticotropin-releasing factor (CRF) signaling pathways coordinate the behavioral, endocrine, autonomic and visceral responses to stress. Convergent anatomical, molecular, pharmacological and functional experimental evidence supports an important role of brain CRF receptor signaling in stress-related alterations of gastrointestinal functions. These include the inhibition of gastric acid secretion and gastro-small intestinal transit, the stimulation of colonic enteric nervous system and secretory-motor function, enhanced intestinal permeability, and visceral hypersensitivity...
February 23, 2017: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/28237803/serotonin-mediated-modulation-of-acetylcholine-induced-intracellular-calcium-responses-in-chromaffin-cells-isolated-from-the-rat-adrenal-medulla
#12
Takuya Yokoyama, Yoshio Yamamoto, Tomoyuki Saino
We examined serotonin (5-HT)-mediated modulation of acetylcholine (ACh)-induced intracellular Ca(2+) ([Ca(2+)]i) responses in rat adrenal chromaffin cells using calcium imaging. 5-HT did not induce any [Ca(2+)]i response in clustered chromaffin cells. However, the magnitude of ACh-induced [Ca(2+)]i increases in the same specimens was inhibited in the presence of 5-HT. ACh-induced [Ca(2+)]i increases in chromaffin cells were also inhibited by the 5-HT1A receptor agonist, 8-hydroxy-2-(dipropylamino) tetralin hydrobromide, but were not changed by the 5-HT1B, 5-HT2, or 5-HT3 receptor agonists, CP93129, α-methyl-5-HT, or 1-(m-chlorophenyl) biguanide, respectively...
February 22, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28221788/substituted-2-aminopyrimidines-selective-for-%C3%AE-7-nicotinic-acetylcholine-receptor-activation-and-association-with-acetylcholine-binding-proteins
#13
Katarzyna Kaczanowska, Gisela Andrea Camacho Hernandez, Larissa Bendiks, Larissa Kohs, Jose Manuel Cornejo-Bravo, Michal Harel, M G Finn, Palmer Taylor
Through studies with ligand binding to the acetylcholine binding protein (AChBP), we previously identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrogate of the nicotinic acetylcholine receptor (nAChR) in a cooperative fashion, not seen for classical nicotinic agonists and antagonists. To examine receptor interactions of this structural family on ligand-gated ion channels, we employed HEK cells transfected with cDNAs encoding three requisite receptor subtypes: α7-nAChR, α4β2-nAChR, and a serotonin receptor (5-HT3AR), along with a fluorescent reporter...
March 1, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28219707/22-azidosalvinorin-a-exhibits-antidepressant-like-effect-in-mice
#14
James Oluwagbamigbe Fajemiroye, Polepally Reddy Prabhakar, Luiz Carlos da Cunha, Elson Alves Costa, Jordan K Zjawiony
The increasing cases of depression has made the searches for new drugs and understanding of the underligning neurobiology of this psychiatric disorder a necessity. Here, we modified the structure of salvinorin A (a known halucinogen) and investigated antidepressant-like activity of its four derivatives; 22-methylsulfanylsalvinorin A(SA1), 2-O-cinnamoylsalvinorin B (CSB), 22-azidosalvinorin A (SA2), and 2-O-(4(')-azidophenylsulfonyl)salvinorin B (SA3). Prior to behavioural tests (Irwin test, open field test - OFT, forced swimming test - FST and tail suspension test - TST), SA1 was prepared by reacting salvinorin B and methylthioacetic acid with 89% yield; CSB was obtained from the reaction of salvinorin B and cinnamic acid with 92% yield; SA2 was obtained from the reaction of salvinorin B and azidoacetic acid with 81% yield; and SA3 was prepared by reacting salvinorin B with 4-azidophenylsulfonyl chloride with 80% yield...
April 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28194935/a-potential-pet-radiotracer-for-the-5-ht2c-receptor-synthesis-and-in-vivo-evaluation-of-4-3-18-f-fluorophenethoxy-pyrimidine
#15
Juhyeon Kim, Byung Seok Moon, Byung Chul Lee, Ho-Young Lee, Hak-Joong Kim, Hyunah Choo, Ae Nim Pae, Yong Seo Cho, Sun-Joon Min
The serotonin 2C receptor subtype (5-HT2C) is an excitatory 5-HT receptor widely distributed throughout the central nervous system. As the 5-HT2C receptor displays multiple actions on various neurotransmitter systems including glutamate, dopamine, epinephrine, and γ-aminobutyric acid (GABA), abnormalities of the 5-HT2C receptor are associated with psychiatric diseases such as depression, schizophrenia, drug abuse, and anxiety. Up to date, three kinds of 5-HT2C PET radiotracers such as [(11)C]N-methylated arylazepine (1), [(11)C]WAY-163909 (2), and [(18)F]fluorophenylcyclopropane (3) have been developed, but they may not be suitable for in vivo 5-HT2C imaging study due to their modest specific binding...
February 27, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28176009/dopamine-and-serotonin-modulation-of-motor-and-non-motor-functions-of-the-non-human-primate-striato-pallidal-circuits-in-normal-and-pathological-states
#16
REVIEW
Véronique Sgambato-Faure, Léon Tremblay
Thanks to the non-human primate (NHP), we have shown that the pharmacological disturbance of the anterior striatum or of external globus pallidus triggers a set of motivation and movement disorders, depending on the functional subterritory involved. One can, therefore, assume that the aberrant activity of the different subterritories of basal ganglia (BG) could lead to different behavioral disorders in neuropsychiatric disorders as Tourette's syndrome and Parkinson's disease. We are now addressing in the NHP the impact of modulating dopamine or serotonin within the BG on behavioral disorders...
February 7, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28134272/transcriptomic-and-anatomic-parcellation-of-5-ht3ar-expressing-cortical-interneuron-subtypes-revealed-by-single-cell-rna-sequencing
#17
Sarah Frazer, Julien Prados, Mathieu Niquille, Christelle Cadilhac, Foivos Markopoulos, Lucia Gomez, Ugo Tomasello, Ludovic Telley, Anthony Holtmaat, Denis Jabaudon, Alexandre Dayer
Cortical GABAergic interneurons constitute a highly diverse population of inhibitory neurons that are key regulators of cortical microcircuit function. An important and heterogeneous group of cortical interneurons specifically expresses the serotonin receptor 3A (5-HT3AR) but how this diversity emerges during development is poorly understood. Here we use single-cell transcriptomics to identify gene expression patterns operating in Htr3a-GFP+ interneurons during early steps of cortical circuit assembly. We identify three main molecular types of Htr3a-GFP+ interneurons, each displaying distinct developmental dynamics of gene expression...
January 30, 2017: Nature Communications
https://www.readbyqxmd.com/read/28132813/the-fabric-of-meaning-and-subjective-effects-in-lsd-induced-states-depend-on-serotonin-2a-receptor-activation
#18
Katrin H Preller, Marcus Herdener, Thomas Pokorny, Amanda Planzer, Rainer Kraehenmann, Philipp Stämpfli, Matthias E Liechti, Erich Seifritz, Franz X Vollenweider
A core aspect of the human self is the attribution of personal relevance to everyday stimuli enabling us to experience our environment as meaningful [1]. However, abnormalities in the attribution of personal relevance to sensory experiences are also critical features of many psychiatric disorders [2, 3]. Despite their clinical relevance, the neurochemical and anatomical substrates enabling meaningful experiences are largely unknown. Therefore, we investigated the neuropharmacology of personal relevance processing in humans by combining fMRI and the administration of the mixed serotonin (5-HT) and dopamine receptor (R) agonist lysergic acid diethylamide (LSD), well known to alter the subjective meaning of percepts, with and without pretreatment with the 5-HT2AR antagonist ketanserin...
February 6, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28129702/triptans-and-migraine-advances-in-use-administration-formulation-and-development
#19
REVIEW
Amanda E Macone, Michael D Perloff
Recent triptan development has focused on new administration methods and formulations, triptan combination therapies, treatment in menstrually related migraines, and novel serotonin receptor subtype agonists (5HTf). Areas covered: Clinical triptan research related to migraine was reviewed, analyzing EMBASE and PUBMED data bases from 01/01/2011 to 06/29/2016, with a focus on clinical trials of class 1 or 2 level of evidence. There have been advances in drug combination therapies, as well as administration devices that aid in ease of use, increase efficacy, and decrease adverse reactions...
March 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28117458/a-new-serotonin-5-ht6-receptor-antagonist-with-procognitive-activity-importance-of-a-halogen-bond-interaction-to-stabilize-the-binding
#20
Juan A González-Vera, Rocío A Medina, Mar Martín-Fontecha, Angel Gonzalez, Tania de la Fuente, Henar Vázquez-Villa, Javier García-Cárceles, Joaquín Botta, Peter J McCormick, Bellinda Benhamú, Leonardo Pardo, María L López-Rodríguez
Serotonin 5-HT6 receptor has been proposed as a promising therapeutic target for cognition enhancement though the development of new antagonists is still needed to validate these molecules as a drug class for the treatment of Alzheimer's disease and other pathologies associated with memory deficiency. As part of our efforts to target the 5-HT6 receptor, new benzimidazole-based compounds have been designed and synthesized. Site-directed mutagenesis and homology models show the importance of a halogen bond interaction between a chlorine atom of the new class of 5-HT6 receptor antagonists identified herein and a backbone carbonyl group in transmembrane domain 4...
January 24, 2017: Scientific Reports
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