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Serotonin receptor 2c

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https://www.readbyqxmd.com/read/28343185/frameworking-memory-and-serotonergic-markers
#1
Alfredo Meneses
The evidence for neural markers and memory is continuously being revised, and as evidence continues to accumulate, herein, we frame earlier and new evidence. Hence, in this work, the aim is to provide an appropriate conceptual framework of serotonergic markers associated with neural activity and memory. Serotonin (5-hydroxytryptamine [5-HT]) has multiple pharmacological tools, well-characterized downstream signaling in mammals' species, and established 5-HT neural markers showing new insights about memory functions and dysfunctions, including receptors (5-HT1A/1B/1D, 5-HT2A/2B/2C, and 5-HT3-7), transporter (serotonin transporter [SERT]) and volume transmission present in brain areas involved in memory...
March 27, 2017: Reviews in the Neurosciences
https://www.readbyqxmd.com/read/28322276/identifying-fast-onset-antidepressants-using-rodent-models
#2
M J Ramaker, S C Dulawa
Depression is a leading cause of disability worldwide and a major contributor to the burden of suicide. A major limitation of classical antidepressants is that 2-4 weeks of continuous treatment is required to elicit therapeutic effects, prolonging the period of depression, disability and suicide risk. Therefore, the development of fast-onset antidepressants is crucial. Preclinical identification of fast-onset antidepressants requires animal models that can accurately predict the delay to therapeutic onset. Although several well-validated assay models exist that predict antidepressant potential, few thoroughly tested animal models exist that can detect therapeutic onset...
March 21, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28302574/the-arginine-vasotocin-and-serotonergic-systems-affect-interspecific-social-behaviour-of-client-fish-in-marine-cleaning-mutualism
#3
Zegni Triki, Redouan Bshary, Alexandra S Grutter, Albert F H Ros
Many species engage in mutualistic relationships with other species. The physiological mechanisms that affect the course of such social interactions are little understood. In the cleaning mutualism, cleaner fish Labroides dimidiatus do not always act cooperatively by eating ectoparasites, but sometimes cheat by taking bites of mucus from so-called "client" reef fish. The physiological mechanisms in these interspecific interactions, however, are little studied. Here, we focussed on three neuromodulator systems known to play important roles in intraspecific social behaviour of vertebrates to examine their role in clients' interspecific behaviour...
March 14, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28292021/antinociceptive-pharmacological-profile-of-dysphania-graveolens-in-mouse
#4
Myrna Déciga-Campos, Rachel Mata, Isabel Rivero-Cruz
This work evaluates the potential antinociceptive activity of Dysphania graveolens, traditional medicinal plant used in Mexico to treat stomach pain. A CH2Cl2-MeOH extract, infusion and essential oil from aerial parts of Dysphania graveolens were evaluated in hot plate and writhing tests in mice. The metabolites pinostrobin, pinocembrin and chrysin were isolated from the Dysphania graveolens infusion; next, they were evaluated in both nociceptive tests. To confirm the antinociceptive activity and explore the possible participation of opioid, GABA and serotonin receptors in the pharmacological mechanism, a formalin test was used...
March 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28290902/-interaction-between-personality-pain-and-genes-in-ischemic-heart-disease
#5
V E Golimbet, B A Volel, S N Enikopolov, G I Korovaytseva, F Yu Kopulov
Personality traits of the patient with ischemic heart disease (IHD) are thought to determine disease course. Their level depends on clinical presentations of IHD including the presence of cardiac pain. The aim of the study was to identify the modifying effect of genes coding for serotonin transporter (5-HTTLPR), serotonin receptor type 2A (A-1438G) and 2C (Cys23Ser) as well as brain-derived neurotrophic factor (Val66Met) on personality traits in pain and painless forms of IHD. We found interaction between pain and personality factors mediated by genetic variant...
July 2016: Kardiologiia
https://www.readbyqxmd.com/read/28275879/enhanced-expression-of-serotonin-receptor-5-hydroxytryptamine-2c-is-associated-with-increased-feather-damage-in-dongxiang-blue-shelled-layers
#6
Junfeng Yao, Xiaoliang Wang, Huangxiang Yan, Xia Cai, Min Wang, Yingying Tu, Changsuo Yang
The gene encoding the serotonin receptor 5-hydroxytraptamine 2C (HTR2C) has been implicated in behavioral phenotypes in a number of species. In previous studies, a mutation in the chicken HTR2C gene was found to be associated with feather condition, thereby suggesting a relationship between the gene and receiving feather pecking activity. The present study analyzed the chicken HTR2C gene at both the genomic make-up and expression level in Dongxiang blue-shelled layer. A significant association between the single nucleotide polymorphism (SNP) rs13640917 (C/T) and feather condition was confirmed in the Chinese local layer...
March 9, 2017: Behavior Genetics
https://www.readbyqxmd.com/read/28208011/glucosylsphingosine-activates-serotonin-receptor-2a-and-2b-implication-of-a-novel-itch-signaling-pathway
#7
Ramsha Afzal, Won-Sik Shim
Recent reports claimed that glucosylsphingosine (GS) is highly accumulated and specifically evoking itch-scratch responses in the skins of atopic dermatitis (AD) patients. However, it was unclear how GS can trigger itch-scratch responses, since there were no known molecular singling pathways revealed yet. In the present study, it was verified for the first time that GS can activate mouse serotonin receptor 2a (mHtr2a) and 2b (mHtr2b), but not 2c (mHtr2c) that are expressed in HEK293T cells. Specifically, effects of GS on all mouse serotonin receptor 2 subfamily were evaluated by calcium imaging techniques...
February 17, 2017: Biomolecules & Therapeutics
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
#8
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 nerve system. As the 5-HT2C receptor displays multiple actions on various neurotransmitter systems including glutamate, dopamine, epinephrine and -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 [11C]N-methylated arylazepine (1), [11C]WAY-163909 (2), [18F]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 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28161375/receptor-stimulated-transamidation-induces-activation-of-rac1-and-cdc42-and-the-regulation-of-dendritic-spines
#9
Zhen Mi, Tuda Si, Khushboo Kapadia, Qian Li, Nancy A Muma
Regulation of dendritic spines is an important component of synaptic function and plasticity whereas dendritic spine dysregulation is related to several psychiatric and neurological diseases. In the present study, we tested the hypothesis that serotonin (5-HT)2A/2C receptor-induced Rho family transamidation and activation regulates dendritic spine morphology and that activation of multiple types of receptors can induce transglutaminase (TGase)-catalyzed transamidation of small G proteins. We previously reported a novel 5-HT2A receptor downstream effector, TGase-catalyzed serotonylation of the small G protein Rac1 in A1A1v cells, a rat embryonic cortical cell line...
May 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28126736/rna-editing-enzyme-adar2-is-a-mediator-of-neuropathic-pain-after-peripheral-nerve-injury
#10
Hitoshi Uchida, Shinji Matsumura, Shunpei Okada, Tsutomu Suzuki, Toshiaki Minami, Seiji Ito
Transcriptional and post-translational regulations are important in peripheral nerve injury-induced neuropathic pain, but little is known about the role of post-transcriptional modification. Our objective was to determine the possible effect of adenosine deaminase acting on RNA (ADAR) enzymes, which catalyze post-transcriptional RNA editing, in tactile allodynia, a hallmark of neuropathic pain. Seven days after L5 spinal nerve transection (SNT) in adult mice, we found an increase in ADAR2 expression and a decrease in ADAR3 expression in the injured, but not in the uninjured, dorsal root ganglions (DRGs)...
January 26, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28099839/trpc5-mediates-acute-leptin-and-serotonin-effects-via-pomc-neurons
#11
Yong Gao, Ting Yao, Zhuo Deng, Jong-Woo Sohn, Jia Sun, Yiru Huang, Xingxing Kong, Kai-Jiang Yu, Rui-Tao Wang, Hong Chen, Hongbo Guo, Jianqun Yan, Kathryn A Cunningham, Yongsheng Chang, Tiemin Liu, Kevin W Williams
The molecular mechanisms underlying acute leptin and serotonin 2C receptor-induced hypophagia remain unclear. Here, we show that neuronal and pro-opiomelanocortin (Pomc)-specific loss of transient receptor potential cation 5 (TrpC5) subunits is sufficient to decrease energy expenditure and increase food intake resulting in elevated body weight. Deficiency of Trpc5 subunits in Pomc neurons is also sufficient to block the anorexigenic effects of leptin and serotonin 2C receptor (Ht2Cr) agonists. The loss of acute anorexigenic effects of these receptors is concomitant with a blunted electrophysiological response to both leptin and Ht2Cr agonists in arcuate Pomc neurons...
January 17, 2017: Cell Reports
https://www.readbyqxmd.com/read/27986974/effects-of-a-serotonin-2c-agonist-and-a-2a-antagonist-on-actigraphy-based-sleep-parameters-disrupted-by-methamphetamine-self-administration-in-rhesus-monkeys
#12
Maylen Perez Diaz, Monica L Andersen, Kenner C Rice, Leonard L Howell
Sleep disorders and substance abuse are highly comorbid and we have previously shown that methamphetamine self-administration significantly disrupts activity-based sleep parameters in rhesus monkeys. To the best of our knowledge, no study has evaluated the effectiveness of any pharmacological intervention to attenuate the effects of methamphetamine on nighttime activity under well-controlled conditions in laboratory animals. Thus, we examined the effects of a 5-HT2C receptor agonist, WAY163909, and a 5-HT2A receptor antagonist, M100907, given alone and in combination, on actigraphy-based sleep parameters disrupted by methamphetamine self-administration in non-human primates...
January 18, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27931246/increased-alternate-splicing-of-htr2c-in-a-mouse-model-for-prader-willi-syndrome-leads-disruption-of-5ht2c-receptor-mediated-appetite
#13
Alastair S Garfield, Jennifer R Davies, Luke K Burke, Hannah V Furby, Lawrence S Wilkinson, Lora K Heisler, Anthony R Isles
Alternate splicing of serotonin (5-hydroxytryptamine; 5-HT) 2C receptor (5-HT2CR) pre-RNA is negatively regulated by the small nucleolar RNA, Snord115, loss of which is observed in nearly all individuals with Prader-Willi Syndrome (PWS), a multigenic disorder characterised by hyperphagia and obesity. Given the role of the 5-HT2CR in the regulation of ingestive behaviour we investigated the pathophysiological implications of Snord115 deficiency on 5-HT2CR regulated appetite in a genotypically relevant PWS mouse model (PWS-IC)...
December 8, 2016: Molecular Brain
https://www.readbyqxmd.com/read/27926574/neural-activity-memory-and-dementias-serotonergic-markers
#14
Alfredo Meneses
Dysfunctional memory seems to be a key component of diverse dementias and other neuropsychiatric disorders; unfortunately, no effective treatment exists for this, probably because of the absence of neural biomarkers accompanying it. Diverse neurotransmission systems have been implicated in memory, including serotonin or 5-hydroxytryptamine (5-HT). There are multiple serotonergic pharmacological tools, well-characterized downstream signaling in mammals' species and neural markers providing new insights into memory functions and dysfunctions...
April 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27857126/repeated-7-day-treatment-with-the-5-ht2c-agonist-lorcaserin-or-the-5-ht2a-antagonist-pimavanserin-alone-or-in-combination-fails-to-reduce-cocaine-vs-food-choice-in-male-rhesus-monkeys
#15
Matthew L Banks, S Stevens Negus
Cocaine use disorder is a global public health problem for which there are no Food and Drug Administration-approved pharmacotherapies. Emerging preclinical evidence has implicated both serotonin (5-HT) 2C and 2A receptors as potential mechanisms for mediating serotonergic attenuation of cocaine abuse-related neurochemical and behavioral effects. Therefore, the present study aim was to determine whether repeated 7-day treatment with the 5-HT2C agonist lorcaserin (0.1-1.0 mg/kg per day, intramuscular; 0.032-0...
April 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27815511/lorcaserin-for-smoking-cessation-and-associated-weight-gain-a-randomized-12-week-clinical-trial
#16
William R Shanahan, Jed E Rose, Alan Glicklich, Scott Stubbe, Matilde Sanchez-Kam
INTRODUCTION: Lorcaserin is a selective serotonin 2C receptor agonist approved by the FDA for chronic weight management. Preclinical data suggest that it may also be effective in smoking cessation through modulation of the dopaminergic reward system. METHODS: This was a 12-week, randomized, double-blind, placebo-controlled trial conducted in 30 centers in the United States. 603 adult smokers with a Body Mass Index (BMI) of 18.5-35 kg/m(2), averaging at least 10 cigarettes/day with no period of abstinence >3 months for the past year were randomized to lorcaserin 10 mg QD, 10 mg BID or placebo; all received standardized smoking cessation counseling weekly...
November 4, 2016: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
https://www.readbyqxmd.com/read/27781135/adjunctive-brexpiprazole-in-patients-with-major-depressive-disorder-and-anxiety-symptoms-an-exploratory-study
#17
Lori L Davis, Ai Ota, Pamela Perry, Kana Tsuneyoshi, Emmanuelle Weiller, Ross A Baker
BACKGROUND: Major depressive disorder (MDD) with concurrent anxiety symptoms may signal a difficult-to-treat patient. Brexpiprazole is a serotonin-dopamine activity modulator: a partial agonist at 5-HT1A and dopamine D2 receptors at similar potency, and an antagonist at 5-HT2A and noradrenaline alpha1B/2C receptors. The objective of this Phase IIIb study was to explore effectiveness, safety, and tolerability of brexpiprazole adjunctive to antidepressant (ADT) monotherapy in patients with MDD and anxiety symptoms (NCT02013531)...
October 2016: Brain and Behavior
https://www.readbyqxmd.com/read/27726356/design-and-discovery-of-functionally-selective-serotonin-2c-5-ht2c-receptor-agonists
#18
Jianjun Cheng, John D McCorvy, Patrick M Giguere, Hu Zhu, Terry Kenakin, Bryan L Roth, Alan P Kozikowski
On the basis of the structural similarity of our previous 5-HT2C agonists with the melatonin receptor agonist tasimelteon and the putative biological cross-talk between serotonergic and melatonergic systems, a series of new (2,3-dihydro)benzofuran-based compounds were designed and synthesized. The compounds were evaluated for their selectivity toward 5-HT2A, 5-HT2B, and 5-HT2C receptors in the calcium flux assay with the ultimate goal to generate selective 5-HT2C agonists. Selected compounds were studied for their functional selectivity by comparing their transduction efficiency at the G protein signaling pathway versus β-arrestin recruitment...
November 10, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27723376/ketamine-up-regulates-a-cluster-of-intronic-mirnas-within-the-serotonin-receptor-2c-gene-by-inhibiting-glycogen-synthase-kinase-3
#19
Steven F Grieco, Dmitry Velmeshev, Marco Magistri, Hagit Eldar-Finkelman, Mohammad A Faghihi, Richard S Jope, Eleonore Beurel
OBJECTIVES: We examined mechanisms that contribute to the rapid antidepressant effect of ketamine in mice that is dependent on glycogen synthase kinase-3 (GSK3) inhibition. METHODS: We measured serotonergic (5HT)-2C-receptor (5HTR2C) cluster microRNA (miRNA) levels in mouse hippocampus after administering an antidepressant dose of ketamine (10 mg/kg) in wild-type and GSK3 knockin mice, after GSK3 inhibition with L803-mts, and in learned helpless mice. RESULTS: Ketamine up-regulated cluster miRNAs 448-3p, 764-5p, 1264-3p, 1298-5p and 1912-3p (2- to 11-fold)...
October 10, 2016: World Journal of Biological Psychiatry
https://www.readbyqxmd.com/read/27714191/asymmetric-total-synthesis-of-o-methylasparvenone-a-rare-nitrogen-free-serotonin-2c-receptor-antagonist
#20
Raphaël Lafleur-Lambert, John Boukouvalas
The first enantioselective synthesis of the fungal metabolite (+)-O-methylasparvenone was achieved in eight steps and 22% overall yield from inexpensive 3,4,5-trimethoxybenzaldehyde dimethyl acetal. Key steps include (i) early-stage asymmetric alkynylation of an aromatic aldehyde with a propiolate, (ii) intramolecular Friedel-Crafts acylation, and (iii) site-selective cleavage of an aryl methyl ether.
September 21, 2016: Organic & Biomolecular Chemistry
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