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Serotonin receptor 2c

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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
#1
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
#2
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...
December 6, 2016: 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
#3
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/day, intramuscular; 0.032-0.1 mg/kg/h, intravenous) or the 5-HT2A inverse agonist/antagonist pimavanserin (0...
November 18, 2016: 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
#4
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
#5
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
#6
Jianjun Cheng, John D McCorvy, Patrick M Giguère, Hu Zhu, Terry Kenakin, Bryan L Roth, Alan P Kozikowski
Based on 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...
October 11, 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
#7
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
#8
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
https://www.readbyqxmd.com/read/27692638/single-and-multiple-dose-pharmacokinetics-of-a-lorcaserin-extended-release-tablet
#9
Ronald Christopher, Mike Morgan, Jim Ferry, Bhaskar Rege, Yong Tang, Allan Kristensen, William Shanahan
PURPOSE: Lorcaserin is a serotonin 2C receptor agonist indicated for chronic weight management as an adjunct to diet and exercise. The initial approved formulation is a 10-mg, immediate-release (IR) tablet for administration BID. These studies investigated the single- and multiple-dose pharmacokinetic properties of a new, recently US Food and Drug Administration-approved, extended-release, 20-mg once-daily formulation. METHODS: We performed 2 separate 2-period, 2-sequence crossover studies in 36 healthy adults: a study comparing the IR formulation to the extended-release formulation under fasting conditions and a study comparing the extended-release formulation under fed and fasted conditions...
September 27, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27679817/single-neuron-and-genetic-correlates-of-autistic-behavior-in-macaque
#10
Kyoko Yoshida, Yasuhiro Go, Itaru Kushima, Atsushi Toyoda, Asao Fujiyama, Hiroo Imai, Nobuhito Saito, Atsushi Iriki, Norio Ozaki, Masaki Isoda
Atypical neurodevelopment in autism spectrum disorder is a mystery, defying explanation despite increasing attention. We report on a Japanese macaque that spontaneously exhibited autistic traits, namely, impaired social ability as well as restricted and repetitive behaviors, along with our single-neuron and genomic analyses. Its social ability was measured in a turn-taking task, where two monkeys monitor each other's actions for adaptive behavioral planning. In its brain, the medial frontal neurons responding to others' actions, abundant in the controls, were almost nonexistent...
September 2016: Science Advances
https://www.readbyqxmd.com/read/27659698/lorcaserin-treatment-allows-for-decreased-number-needed-to-treat-for-weight-and-glycemic-parameters-in-week-12-responders-with-%C3%A2-5-weight-loss
#11
Yehuda Handelsman, Randi Fain, Zhixiao Wang, Xuan Li, Ken Fujioka, William Shanahan
OBJECTIVES: Lorcaserin is a serotonin 2C receptor agonist approved for chronic weight management. This analysis explores the number of patients needed to be treated (NNT) with lorcaserin for one more patient to achieve weight loss and glycemic goals. METHODS: This is a post hoc analysis of three Phase 3 studies in adults with and without type 2 diabetes mellitus (T2DM) treated with lorcaserin 10 mg BID or placebo. NNT is reported for patients achieving ≥5% or ≥10% weight loss, achievement of either HbA1c <5...
September 23, 2016: Postgraduate Medicine
https://www.readbyqxmd.com/read/27640338/characterization-of-the-discriminative-stimulus-effects-of-lorcaserin-in-rats
#12
Katherine M Serafine, Kenner C Rice, Charles P France
Lorcaserin is approved by the Food and Drug Administration for treating obesity and is under consideration for treating substance use disorders; it has agonist properties at serotonin (5-HT)2C receptors and might also have agonist properties at other 5-HT receptor subtypes. This study used drug discrimination to investigate the mechanism(s) of action of lorcaserin. Male Sprague-Dawley rats discriminated 0.56 mg/kg i.p. lorcaserin from saline while responding under a fixed-ratio 5 schedule for food. Lorcaserin (0...
September 2016: Journal of the Experimental Analysis of Behavior
https://www.readbyqxmd.com/read/27627785/safety-and-tolerability-review-of-lorcaserin-in-clinical-trials
#13
REVIEW
F L Greenway, W Shanahan, R Fain, T Ma, D Rubino
Lorcaserin is a novel selective serotonin 2C receptor agonist indicated by the US Food and Drug Administration for chronic weight management in adults with obesity or overweight with ≥1 comorbidity. The safety and efficacy of lorcaserin were established during two Phase III clinical trials in patients without diabetes (BLOOM and BLOSSOM) and one Phase III clinical trial in patients with type 2 diabetes (BLOOM-DM). Headache was the most common adverse event experienced by patients during all Phase III trials...
October 2016: Clinical Obesity
https://www.readbyqxmd.com/read/27616344/5-hydroxytryptamine2a-2c-receptors-of-nucleus-raphe-magnus-and-gigantocellularis-paragigantocellularis-pars-%C3%AE-reticular-nuclei-modulate-the-unconditioned-fear-induced-antinociception-evoked-by-electrical-stimulation-of-deep-layers-of-the-superior-colliculus
#14
Ricardo de Oliveira, Rithiele Cristina de Oliveira, Luiz Luciano Falconi-Sobrinho, Raimundo da Silva Soares, Norberto Cysne Coimbra
The electrical stimulation of the dorsolateral columns of the periaquedutal grey matter (dlPAG) or deep layers of the superior colliculus (dlSC) evokes defensive behaviours followed by an antinociceptive response. Monoaminergic brainstem reticular nuclei are suggested to comprise the endogenous pain modulatory system. The aim of the present work was to investigate the role played by 5-HT2 subfamily of serotonergic receptors of the nucleus raphe magnus (NRM) and the gigantocellularis/paragigantocellularis pars α reticular nuclei (Gi/PGiα) in the elaboration of instinctive fear-induced antinociception elicited by electrical stimulation of dlPAG or of dlSC...
January 1, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/27585751/activation-of-5-ht2a-2c-receptors-reduces-the-excitability-of-cultured-cortical-neurons
#15
Lingli Hu, Chunhua Liu, Minyan Dang, Bin Luo, Yiping Guo, Haitao Wang
The abundant forebrain serotonergic projections are believed to modulate the activities of cortical neurons. 5-HT2 receptor among multiple subtypes of serotonin receptors contributes to the modulation of excitability, synaptic transmissions and plasticity. In the present study, whole-cell patch-clamp recording was adopted to examine whether activation of 5-HT2A/2C receptors would have any impact on the excitability of cultured cortical neurons. We found that 2,5-Dimethoxy-4-iodoamphetamine (DOI), a selective 5-HT2A/2C receptor agonist, rapidly and reversibly depressed spontaneous action potentials mimicking the effect of serotonin...
October 6, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27576167/region-specific-alterations-of-a-to-i-rna-editing-of-serotonin-2c-receptor-in-the-cortex-of-suicides-with-major-depression
#16
D Weissmann, S van der Laan, M D Underwood, N Salvetat, L Cavarec, L Vincent, F Molina, J J Mann, V Arango, J F Pujol
Brain region-specific abnormalities in serotonergic transmission appear to underlie suicidal behavior. Alterations of RNA editing on the serotonin receptor 2C (HTR2C) pre-mRNA in the brain of suicides produce transcripts that attenuate 5-HT2CR signaling by impairing intracellular G-protein coupling and subsequent intracellular signal transduction. In brain, the distribution of RNA-editing enzymes catalyzing deamination (A-to-I modification) shows regional variation, including within the cerebral cortex. We tested the hypothesis that altered pre-mRNA 5-HT2CR receptor editing in suicide is region-specific...
2016: Translational Psychiatry
https://www.readbyqxmd.com/read/27566488/behavioral-pharmacological-and-neuroanatomical-analysis-of-serotonin-2c-receptor-agonism-on-maternal-behavior-in-rats
#17
Ruiyong Wu, Jun Gao, Shinnyi Chou, Collin Davis, Ming Li
As a highly motivated social behavior, maternal behavior in rats has been routinely used to study psychoactive drugs for clinical, neuroscience and pharmacological purposes. Recent evidence indicates that acute activation of serotonin 2C (5-HT2C) receptors causes a disruption of rat maternal behavior. The present study was designed to elucidate the behavioral, pharmacological mechanisms and neuroanatomical basis of this 5-HT2C effect. First, we replicated the finding that acute MK212 injection (2.0mg/kg, a highly selective 5-HT2C agonist) disrupts maternal behavior, especially on pup retrieval...
November 2016: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/27540314/experimental-treatment-of-antipsychotic-induced-movement-disorders
#18
REVIEW
Erum Shireen
Antipsychotic drugs are extensively prescribed for the treatment of schizophrenia and other related psychiatric disorders. These drugs produced their action by blocking dopamine (DA) receptors, and these receptors are widely present throughout the brain. Therefore, extended antipsychotic use also leads to severe extrapyramidal side effects. The short-term effects include parkinsonism and the later appearing tardive dyskinesia. Currently available treatments for these disorders are mostly symptomatic and insufficient, and are often linked with a number of detrimental side effects...
2016: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/27516377/activation-of-serotonin-2c-receptors-in-dopamine-neurons-inhibits-binge-like-eating-in-mice
#19
Pingwen Xu, Yanlin He, Xuehong Cao, Lourdes Valencia-Torres, Xiaofeng Yan, Kenji Saito, Chunmei Wang, Yongjie Yang, Antentor Hinton, Liangru Zhu, Gang Shu, Martin G Myers, Qi Wu, Qingchun Tong, Lora K Heisler, Yong Xu
BACKGROUND: Neural networks that regulate binge eating remain to be identified, and effective treatments for binge eating are limited. METHODS: We combined neuroanatomic, pharmacologic, electrophysiological, Cre-lox, and chemogenetic approaches to investigate the functions of 5-hydroxytryptamine (5-HT) 2C receptor (5-HT2CR) expressed by dopamine (DA) neurons in the regulation of binge-like eating behavior in mice. RESULTS: We showed that 5-HT stimulates DA neural activity through a 5-HT2CR-mediated mechanism, and activation of this midbrain 5-HT→DA neural circuit effectively inhibits binge-like eating behavior in mice...
June 9, 2016: Biological Psychiatry
https://www.readbyqxmd.com/read/27512006/the-inhibitory-effect-of-combination-treatment-with-leptin-and-cannabinoid-cb1-receptor-agonist-on-food-intake-and-body-weight-gain-is-mediated-by-serotonin-1b-and-2c-receptors
#20
M Wierucka-Rybak, M Wolak, M Juszczak, J Drobnik, E Bojanowska
Previous studies reported that the co-injection of leptin and cannabinoid CB1 receptor antagonists reduces food intake and body weight in rats, and this effect is more profound than that induced by these compounds individually. Additionally, serotonin mediates the effects of numerous anorectic drugs. To investigate whether serotonin interacts with leptin and endocannabinoids to affect food intake and body weight, we administered 5-hydroxytryptamine(HT)1B and 5-hydroxytryptamine(HT)2C serotonin receptor antagonists (3 mg/kg GR 127935 and 0...
June 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
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