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Serotonin receptor 2c

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https://www.readbyqxmd.com/read/28821448/cognitive-impairment-and-gene-expression-alterations-in-a-rodent-model-of-binge-eating-disorder
#1
A Chawla, Z A Cordner, G Boersma, T H Moran
Binge eating disorder (BED) is defined as recurrent, distressing over-consumption of palatable food (PF) in a short time period. Clinical studies suggest that individuals with BED may have impairments in cognitive processes, executive functioning, impulse control, and decision-making, which may play a role in sustaining binge eating behavior. These clinical reports, however, are limited and often conflicting. In this study, we used a limited access rat model of binge-like behavior in order to further explore the effects of binge eating on cognition...
August 15, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28805659/the-atypical-antipsychotic-olanzapine-causes-weight-gain-by-targeting-serotonin-receptor-2c
#2
Caleb C Lord, Steven C Wyler, Rong Wan, Carlos M Castorena, Newaz Ahmed, Dias Mathew, Syann Lee, Chen Liu, Joel K Elmquist
Atypical antipsychotics such as olanzapine often induce excessive weight gain and type 2 diabetes. However, the mechanisms underlying these drug-induced metabolic perturbations remain poorly understood. Here, we used an experimental model that reproduces olanzapine-induced hyperphagia and obesity in female C57BL/6 mice. We found that olanzapine treatment acutely increased food intake, impaired glucose tolerance, and altered physical activity and energy expenditure in mice. Furthermore, olanzapine-induced hyperphagia and weight gain were blunted in mice lacking the serotonin 2C receptor (HTR2C)...
August 14, 2017: Journal of Clinical Investigation
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
#3
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/28710888/chronic-spinal-cord-injury-causes-up-regulation-of-serotonin-5-ht-2a-and-2c-receptors-in-lumbosacral-cord-motoneurons
#4
Nailong Cao, Jianshu Ni, Xiaohu Wang, Hongjian Tu, Baojun Gu, Jiemin Si, Gang Wu, Karl-Erik Andersson
OBJECTIVES: To explore if the mechanism of the voiding dysfunction caused by spinal cord injury in rats can be improved by intravenous administration of the 5-HT2A/2C receptor agonist, DOI, and discuss whether it can be ascribed to serotonin 2A and 2C receptor up-regulation in lumbosacral cord motoneurons. MATERIALS AND METHODS: Female Sprague-Dawley rats were used, which were divided into two groups (Spinal cord injury group VS Normal control group). Under urethane anesthesia, cystometry was performed to examine the variation of urodynamic parameters before and after successive intrathecal administration of various doses of DOI into the lumbosacral cord...
July 15, 2017: BJU International
https://www.readbyqxmd.com/read/28706567/25i-nboh-a-new-potent-serotonin-5-ht2a-receptor-agonist-identified-in-blotter-paper-seizures-in-brazil
#5
Luciano Chaves Arantes, Ettore Ferrari Júnior, Luciano Figueiredo de Souza, Andriele Costa Cardoso, Thaynara Lino Fernandes Alcântara, Luciano Morais Lião, Yuri Machado, Rogério Araújo Lordeiro, José Coelho Neto, Ana Flávia B Andrade
A new potent serotonin 5-HT2A receptor agonist was identified in blotter papers by several state level forensic laboratories in Brazil. The 25I-NBOH is a labile molecule, which fragments into 2C-I when analyzed by routine seized material screening gas chromatography (GC) methods. GC-mass spectrometry (MS), liquid chromatography-quadrupole time-of-flight-MS, and Fourier transform infrared and nuclear magnetic resonance analyses were performed to complete molecular characterization. Individual doses range from 300 to 1000 μg...
2017: Forensic Toxicology
https://www.readbyqxmd.com/read/28676029/cardiovascular-concern-of-5-ht2b-receptor-and-recent-vistas-in-the-development-of-its-antagonists
#6
Komal Padhariya, Richie R Bhandare, Daniel Canney, Vinay Velingkar
The serotonin 2B receptor subtype (5-HT2BR), located in central nervous system (CNS), cardiovascular system (CVS) and the gastrointestinal tract (GIT), is an important target for the treatment of migraine, obesity and irritable bowel syndrome. 5-HT2BR is necessary for the myocardial cell proliferation and differentiation at the embroyonic stage for healthy development of heart. Recently, its involvement in drug induced valvulopathy and other myocardial disorders have paved a way for selective antagonist for the treatment of cardiac disorders...
July 3, 2017: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/28664341/the-activity-of-the-serotonin-receptor-2c-is-regulated-by-alternative-splicing
#7
REVIEW
Stefan Stamm, Samuel B Gruber, Alexander G Rabchevsky, Ronald B Emeson
The central nervous system-specific serotonin receptor 2C (5HT2C) controls key physiological functions, such as food intake, anxiety, and motoneuron activity. Its deregulation is involved in depression, suicidal behavior, and spasticity, making it the target for antipsychotic drugs, appetite controlling substances, and possibly anti-spasm agents. Through alternative pre-mRNA splicing and RNA editing, the 5HT2C gene generates at least 33 mRNA isoforms encoding 25 proteins. The 5HT2C is a G-protein coupled receptor that signals through phospholipase C, influencing the expression of immediate/early genes like c-fos...
June 29, 2017: Human Genetics
https://www.readbyqxmd.com/read/28657744/discovery-of-n-substituted-2-phenylcyclopropyl-methylamines-as-functionally-selective-serotonin-2c-receptor-agonists-for-potential-use-as-antipsychotic-medications
#8
Guiping Zhang, Jianjun Cheng, John D McCorvy, Paul J Lorello, Barbara J Caldarone, Bryan L Roth, Alan P Kozikowski
A series of N-substituted (2-phenylcyclopropyl)methylamines were designed and synthesized, with the aim of finding serotonin 2C (5-HT2C)-selective agonists with a preference for Gq signaling. A number of these compounds exhibit 5-HT2C selectivity with a preference for Gq-mediated signaling compared with β-arrestin recruitment. Furthermore, the N-methyl compound (+)-15a, which displayed an EC50 of 23 nM in the calcium flux assay while showing no β-arrestin recruitment activity, is the most functionally selective 5-HT2C agonist reported to date...
July 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28636828/pharmacokinetic-drug-evaluation-of-extended-release-lorcaserin-for-the-treatment-of-obesity
#9
REVIEW
Kathryn M Hurren, Marissa W Dunham
Lorcaserin is a serotonin 2C receptor antagonist that was FDA approved in 2012. Lorcaserin is recently available as an extended-release (ER) formulation for the treatment of obesity as an adjunct to lifestyle modification. Areas covered: The pharmacokinetics, pharmacodynamics, efficacy, and safety of lorcaserin ER will be reviewed. Expert opinion: Lorcaserin ER 20mg daily provides drug exposure bioequivalent to lorcaserin immediate release (IR) 10mg twice daily. Lorcaserin IR is associated with 3.3 and 3.0% placebo-subtracted weight loss in patients without and with diabetes, respectively...
August 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28588509/behavioral-effects-of-a-novel-benzofuranyl-piperazine-serotonin-2c-receptor-agonist-suggest-a-potential-therapeutic-application-in-the-treatment-of-obsessive-compulsive-disorder
#10
Michelle M Rodriguez, Carl Overshiner, J David Leander, Xia Li, Denise Morrow, Richard G Conway, David L Nelson, Karin Briner, Jeffrey M Witkin
Selective serotonin reuptake inhibitors (SSRIs) are the only effective pharmacological treatments for obsessive-compulsive disorder (OCD). Nonetheless, their generally limited efficacy, side-effects, and delayed onset of action require improved medications for this highly prevalent disorder. Preclinical and clinical findings have suggested serotonin2C (5-HT2C) receptors as a potential drug target. Data in rats and mice are presented here on the effects of a novel 5-HT2C receptor agonist ((3S)-3-Methyl-1-[4-(trifluoromethyl)-7-benzofuranyl]-piperazine) (CPD 1) with high potency and full efficacy at 5-HT2C receptors and less potency and partial agonism at 5-HT2A and 5-HT2B receptors...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28584928/effects-of-the-serotonin-2c-receptor-agonist-way163909-on-the-abuse-related-effects-and-mesolimbic-dopamine-neurochemistry-induced-by-abused-stimulants-in-rhesus-monkeys
#11
Laís F Berro, Maylen Perez Diaz, Eric Maltbie, Leonard L Howell
RATIONALE: Accumulating evidence shows that the serotonergic system plays a major role in psychostimulant abuse through its interactions with the dopaminergic system. Studies indicate that serotonin 5-HT2C receptors are one of the main classes of receptors involved in mediating the influence of serotonin in drug abuse. OBJECTIVE: The aim of the present study was to evaluate the effects of the selective serotonin 5-HT2C receptor agonist WAY163909 on the behavioral neuropharmacology of cocaine and methamphetamine in adult rhesus macaques...
June 5, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28499663/htr2c-splice-variants-and-5ht2cr-mediated-appetite
#12
Anthony R Isles
Serotonin 2C receptor (5HT2CR) exists as different isoforms as a result of alternate splicing. A truncated variant (5HT2CR-trunc) has no canonical receptor function and yet shows robust expression levels throughout the brain. Recent work has demonstrated the biochemical role of this isoform and how altering levels of 5HT2CR-trunc leads to changes in behaviour.
May 9, 2017: Trends in Endocrinology and Metabolism: TEM
https://www.readbyqxmd.com/read/28343185/frameworking-memory-and-serotonergic-markers
#13
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...
July 26, 2017: Reviews in the Neurosciences
https://www.readbyqxmd.com/read/28322276/identifying-fast-onset-antidepressants-using-rodent-models
#14
REVIEW
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...
May 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
#15
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
#16
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...
May 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28290902/-interaction-between-personality-pain-and-genes-in-ischemic-heart-disease
#17
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
#18
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
#19
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
#20
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
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