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Serotonin receptor 2c

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https://www.readbyqxmd.com/read/29217539/inhibition-of-cocaine-and-3-4-methylenedioxypyrovalerone-mdpv-self-administration-by-lorcaserin-is-mediated-by-5-ht2c-receptors-in-rats
#1
Brenda M Gannon, Agnieszka Sulima, Kenner C Rice, Gregory T Collins
Lorcaserin is a serotonin (5-HT)2C receptor-preferring agonist approved by the US Food and Drug Administration to treat obesity. Lorcaserin has been shown to decrease cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB 242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. The goals of this study were to determine: (1) the potency and effectiveness of lorcaserin to decrease self-administration of cocaine and 3,4-methylenedioxypyrovalerone (MDPV), a common "bath salts" constituent; and (2) the receptor(s) mediating the effects of lorcaserin on cocaine and MDPV self-administration...
December 7, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29136336/effect-of-polymorphisms-on-the-pharmacokinetics-pharmacodynamics-and-safety-of-sertraline-in-healthy-volunteers
#2
Miriam Saiz-Rodríguez, Carmen Belmonte, Manuel Román, Dolores Ochoa, Dora Koller, María Talegón, María C Ovejero-Benito, Rosario López-Rodríguez, Teresa Cabaleiro, Francisco Abad-Santos
Sertraline is a selective serotonin reuptake inhibitor (SSRI) widely metabolized in the liver by cytochrome P450 (CYP) enzymes. Besides, it is a P-glycoprotein substrate. Moreover, serotonin transporters and serotonin receptors are involved in its efficacy and safety. The aim of the present study was to evaluate the role of polymorphisms of metabolizing enzymes, transporters and receptors on the pharmacokinetics, pharmacodynamics and tolerability of sertraline in healthy volunteers. Forty-six healthy volunteers (24 men and 22 women) receiving a 100-mg single oral dose of sertraline were genotyped for 17 genetic variants of CYP enzymes (CYP2B6, CYP2C9, CYP2C19, CYP2D6), ATP binding cassette subfamily B member 1 (ABCB1), Solute carrier family 6 member 4 (SLC6A4), 5-Hydroxytryptamine receptor 2A (HTR2A) and 5-Hydroxytryptamine receptor 2C (HTR2C) genes...
November 14, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29125864/psychological-stress-in-aged-female-mice-causes-acute-hypophagia-independent-of-central-serotonin-2c-receptor-activation
#3
Chinami Matsumoto, Chihiro Yamada, Chiharu Sadakane, Miwa Nahata, Tomohisa Hattori, Hiroshi Takeda
Sex differences exist in the activation of the hypothalamic-pituitary-adrenal axis following exposure to stress, and the stress response is further affected by aging. This study was conducted to elucidate the mechanism of hypophagia in aged female mice exposed to stress. Immediately after a stress load, aged female mice exhibited acute hypophagia and a rise in plasma corticosterone levels. The administration of a serotonin 2C receptor (5-HT2CR) antagonist suppressed plasma corticosterone but did not affect the reduction in food intake...
2017: PloS One
https://www.readbyqxmd.com/read/29119704/pharmacokinetics-of-rp5063-following-single-doses-to-normal-healthy-volunteers-and-multiple-doses-over-10-days-to-stable-schizophrenic-patients
#4
Marc Cantillon, Robert Ings, Laxminarayan Bhat
RP5063, a multimodal dopamine (D)-serotonin (5-HT) stabilizer, possesses high affinity for D2/3/4 and 5-HT1A/2A/2B/2C/6/7 receptors and moderate affinity for the serotonin transporter. Two phase I studies characterized the pharmacokinetics of a single dose (10 and 15 mg fasting, 15 mg fed/fasting) in healthy volunteers and multiple doses (10, 20, 50, and 100 mg fed) over 10 days in patients with stable schizophrenia. RP5063 displayed a dose-dependent Cmax at 4 to 6 h, linear dose proportionality for both Cmax and AUC, and a half-life between 40 and 71 h...
November 8, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/29119689/decreased-5-ht2cr-and-ghsr1a-interaction-in-antipsychotic-drug-induced-obesity
#5
REVIEW
X-F Huang, K Weston-Green, Y Yu
Second generation antipsychotics (SGAs), notably atypical antipsychotics including olanzapine, clozapine and risperidone, can cause weight gain and obesity side effects. Antagonism of serotonin 2c receptors (5-HT2cR) and activation of ghrelin receptor type 1a (GHSR1a) signalling have been identified as a main cause of SGA induced obesity. Here we review the pivotal regulatory role of the 5-HT2cR in ghrelin-mediated appetite signalling. The 5-HT2cR dimerizes with GHSR1a to inhibit orexigenic signalling, while 5-HT2cR antagonism reduces dimerization and increases GHSR1a-induced food intake...
November 9, 2017: Obesity Reviews: An Official Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/29049139/the-role-of-the-cys23ser-rs6318-polymorphism-of-the-htr2c-gene-in-suicidal-behavior-systematic-review-and-meta-analysis
#6
Thelma B González-Castro, Yazmín Hernandez-Diaz, Isela E Juárez-Rojop, Lilia López-Narváez, Carlos A Tovilla-Zárate, José M Rodriguez-Perez, Juan P Sánchez-de la Cruz
The polymorphisms of the serotonin receptor 2C (HTR2C) gene have been proposed to influence suicidal behavior. The aim of our study was to explore the role of the HTR2C gene variant Cys23Ser (rs6318) in the pathogenesis of suicidal behavior through a systematic review and meta-analysis. The search was performed using EBSCO and PubMed databases. To be included in the analysis, the studies had to evaluate suicidal behavior (attempted, ideation, or completed suicide). The results of the meta-analysis were expressed as odds ratios (ORs)...
December 2017: Psychiatric Genetics
https://www.readbyqxmd.com/read/29031711/lorcaserin-improves-glycemic-control-via-a-melanocortin-neurocircuit
#7
Luke K Burke, Emmanuel Ogunnowo-Bada, Teodora Georgescu, Claudia Cristiano, Pablo B Martinez de Morentin, Lourdes Valencia Torres, Giuseppe D'Agostino, Christine Riches, Nicholas Heeley, Yue Ruan, Marcelo Rubinstein, Malcolm J Low, Martin G Myers, Justin J Rochford, Mark L Evans, Lora K Heisler
OBJECTIVE: The increasing prevalence of type 2 diabetes (T2D) and associated morbidity and mortality emphasizes the need for a more complete understanding of the mechanisms mediating glucose homeostasis to accelerate the identification of new medications. Recent reports indicate that the obesity medication lorcaserin, a 5-hydroxytryptamine (5-HT, serotonin) 2C receptor (5-HT2CR) agonist, improves glycemic control in association with weight loss in obese patients with T2D. Here we evaluate whether lorcaserin has an effect on glycemia without body weight loss and how this effect is achieved...
October 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28981869/overexpression-of-neuregulin-1-type-iii-confers-hippocampal-mrna-alterations-and-schizophrenia-like-behaviors-in-mice
#8
Juan C Olaya, Carrie L Heusner, Mitsuyuki Matsumoto, Duncan Sinclair, Mari A Kondo, Tim Karl, Cynthia Shannon Weickert
Neuregulin 1 (NRG1) is a schizophrenia candidate gene whose protein product is involved in neuronal migration, survival, and synaptic plasticity via production of specific isoforms. Importantly, NRG1 type III (NRG1 III) mRNA is increased in humans inheriting a schizophrenia risk haplotype for the NRG1 gene (HapICE), and NRG1 protein levels can be elevated in schizophrenia. The nature by which NRG1 type III overexpression results in schizophrenia-like behavior and brain pathology remains unclear, therefore we constructed a transgenic mouse with Nrg1 III overexpression in forebrain neurons (CamKII kinase+)...
September 8, 2017: Schizophrenia Bulletin
https://www.readbyqxmd.com/read/28942286/antidepressant-like-effect-of-gallic-acid-in-mice-dual-involvement-of-serotonergic-and-catecholaminergic-systems
#9
Özgür Devrim Can, Nazlı Turan, Ümide Demir Özkay, Yusuf Öztürk
AIMS: This study was planned to examine the antidepressant potency of gallic acid (30 and 60mg/kg), a phenolic acid widely distributed in nature, together with its possible underlying monoaminergic mechanisms. MAIN METHODS: Antidepressant-like activity was assessed using the tail suspension (TST) and the modified forced swimming tests (MFST). Locomotor activity was evaluated in an activity cage. KEY FINDINGS: Administration of gallic acid at 60mg/kg reduced the immobility duration of mice in both the TST and MFST without any changes in the locomotor activity...
December 1, 2017: Life Sciences
https://www.readbyqxmd.com/read/28919062/progress-and-challenges-in-anti-obesity-pharmacotherapy
#10
REVIEW
Daniel H Bessesen, Luc F Van Gaal
Obesity is a serious and growing worldwide health challenge. Healthy lifestyle choices are the foundation of obesity treatment. However, weight loss can lead to physiological adaptations that promote weight regain. As a result, lifestyle treatment alone typically produces only modest weight loss that is difficult to sustain. In other metabolic diseases, pharmacotherapy is an accepted adjunct to lifestyle. Several anti-obesity drugs have been approved in the USA, European Union, Australia, and Japan including sympathomimetics, pancreatic lipase inhibitors, GABAA receptor activators, a serotonin 2C receptor agonist, opioid antagonist, dopamine-norepinephrine reuptake inhibitor, and glucagon-like peptide-1 (GLP-1) receptor agonists...
September 14, 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/28894586/a-pilot-study-on-the-impact-of-dopamine-serotonin-and-brain-derived-neurotrophic-factor-genotype-on-long-term-functional-outcomes-after-subarachnoid-hemorrhage
#11
Ansley Stanfill, Claire Simpson, Paula Sherwood, Samuel Poloyac, Elizabeth Crago, Hyungsuk Kim, Yvette Conley
OBJECTIVES: Many that survive an aneurysmal subarachnoid hemorrhage experience lasting physical disability, which might be improved by medications with effects on the dopaminergic, serotonergic, and brain-derived neurotrophic factor neurotransmitter systems. But it is not clear which patients are most likely to benefit from these therapies. The purpose of this pilot study was to explore the relationship of genetic polymorphisms in these pathways with 12-month functional outcomes after aneurysmal subarachnoid hemorrhage...
2017: SAGE Open Medicine
https://www.readbyqxmd.com/read/28890736/the-psychoactive-drug-25b-nbome-recapitulates-rhabdomyolysis-in-zebrafish-larvae
#12
Genri Kawahara, Hideyuki Maeda, Ruri Kikura-Hanajiri, Ken-Ichi Yoshida, Yukiko K Hayashi
N-Benzyl-substituted 2C class phenethylamines (NBOMes) are psychoactive designer drugs, with strong hallucinogenic and stimulant effects, even at low doses. The designer drug, 2-(4-bromo-2, 5-dimethoxyphenyl)-N-(2-methoxybenzyl) ethanamine (25B-NBOMe) is considered to be one of the most potent agonists of the serotonin-2A (5-HT2A) receptor. Recently, we reported the first lethal case of 25B-NBOMe intoxication with severe rhabdomyolysis, concluded by clinical, pathological and toxicological analyses. There are currently no good animal models that closely recapitulate serotonin receptor-dependent rhabdomyolysis...
2017: Forensic Toxicology
https://www.readbyqxmd.com/read/28821448/cognitive-impairment-and-gene-expression-alterations-in-a-rodent-model-of-binge-eating-disorder
#13
Anjali Chawla, Zachary A Cordner, Gretha Boersma, Timothy 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...
October 15, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28805659/the-atypical-antipsychotic-olanzapine-causes-weight-gain-by-targeting-serotonin-receptor-2c
#14
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)...
September 1, 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
#15
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-upregulation-of-serotonin-5-ht-2a-and-5-ht2c-receptors-in-lumbosacral-cord-motoneurons
#16
Nailong Cao, Jianshu Ni, Xiaohu Wang, Hongjian Tu, Baojun Gu, Jiemin Si, Gang Wu, Karl-Erik Andersson
OBJECTIVES: To investigate whether the voiding dysfunction caused by spinal cord injury (SCI) in rats can be improved by i.v. administration of the serotonin (5-HT)2A/2C receptor agonist 2,5-dimethoxy-4-iodophenyl-2-aminopropanehydrochloride (DOI), and to discuss whether the mechanism can be ascribed to 5-HT2A and 5-HT 2C receptor upregulation in lumbosacral cord motoneurons. MATERIALS AND METHODS: Female Sprague-Dawley rats were divided into two groups (SCI group vs normal control [NC] group)...
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
#17
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
#18
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
#19
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...
September 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
#20
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
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