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Serotonin receptor 2c

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https://www.readbyqxmd.com/read/29441581/genetic-polymorphisms-of-htr2c-lep-and-lepr-on-metabolic-syndromes-in-patients-treated-with-atypical-antipsychotic-drugs
#1
Apichaya Puangpetch, Weerapon Unaharassamee, Napa Jiratjintana, Napatrupron Koomdee, Chonlaphat Sukasem
OBJECTIVE: Single nucleotide polymorphisms in serotonin 2C receptor (HTR2C), leptin (LEP), and leptin receptor (LEPR) genes are reportedly associated with the presence of metabolic syndrome (MS). We investigated whether HTR2C:rs518147 (-697G/C), rs12836771 (A/G), LEP: rs7799039 (-2548G/A) and LEPR:rs1137101 (668A/G) are related to MS in psychotic disorder patients treated with atypical antipsychotics. METHODS: A cross-sectional study including 200 patients was conducted; genetic polymorphisms in HTR2C (rs518147 and rs12836771), LEP (rs7799039) and LEPR (rs1137101) were genotyped...
February 13, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29401659/non-imidazole-histamine-h%C3%A2-ligands-part-vii-synthesis-in-vitro-and-in-vivo-characterization-of-5-substituted-2-thiazol-4-n-propylpiperazines
#2
Roman Guryn, Marek Staszewski, Anna Stasiak, Daniel McNaught Flores, Wiesława Agnieszka Fogel, Rob Leurs, Krzysztof Walczyński
H₃ receptors present on histaminergic and non-histaminergic neurons, act as autoreceptors or heteroreceptors controlling neurotransmitter release and synthesis. Previous, studies have found that the compound N-methyl-N-3-phenylalkyl-2-[2-(4-n-propylpiperazin-1-yl)-1,3-thiazol-5-yl]ethan-1-amine (ADS-531, 2c) exhibits high in vitro potency toward H₃ guinea pig jejunal receptors, with pA₂ = 8.27. To optimize the structure of the lead compound ADS-531, a series of 5-substituted-2-thiazol-4-n-propylpiperazines 3 were synthesized and subjected to in vitro pharmacological characterization; the alkyl chain between position 2 of the thiazole ring and the terminal secondary N-methylamino function was elongated from three to four methylene groups and the N-methylamino functionality was substituted by benzyl-, 2-phenylethyl-, and 3-phenyl-propyl- moieties...
February 3, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29397535/the-leptin-dopamine-and-serotonin-receptors-in-hypothalamic-pomc-neurons-of-normal-and-obese-rodents
#3
Irina V Romanova, Kira V Derkach, Anastasiya L Mikhrina, Ivan B Sukhov, Elena V Mikhailova, Alexander O Shpakov
The pro-opiomelanocortin (POMC)-expressing neurons of the hypothalamic arcuate nucleus (ARC) are involved in the control of food intake and metabolic processes. It is assumed that, in addition to leptin, the activity of these neurons is regulated by serotonin and dopamine, but only subtype 2C serotonin receptors (5-HT2CR) was identified earlier on the POMC-neurons. The aim of this work was a comparative study of the localization and number of leptin receptors (LepR), types 1 and 2 dopamine receptors (D1R, D2R), 5-HT1BR and 5-HT2CR on the POMC-neurons and the expression of the genes encoding them in the ARC of the normal and diet-induced obese (DIO) rodents and the agouti mice (A y /a) with the melanocortin obesity...
February 3, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29367407/an-interaction-between-serotonin-receptor-signaling-and-dopamine-enhances-goal-directed-vigor-and-persistence-in-mice
#4
Matthew R Bailey, Olivia Goldman, Estefanía P Bello, Muhammad O Chohan, Nuri Jeong, Vanessa Winiger, Eileen Chun, Elke Schipani, Abigail Kalmbach, Joseph F Cheer, Peter D Balsam, Eleanor H Simpson
The functionally selective 5HT-2C receptor ligand SB242084 can increase motivation and have rapid onset anti-depressant like effects. We sought to identify the specific behavioural effects of SB242084 treatment and elucidate the mechanism in female and male mice. Using a quantitative behavioural approach we determined that SB242084 increases the vigor and persistence of goal-directed activity across different types of physical work, particularly when work requirements are demanding. We found this influence of SB242084 on effort, rather than reward to be reflected in striatal dopamine measured during behavior...
January 24, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29364761/serotonin-2b-2c-receptors-mediate-bovine-ciliary-muscle-contraction-role-in-intraocular-pressure-regulation
#5
Sunny E Ohia, Ya Fatou Njie-Mbye, Jenaye Robinson, Leah Mitchell, Marshalyn Mckoy, Catherine A Opere, Naj A Sharif
PURPOSE: To study the pharmacological profile of the serotonin (5-hydroxytryptamine [5-HT]) receptor subtype mediating contractions in bovine isolated ciliary muscles. METHODS: Ciliary muscle strips were isolated from bovine eyeballs and mounted in organ baths containing aerated (95% O2, 5% CO2) Krebs buffer solution maintained at 37°C. Each muscle strip was attached at 1 end to a Grass Force-displacement Transducer connected to a Polyview Computer System for recording changes in isometric tension...
January 24, 2018: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29310578/a-to-i-rna-editing-in-the-rat-brain-is-age-dependent-region-specific-and-sensitive-to-environmental-stress-across-generations
#6
Hiba Zaidan, Gokul Ramaswami, Yaela N Golumbic, Noa Sher, Assaf Malik, Michal Barak, Dalia Galiani, Nava Dekel, Jin B Li, Inna Gaisler-Salomon
BACKGROUND: Adenosine-to-inosine (A-to-I) RNA editing is an epigenetic modification catalyzed by adenosine deaminases acting on RNA (ADARs), and is especially prevalent in the brain. We used the highly accurate microfluidics-based multiplex PCR sequencing (mmPCR-seq) technique to assess the effects of development and environmental stress on A-to-I editing at 146 pre-selected, conserved sites in the rat prefrontal cortex and amygdala. Furthermore, we asked whether changes in editing can be observed in offspring of stress-exposed rats...
January 8, 2018: BMC Genomics
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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