keyword
MENU ▼
Read by QxMD icon Read
search

Serotonin receptor 2c

keyword
https://www.readbyqxmd.com/read/29661535/synthesis-of-carbon-11-labeled-5-ht-6-r-antagonists-as-new-candidate-pet-radioligands-for-imaging-of-alzheimer-s-disease
#1
Xiaohong Wang, Fugui Dong, Caihong Miao, Wei Li, Min Wang, Mingzhang Gao, Qi-Huang Zheng, Zhidong Xu
Carbon-11-labeled serotonin (5-hydroxytryptamine) 6 receptor (5-HT6 R) antagonists, 1-[(2-bromophenyl)sulfonyl]-5-[11 C]methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole (O-[11 C]2a) and 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-[11 C]methyl-1-piperazinyl)methyl]-1H-indole (N-[11 C]2a), 5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1-(phenylsulfonyl)-1H-indole (O-[11 C]2b) and 5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1-(phenylsulfonyl)-1H-indole (N-[11 C]2b), 1-((4-isopropylphenyl)sulfonyl)-5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1H-indole (O-[11 C]2c) and 1-((4-isopropylphenyl)sulfonyl)-5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1H-indole (N-[11 C]2c), 1-((4-fluorophenyl)sulfonyl)-5-[11 C]methoxy-3-((4-methylpiperazin-1-yl)methyl)-1H-indole (O-[11 C]2d) and 1-((4-fluorophenyl)sulfonyl)-5-methoxy-3-((4-[11 C]methylpiperazin-1-yl)methyl)-1H-indole (N-[11 C]2d), were prepared from their O- or N-desmethylated precursors with [11 C]CH3 OTf through O- or N-[11 C]methylation and isolated by HPLC combined with SPE in 40-50% radiochemical yield, based on [11 C]CO2 and decay corrected to end of bombardment (EOB)...
April 7, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29621775/association-of-polymorphisms-of-serotonin-transporter-5httlpr-and-5-ht2c-receptor-genes-with-criminal-behavior-in-russian-criminal-offenders
#2
Valentina A Toshchakova, Yalda Bakhtiari, Alexander V Kulikov, Sergey I Gusev, Marina V Trofimova, Olga Yu Fedorenko, Ekaterina V Mikhalitskaya, Nina K Popova, Nikolay A Bokhan, Johannes E Hovens, Anton J M Loonen, Bob Wilffert, Svetlana A Ivanova
BACKGROUND: Human aggression is a heterogeneous behavior with biological, psychological, and social backgrounds. As the biological mechanisms that regulate aggression are components of both reward-seeking and adversity-fleeing behavior, these phenomena are difficult to disentangle into separate neurochemical processes. Nevertheless, evidence exists linking some forms of aggression to aberrant serotonergic neurotransmission. We determined possible associations between 6 serotonergic neurotransmission-related gene variants and severe criminal offenses...
April 5, 2018: Neuropsychobiology
https://www.readbyqxmd.com/read/29593537/acute-pharmacological-effects-of-2c-b-in-humans-an-observational-study
#3
Esther Papaseit, Magí Farré, Clara Pérez-Mañá, Marta Torrens, Mireia Ventura, Mitona Pujadas, Rafael de la Torre, Débora González
2,5-dimethoxy-4-bromophenethylamine (2C-B) is a psychedelic phenylethylamine derivative, structurally similar to mescaline. It is a serotonin 5-hydroxytryptamine-2A (5-HT2A ), 5-hydroxytryptamine-2B (5-HT2B ), and 5-hydroxytryptamine-2C (5-HT2C ) receptor partial agonist used recreationally as a new psychoactive substance. It has been reported that 2C-B induces mild psychedelic effects, although its acute pharmacological effects and pharmacokinetics have not yet been fully studied in humans. An observational study was conducted to assess the acute subjective and physiological effects, as well as pharmacokinetics of 2C-B...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29577069/identification-of-natural-products-as-novel-ligands-for-the-human-5-ht-2c-receptor
#4
Yao Peng, Simeng Zhao, Yiran Wu, Haijie Cao, Yueming Xu, Xiaoyan Liu, Wenqing Shui, Jianjun Cheng, Suwen Zhao, Ling Shen, Jun Ma, Ronald J Quinn, Raymond C Stevens, Guisheng Zhong, Zhi-Jie Liu
G protein-coupled receptors (GPCRs) constitute the largest human protein family with over 800 members, which are implicated in many important medical conditions. Serotonin receptors belong to the aminergic GPCR subfamily and play important roles in physiological and psychological activities. Structural biology studies have revealed the structures of many GPCRs in atomic details and provide the basis for the identification and investigation of the potential ligands, which interact with and modulate the receptors...
2018: Biophysics Reports
https://www.readbyqxmd.com/read/29572515/neuronal-differentiation-induces-snord115-expression-and-is-accompanied-by-post-transcriptional-changes-of-serotonin-receptor-2c-mrna
#5
Tomaž Bratkovič, Miha Modic, Germán Camargo Ortega, Micha Drukker, Boris Rogelj
The serotonin neurotransmitter system is widespread in the brain and implicated in modulation of neuronal responses to other neurotransmitters. Among 14 serotonin receptor subtypes, 5-HT2cR plays a pivotal role in controlling neuronal network excitability. Serotonergic activity conveyed through receptor 5-HT2cR is regulated post-transcriptionally via two mechanisms, alternative splicing and A-to-I RNA editing. Brain-specific small nucleolar RNA SNORD115 harbours a phylogenetically conserved 18-nucleotide antisense element with perfect complementarity to the region of 5ht2c primary transcript that undergoes post-transcriptional changes...
March 23, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29555337/5-ht-2c-receptors-in-the-ventral-tegmental-area-but-not-in-the-arcuate-nucleus-mediate-the-hypophagic-and-hypolocomotor-effects-of-the-selective-5-ht-2c-receptor-agonist-ar231630-in-rats
#6
Sina Faton, Jean-Pol Tassin, Flore Duranton, Didier Bagnol, Anne-Dominique Lajoix
Central serotonin systems have long been associated with the control of feeding behavior and the modulation of behavioral effects of psychostimulants. 5-HT2C receptors are present in hypothalamic centers such as the arcuate nucleus (ARC), controlling homeostatic regulation of food intake, as well as in the ventral tegmental area (VTA), a region involved in motivation aspects in multiple behaviors, including feeding. In the present study, we investigated whether the 5-HT2C receptors control amphetamine-evoked locomotor activity and regulate food consumption...
March 16, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29548885/activation-of-5-ht-2c-but-not-5-ht-1a-receptors-in-the-amygdala-enhances-fear-induced-antinociception-blockade-with-local-5-ht-2c-antagonist-or-systemic-fluoxetine
#7
Lígia Renata Rodrigues Tavares, Daniela Baptista-de-Souza, Azair Canto-de-Souza
It is well-known that the exposure of rodents to threatening environments [e.g., the open arm of the elevated-plus maze (EPM)] elicits pain inhibition. Systemic and/or intracerebral [e.g., periaqueductal gray matter, amygdala) injections of antiaversive drugs [e.g., serotonin (5-HT) ligands, selective serotonin reuptake inhibitors (SSRIs)] have been used to change EPM-open arm confinement induced antinociception (OAA). Here, we investigated (i) the role of the 5-HT1A and 5-HT2C receptors located in the amygdaloid complex on OAA as well as (ii) the effects of systemic pretreatment with fluoxetine (an SSRI) on the effects of intra-amygdala injections of 8-OH-DPAT (a 5-HT1A agonist) or MK-212 (a 5-HT2C agonist) on nociception in mice confined to the open arm or enclosed arm of the EPM...
March 13, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29523295/molecular-hypotheses-to-explain-the-shared-pathways-and-underlying-pathobiological-causes-in-catatonia-and-in-catatonic-presentations-in-neuropsychiatric-disorders
#8
E M Peter-Ross
The pathobiological causes, the shared cellular and molecular pathways in catatonia and in catatonic presentation in neuropsychiatric disorders are yet to be determined. The hypotheses in this paper have been deduced from the latest scientific research findings and clinical observations of patients with genetic disorders, behavioral phenotypes and other family members suffering mental disorders. The first hypothesis postulates that catatonia and the heterogeneity of catatonic signs and symptoms involve nucleolar dysfunction arising from abnormalities of the brain-specific, non-coding micro-RNA, SNORD115 genes (either duplications or deletions) which result in pathobiological dysfunction of various combinations in the downstream pathways (possibly along with other genes in these shared pathways)...
April 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29522726/valnoctamide-the-effect-on-relieving-of-neuropathic-pain-and-possible-mechanisms
#9
Dilara Nemutlu Samur, Rana Arslan, Sule Aydın, Nurcan Bektas
The purpose of this study is to assess the possible anti-allodynic and antihyperalgesic effect of valnoctamide, an amide derivative of valproic acid, at the doses of 40, 70 and 100 mg/kg (i.p.) in neuropathic pain model induced by chronic constriction injury in rats, by using dynamic plantar test and plantar test (Hargreaves method), and to evaluate that the possible role of certain serotonin, noradrenergic, opioid and GABAergic receptors by pre-treatment with 1 mg/kg (i.p.) ketanserin, yohimbine, naloxone and 0...
March 6, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29479825/preferential-modulation-of-the-lateral-habenula-activity-by-serotonin-2a-rather-than-2c-receptors-electrophysiological-and-neuroanatomical-evidence
#10
Francis Delicata, Cristiano Bombardi, Massimo Pierucci, Roberto Di Maio, Philippe De Deurwaerdère, Giuseppe Di Giovanni
AIMS: Serotonergic (5-HT) modulation of the lateral habenula (LHb) activity is central in normal and pathologic conditions such as mood disorders. Among the multiple 5-HT receptors (5-HTRs) involved, the 5-HT2C R seems to play a pivotal role. Yet, the role of 5-HT2A Rs in the control of the LHb neuronal activity is completely unknown. METHODS: Single-cell extracellular recording of the LHb neurons was used in rats to study the effect of the general activation and blockade of the 5-HT2C R and 5-HT2A R with Ro 60-0175 and SB242084, TCB-2 and MDL11939, respectively...
February 25, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29454752/effects-of-5-ht-2-receptor-antagonists-on-bronchoconstriction-and-pulmonary-remodeling-processes
#11
Anna Löfdahl, Christina Wenglén, Kristina Rydell-Törmänen, Gunilla Westergren-Thorsson, Anna-Karin Larsson-Callerfelt
Serotonin (5-hydroxytryptamine, 5-HT) is associated with several chronic pulmonary diseases, recognizing 5-HT2 receptor antagonists as potential inhibitors of tissue remodeling. However, the effects of 5-HT2 receptors, especially, 5-HT2B receptors on airway function and remodeling, are unclear. We investigated the role of 5-HT2B receptors on airway smooth muscle contractility and remodeling processes. Murine precision-cut lung slices were pre-treated with 5-HT2B receptor antagonists; EXT5, EXT9, RS127445, and PRX08066, as well as ketanserin (5-HT2A/2C receptor antagonist) (1 μM, 10 μM), prior to addition of cumulative concentrations of 5-HT to induce bronchoconstriction...
February 15, 2018: American Journal of Pathology
https://www.readbyqxmd.com/read/29441581/genetic-polymorphisms-of-htr2c-lep-and-lepr-on-metabolic-syndromes-in-patients-treated-with-atypical-antipsychotic-drugs
#12
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
#13
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
#14
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-HT2C R) 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 (D1 R, D2 R), 5-HT1B R and 5-HT2C R 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 (Ay /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
#15
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 5-HT2C receptor ligand SB242084 can increase motivation and have rapid onset anti-depressant-like effects. We sought to identify the specific behavioral effects of SB242084 treatment and elucidate the mechanism in female and male mice. Using a quantitative behavioral 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 DA measured during behavior...
February 28, 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
#16
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
#17
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
#18
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 decreases cocaine self-administration in rats and monkeys. Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB242084), 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...
March 2018: 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
#19
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 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 this 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
#20
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
keyword
keyword
76986
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"