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Serotonin Receptor C/C 5HT2C

Julia Brill, Zuoyi Shao, Adam C Puche, Matt Wachowiak, Michael T Shipley
Serotoninergic fibers densely innervate olfactory bulb glomeruli, the first sites of synaptic integration in the olfactory system. Acting through 5HT2A receptors, serotonin (5HT) directly excites external tufted cells (ETCs), key excitatory glomerular neurons, and depolarizes some mitral cells (MCs), the olfactory bulb's main output neurons. We further investigated 5HT action on MCs and determined its effects on the two major classes of glomerular interneurons: GABAergic/dopaminergic short axon cells (SACs) and GABAergic periglomerular cells (PGCs)...
March 2016: Journal of Neurophysiology
María Teresa Rivera-García, Carolina López-Rubalcava, Silvia L Cruz
RATIONALE: Toluene is a misused inhalant with hallucinogenic properties and complex effects. Toluene blocks N-methyl-D-aspartate (NMDA) receptors, releases dopamine (DA), and modifies several neurotransmitter levels; nonetheless, the mechanism by which it produces hallucinations is not well characterized. OBJECTIVES: This study aims (a) to study toluene's effects on the 5-HT2A-mediated head-twitch response (HTR), dopamine (DA), and serotonin (5-HT) tissue levels in discrete brain regions; (b) to compare the actions of toluene, ketamine, and 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI) on HTR; and (c) to study the pharmacological blockade of toluene's and ketamine's effects by selective drugs...
October 2015: Psychopharmacology
L M Kozhevnikova, M V Mesitov, A A Moskovtsev
We investigated the role of 5HT2C receptors in regulation of blood vessel contractility. We determined expression of 5HT2C receptors in smooth muscle cell line A7r5 as well as on isolated rat aorta. It was shown that strong vasoconstriction effect of 5HT2C receptor agonists - SCH 23390 and MK 212 appeared on blood vessels after preliminary activation of angiotensin ATIA- and vasopressin V1A-receptors. Biphasic contraction (a rhythmic alternation of contraction and subsequent relaxation phases of aoitic rings) and tonic contraction were observed in 75% and 25% of the cases after 5HT2C receptor activation, respectively...
October 2014: Patologicheskaia Fiziologiia i èksperimental'naia Terapiia
L M Kozhevnikova, A A Moskovtsev, M V Mesitov
We found that the inhibitor of Rho-kinase fasudil selectively inhibited constriction of isolated rings of the aorta and mesenteric artery in rats in response to application of the agonists of 5HT2A-(DOI and TBC-2) and 5HT1A-receptors (8-OH-DPAT) and did not influence vasoconstriction induced by serotonin. We demonstrate for the first time that application of the agonists of 5HT2C-receptors (MK 212 and SCH 23390) did not influence the tone of "intact" vessels. The marked vasoconstrictory effect of the agonists of 5HT2C-receptors was observed in the vessels preconstricted due to angiotensin II or vasopressin...
September 2014: Izvestiia Akademii Nauk. Seriia Biologicheskaia
N V Kost, V K Meshavkin, E Yu Khashaba, O Yu Sokolov, M E Voevodina, Yu A Zolotarev, L A Andreeva, N F Myasoedov
Neurotensin-like peptides acting as functional antagonists of serotonin receptors were revealed in the head-shaking test on mice. The neurotensin-like peptides block the serotonin-induced platelet aggregation in humans. Radioligand binding assay showed that neurotensin-like peptides modulate specifi c binding of 5НТ2 serotonin receptor antagonist ketanserin, but have no effect on binding of ligands of 5HT2c receptor mesulergine and 5HT1а receptors NAN-190. Similar effects of neurotensin-like peptides in the experiments in vivo and in vitro suggest that the mechanisms of the detected antipsychotic effect of the peptides can be mediated by serotonin receptors...
October 2014: Bulletin of Experimental Biology and Medicine
Vanessa Cousins, Jed E Rose, Edward D Levin
Tobacco smoking is characterized by repeated self-administration of nicotine by placing the cigarette in the mouth. The repeated hand-to-mouth self-administration is essentially a consummatory act. We recently developed a paradigm in which rats lick one of two spouts to trigger intravenous (IV) delivery of nicotine, which combines a consummatory act with rapid delivery of nicotine to model the act of tobacco smoking. We have found that rats will lick hundreds of times per nicotine infusion. In the current study, using the operant licking nicotine self-administration model with young adult Sprague-Dawley rats (0...
October 3, 2014: Progress in Neuro-psychopharmacology & Biological Psychiatry
M Pardini, C Cordano, F Benassi, C Mattei, D Sassos, S Guida, C Serrati, A Primavera, M Amore, L Cocito, L Emberti Gialloreti
Chronic Fatigue Syndrome (CFS) represents a disabling condition characterized by persistent mental and physical fatigue, bodily discomfort and cognitive difficulties. To date the neural bases of CFS are poorly understood; however, mono-aminergic abnormalities, sleep-wake cycle changes and prefrontal dysfunctions are all thought to play a role in the development and maintenance of this condition. Here we explored in a group of 62 CFS subjects the impact on fatigue levels of agomelatine, an antidepressant with agonist activity at melatonin receptors (MT1 and MT2) and antagonist activity at serotoninergic 2C receptors (5HT2C)...
June 2014: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Ramesh Neelamegam, Tim Hellenbrand, Frederick A Schroeder, Changning Wang, Jacob M Hooker
The serotonin subtype 2C (5HT2C) receptor is an emerging and promising drug target to treat several disorders of the human central nervous system. In this current report, two potent and selective 5HT2C full agonists, WAY-163909 (2) and vabicaserin (3), were radiolabeled with carbon-11 via Pictet-Spengler cyclization with [(11)C]formaldehyde and used in positron emission tomography (PET) imaging. Reaction conditions were optimized to exclude the major source of isotope dilution caused by the previously unknown breakdown of N,N-dimethylformamide (DMF) to formaldehyde at high temperature under mildly acid conditions...
February 27, 2014: Journal of Medicinal Chemistry
Jorge J Pérez Maceira, María J Mancebo, Manuel Aldegunde
It is known that in fish the serotonergic system is part of the neural network that controls feeding and that a pharmacologically induced increase in the brain 5-HT inhibits food intake. However, nothing is known about the 5-HT receptors involved in this inhibitory effect. In this study, we investigated the effects of several 5-HT1 and 5-HT2 receptor agonists on food intake in rainbow trout. In the first experiment, fish were injected i.p. or i.c.v. with two 5-HT1B receptor agonists, anpirtoline (2mg/kg, i...
April 2014: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
Mirella Nardo, Plinio C Casarotto, Felipe V Gomes, Francisco S Guimarães
Cannabidiol (CBD), one of the main components of Cannabis sp., presents clinical and preclinical anxiolytic properties. Recent results using the marble-burying test (MBT) suggest that CBD can also induce anticompulsive-like effects. Meta-chloro-phenyl-piperazine (mCPP) is a nonspecific serotonergic agonist (acting mainly at 5HT1A, 5HT2C and 5HT1D receptors) reported to increase symptoms in OCD patients and block the anticompulsive-like effect of serotonin reuptake inhibitors (SRIs) in animal models. The aim of this study was to investigate the interference of CBD on mCPP effects in repetitive burying...
October 2014: Fundamental & Clinical Pharmacology
Melanie Dawn Guenette, Adria Giacca, Margaret Hahn, Celine Teo, Loretta Lam, Araba Chintoh, Tamara Arenovich, Gary Remington
Atypical antipsychotics (AAPs) are associated with several metabolic sequelae including increased risk of type 2 diabetes. Growing evidence points to a direct drug effect of these compounds on glucose homeostasis, independent of weight gain. While the responsible mechanisms have yet to be elucidated, the heterogeneous binding profiles of AAPs likely include receptors involved in glucose metabolism. This study aimed to clarify weight-gain independent mechanisms of AAP-induced alterations in insulin secretion...
May 2013: Schizophrenia Research
Janusz K Rybakowski, Piotr Czerski, Monika Dmitrzak-Weglarz, Sebastian Kliwicki, Anna Leszczynska-Rodziewicz, Agnieszka Permoda-Osip, Maria Skibinska, Aleksandra Suwalska, Aleksandra Szczepankiewicz, Joanna Hauser
A number of candidate genes for lithium prophylactic efficacy have been proposed, some of them being also associated with a predisposition to bipolar illness. The aim of the present study was to investigate a possible association between polymorphisms of 14 common genes with the quality of prophylactic lithium response in patients with bipolar mood disorder, in relation to the putative role of these genes in the pathogenesis of this disorder. Some association with lithium prophylactic efficacy was found for the polymorphisms of 5HTT, DRD1, COMT, BDNF and FYN genes, but not for 5HT2A, 5HT2C, DRD2, DRD3, DRD4, GSK-3, NTRK2, GRIN2B and MMP-9...
March 2012: Journal of Psychopharmacology
Kevin K-C Liu, Bruce A Lefker, Mark A Dombroski, Phoebe Chiang, Peter Cornelius, Terrell A Patterson, Yuan Zeng, Stephanie Santucci, Elizabeth Tomlinson, Colleen P Gibbons, Ravi Marala, Janice A Brown, Jimmy X Kong, Eunsun Lee, Wendy Werner, Zane Wenzel, Craig Giragossian, Hou Chen, Steven B Coffey
Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.
April 1, 2010: Bioorganic & Medicinal Chemistry Letters
Kevin K-C Liu, Peter Cornelius, Terrell A Patterson, Yuan Zeng, Stephanie Santucci, Elizabeth Tomlinson, Colleen Gibbons, Tristan S Maurer, Ravi Marala, Janice Brown, Jimmy X Kong, Eunsun Lee, Wendy Werner, Zane Wenzel, Chandra Vage
Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose-responsive in vivo efficacy in our pre-clinical food intake model.
January 1, 2010: Bioorganic & Medicinal Chemistry Letters
J A Henderson, C L Bethea
To further understand the role of ovarian hormones in the function of the serotonin neural system, we investigated the effects of estradiol (E), progesterone (P), and raloxifene on 5HT 1A and 2C receptor protein expression in the dorsal raphe region using Western blot analysis. Adult rhesus macaques (Macaca mulatta) were ovariectomized (Ovx) and implanted with Silastic capsules containing E or P. In the first paradigm, animals that had been Ovx for 6-16 months were treated for 1 month with E (El) or E + P (EP1) and compared to animals that were untreated and Ovx for 5 months (n = 4 per group)...
June 2008: Endocrine
K E Borgmann-Winter, N E Rawson, H-Y Wang, H Wang, M L Macdonald, M H Ozdener, K K Yee, G Gomez, J Xu, B Bryant, G Adamek, N Mirza, E Pribitkin, C-G Hahn
The olfactory epithelium constitutes the sole source of regenerating neural cells that can be obtained from a living human. As such, primary cultures derived from human olfactory epithelial biopsies can be utilized to study neurobiological characteristics of individuals under different conditions and disease states. Here, using such human cultures, we report in vitro generation of cells that exhibit a complex neuronal phenotype, encompassing receptors and signaling pathways pertinent to both olfaction and other aspects of CNS function...
January 23, 2009: Neuroscience
Sudhir C Sharma, Chamila N Rupasinghe, Rachel B Parisien, Mark R Spaller
PDZ10 is the 10th of 13 PDZ domains found within MUPP1, a cytoplasmic scaffolding protein first identified as an endogenous binding partner of serotonin receptor type 2c (5HT2c). This association, as with those of several other interacting proteins that have subsequently been identified, is mediated through the C-terminal tail of the PDZ domain partner. Using isothermal titration calorimetry (ITC), we measured the thermodynamic binding parameters [changes in Gibbs free energy (DeltaG), enthalpy (DeltaH) and entropy (TDeltaS)] of the isolated PDZ10 domain for variable-length N-acetylated peptides from the 5HT2c serotonin receptor C-terminal sequence, as well as for octapeptides of eight other putative partner proteins of PDZ10 (5HT2a, hc-kit, hTapp1, mTapp2, TARP, NG2, claudin-1, and HPV-18 E6)...
November 6, 2007: Biochemistry
Vincenzo De Luca, Daniel J Müller, Rudi Hwang, Jeffrey A Lieberman, Jan Volavka, Herbert Y Meltzer, James L Kennedy
UNLABELLED: The 5HT2C receptor (HTR2C) has been hypothesized to represent an important modulator in feeding behavior. Evidence was based on the observation that knock-out mice for the HTR2C receptor gene develop obesity and that many antipsychotics (AP) with potent HTR2C antagonism may induce weight gain in susceptible individuals. Pharmacogenetic studies focusing either on the Cys23Ser polymorphism or on the -759C/T promoter polymorphism of the X-linked HTR2C receptor gene revealed significant findings for the -759C/T polymorphism, however, no study has performed haplotype analyses for both polymorphisms...
October 2007: Human Psychopharmacology
M W Nash, K Sugden, P Huezo-Diaz, R Williamson, A Sterne, S Purcell, P C Sham, I W Craig
Evidence indicates the genetic susceptibility to depression and anxiety is both overlapping and dimensional. In the current study, a quantitative phenotype had been created from several depression and anxiety-related measures in order to index this common genetic susceptibility (G). This has been studied in 119 sibships comprising 312 individuals, selected for extreme scores on G, from a community-based sample of 34,371 individuals. In a pathway based candidate gene study, we examined five microsatellite markers located within or nearby to five serotonin system genes (5HT2C, 5HT1D, 5HT1B, TPH1, and MAOB)...
May 5, 2005: American Journal of Medical Genetics. Part B, Neuropsychiatric Genetics
Vicki L Ellingrod, Paul J Perry, John C Ringold, Brian C Lund, Kristy Bever-Stille, Frank Fleming, Timothy L Holman, Del Miller
BACKGROUND: Weight gain from atypical antipsychotic use has become a significant problem. Recent reports have liked the -759 polymorphism of the 5HT2C receptor and obesity as well as weight gain from chlorpromazine, risperidone, and clozapine. AIM: To determine associations between weight gain during olanzapine treatment and the -759C/T polymorphism of the 5HT2C receptor gene. METHODS: This study included 42 acutely ill patients with schizophrenia (DSM-IV)...
April 5, 2005: American Journal of Medical Genetics. Part B, Neuropsychiatric Genetics
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