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Receptor, Serotonin, 5-HT2C (0):
Recent article
Receptor, Serotonin, 5-HT2C
Abstract
RNA editing by adenosine deamination is a form of epigenetic control of gene expression wherein the ADAR enzymes convert adenosine to inosine in RNA often changing the meaning of codons. The pre-mRNA for the 2c subtype of serotonin receptor (5-HT2cR) is shown here to support small molecule binding n...
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PMID: 20820662
PDF is available here.
PDF is available here.
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Abstract
The 5-HT(2C) receptor is a GPCR and is one of the 14 subtypes that constitute the serotonin receptor family. The 5-HT₂(C) receptor is exclusively expressed in the CNS where it demonstrates a wide distribution and displays high-affinity interactions with a wide variety of psychiatric medications. M...
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PMID: 20849206
PDF is available here.
PDF is available here.
Abstract
Experiments on rats showed that meta-chlorophenylpiperazine, as well as serotonin, decreases cerebral blood flow registered in internal carotid artery of narcotized animals. Therefore, this agonist of postsynaptic 5HT(2B/2C) receptors can be used for directed search of new antimigraine drugs. Tropox...
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PMID: 21086646
PDF is available here.
PDF is available here.
Psychopharmacology (211)2 2010
Abstract
We tested a range of proposed agonists, neutral antagonists, and inverse agonists with activity at 5-HT(2C) receptors in three groups of pigeons trained to discriminate saline from: 1.0 mg/kg MK212, an agonist; 0.1 mg/kg methysergide, a proposed neutral antagonist; or, 10 mg/kg mianserin, a proposed...
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PMID: 20526585
PDF is available here.
PDF is available here.
Abstract
Targeting the 5-HT(2B) receptor may be an effective antiproliferative and antifibrotic strategy for SI-NETs because it inhibits tumor microenvironment fibroblasts as well as NET cells. Fibrosis and proliferation appear to be biologically interfaced neuroendocrine neoplasia domains....
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PMID: 20564397
PDF is available here.
PDF is available here.
Abstract
To demonstrate the clinical effectiveness of an antidepressant drug requires evidence beyond short- and long-term efficacy, including a favourable adverse-effect profile and sustained treatment adherence. Under these conditions, patients should experience enhanced social and functional outcomes. The...
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PMID: 20192279
PDF is available here.
PDF is available here.
Molecular Pharmacology (77)6 2010
Abstract
We have developed an improved method for quantifying RNA editing patterns that increases sequence analysis to an average of more than 800,000 individual cDNAs per sample, substantially increasing accuracy and sensitivity. Our method is based on the serotonin 2C receptor (5-hydroxytryptamine(2C); 5HT...
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PMID: 20181818
PDF is available here.
PDF is available here.
Psychopharmacology (209)2 2010
Abstract
We conclude that the HTR to DOI in mice is strongly modulated by 5-HT(2C) receptor activity. This novel finding invites reassessment of hallucinogenic mechanisms involving 5-HT(2) receptors....
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PMID: 20165943
PDF is available here.
PDF is available here.
Abstract
The aim of the present work was an estimation of influence of chronic administration of 5-receptors antagonist--NAN-190 (0.1 mg/kg, i. p.) and 5-HT2A/2C receptors antagonist--ketanzerine (0.1 mg/kg, i. p.) for 14 days on anxiety and depressive-like behavior in the adult female rats. Model of depress...
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PMID: 20564963
PDF is available here.
PDF is available here.
Abstract
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.
201...
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PMID: 20202843
PDF is available here.
PDF is available here.
Abstract
We have developed and optimized a cellular IP(1) assay using homogeneous time-resolved fluorescence (HTRF), a fluorescence resonance energy transfer (FRET)-based technology (Cisbio; Gif sur Yvette, France). The measurement is simple to carry out without the cumbersome steps associated with radioacti...
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PMID: 19922239
PDF is available here.
PDF is available here.
Pharmacogenomics Journal (10)1 2010
Abstract
We investigated the influence of CYP1A2*1F (-163A, rs762551) and serotonergic polymorphisms on olanzapine serum concentrations and clinical outcome in a naturalistic clinical setting. Included were 124 Caucasian psychiatric inpatients treated with olanzapine for at least 4 weeks with steady-state se...
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PMID: 19636338
PDF is available here.
PDF is available here.
Abstract
We previously revealed the altered mRNA expression and RNA editing of HTR2C in the postmortem brains of patients with mental disorders. Here we examined the relationship between genetic variations and expression level or RNA editing level of HTR2C in the human brain.
We performed mut...
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PMID: 20015120
PDF is available here.
PDF is available here.
Abstract
We investigated the effects of genetic polymorphisms in the serotonin 1A, 2A, 2C, 3A, and 3B receptor, the serotonin transporter, and the cytochrome P450 2D6 (CYP2D6) genes on the occurrence of paroxetine discontinuation syndrome. A consecutive series of 56 Japanese patients who had a diagnosis of m...
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PMID: 20075642
PDF is available here.
PDF is available here.
Abstract
Serotonin 2C receptors are G protein-coupled receptors expressed by GABAergic, glutamatergic, and dopaminergic neurons. Anatomically, they are present in various brain regions, including cortical areas, hippocampus, ventral midbrain, striatum, nucleus accumbens, hypothalamus, and amy...
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PMID: 20852829
PDF is available here.
PDF is available here.
Abstract
We currently understand the mental effects of psychedelics to be caused by agonism or partial agonism of 5-HT(2A) (and possibly 5-HT(2C)) receptors, and we understand that psychedelic drugs, especially phenylalkylamines, are fairly selective for these two receptors. This manuscript is a reference wo...
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PMID: 20126400
PDF is available here.
PDF is available here.
BMC Neuroscience (11) 2010
Abstract
These results suggest a potential synergy between melatonergic and serotonergic pathways in the action of agomelatine....
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PMID: 20525261
PDF is available here.
PDF is available here.
Neuroendocrinology (91)2 2010
Abstract
No difference in body weight gained during treatment was observed between risperidone and vehicle treated rats, but plasma risperidone levels positively correlated with visceral fat mass. Risperidone treatment increased CB(1) receptor binding in the arcuate nucleus (40%), hippocampus (25-30%) and am...
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PMID: 19815998
PDF is available here.
PDF is available here.
Abstract
Our findings also suggest that 5-HT receptors are involved in the mediation of rat maternal behavior....
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PMID: 19539643
PDF is available here.
PDF is available here.
Abstract
Agomelatine (beta-methyl-6-chloromelatonin), which is structurally homologous to melatonin, is a potent agonist of melatonin MT1 and MT2 receptors as well as an antagonist of serotonin 5-HT(2C) receptors. Agomelatine appears to improve sleep without causing daytime sedation. It has not been found to...
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PMID: 19758108
PDF is available here.
PDF is available here.
Abstract
A series of 4-substituted piperazine derivatives bearing a norbornene nucleus have been prepared and their affinity for serotonin 5-HT1A, 5-HT2A and 5-HT2C receptors has been evaluated. Compounds showing the highest affinity have been selected and evaluated on dopaminergic (D1 and D2) and adrenergic...
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PMID: 19827295
PDF is available here.
PDF is available here.
Abstract
The findings are important in 2 respects. First, agomelatine is an effective and safe antidepressant continuation therapy, which confirms efficacy seen in short-term studies. Second, few early relapses were observed in the patient group switched to placebo: the survival curve for placebo separated g...
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PMID: 19689920
PDF is available here.
PDF is available here.
Abstract
European Journal of Pharmacology (615)1-3 2009
Abstract
The serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) G protein-coupled receptors signal primarily through G alpha(q) to activate phospholipase C (PLC) and formation of inositol phosphates (IP) and diacylglycerol. The human 5-HT(2C) receptor, expressed exclusively in the central nervous system, is involved...
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PMID: 19397907
PDF is available here.
PDF is available here.
Journal of Neurophysiology (102)2 2009
Abstract
We identified the types of serotonin receptors mediating vocal activation pharmacologically using a whole brain, fictive preparation. The results showed that 5-HT(2C)-like receptors are important for activation of fictive vocalizations in the sexes. 5-HT(2C) receptor agonists elicited fictive vocali...
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PMID: 19474172
PDF is available here.
PDF is available here.
Abstract
We recently found that the response of DBA/2 mice to SSRIs in the forced swim test (FST) was impaired and they also had a smaller basal and citalopram-stimulated increase in brain extracellular serotonin (5-HT) than 'responder' strains. We employed intracerebral microdialysis, FST and selective anta...
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PMID: 19123962
PDF is available here.
PDF is available here.
Neuropharmacology (57)1 2009
Abstract
We show in the present study that the purported selective 5-HT(2C) receptor antagonist, SB242,084, dose-dependently counteracts citalopram-induced inhibition of serotonin cell firing. Even though the effect of SB242,084 is significant at a dose found in vivo to also partially occupy 5-HT(2A) recepto...
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PMID: 19376075
PDF is available here.
PDF is available here.
Abstract
Bodyweight gain is a common side effect of treatment with antidepressive drugs; however, little is known about the mechanisms behind this weight gain. Genetic differences may contribute to the susceptibility for bodyweight gain during antidepressive treatment. The objective of this study was to exam...
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PMID: 19474754
PDF is available here.
PDF is available here.
Abstract
Pharmacophore modelling, docking and virtual screening have become important tool in drug discovery process. Serotonin 2C (5-HT(2C)) receptor ligands have got major attention for their therapeutic uses as antidepressant and anorectic agents. Two step pharmacophore and docking based v...
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PMID: 19464901
PDF is available here.
PDF is available here.
Abstract
A series of N-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}acetamides were synthesized as prospective novel atypical antipsychotic agents. Microwave irradiation of acetyl glycine (I) with substituted piperazines in the presence of DCC in DMF for about 3-5 min gave the titled compounds (P:1-7). All...
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PMID: 18825551
PDF is available here.
PDF is available here.
Abstract
Sustained administration of escitalopram robustly decreased the firing rate and burst activity of DA neurons. There was no difference in the mean number of spontaneously active DA neurons per tract among the 3 groups (citalopram, escitalopram, control). This inhibition was reversed by the selective...
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PMID: 19448853
PDF is available here.
PDF is available here.
Journal of Neurochemistry (109)3 2009
Abstract
These results reveal that the lack of CB(1) receptor induces a facilitation of the activity of serotonergic neurons in the DRN by altering different components of the 5-HT feedback as well as an increase in 5-HT extracellular levels in the prefrontal cortex in mice....
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PMID: 19302195
PDF is available here.
PDF is available here.
Psychiatric Genetics (19)2 2009
Abstract
Abstract
Functional activity of the brain 5-HT2A and 5-HT2C serotonin receptors and expression of 5-HT2A and 5-HT2C genes in Norway rats selectively bred for 60 generations for high level and for a lack of fear-induced aggression towards humans were studied. There were no essential differences between aggres...
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PMID: 19368306
PDF is available here.
PDF is available here.
Abstract
Serotonin 2C and 2A receptor (5-HT2C and 5-HT2A) antagonisms are hypothesized to play a role in the metabolic adverse effects induced by olanzapine and clozapine. Associations between polymorphisms in 5-HT2C and 5-HT2A receptor coding genes, HTR2C and HTR2A, with antipsychotic-induced weight gain ha...
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PMID: 19142110
PDF is available here.
PDF is available here.
Abstract
We found an association between 5-hydroxytryptamine (serotonin) receptor 2C (HTR2C) polymorphisms and the occurrence of the metabolic syndrome in patients using antipsychotics. In the current study, we set out to replicate our findings in another sample of patients and to explore in a pooled analysi...
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PMID: 19142101
PDF is available here.
PDF is available here.
Abstract
We investigated developmental changes in editing frequencies at sites A-E in the rat cerebral cortex and primary cultured cortical neurons. The editing at sites A and B increased in parallel with the rat brain development and reached a plateau of 80-100% frequency at postnatal days 1-3. Although edi...
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PMID: 19182391
PDF is available here.
PDF is available here.
Brain Research (1250) 2009
Abstract
We have performed a case-control and a family-based study with 9 polymorphisms mapped to two serotonin receptor genes (HTR1B and HTR2C) in 252 Brazilian male ASD patients of European ancestry. These analyses showed evidence of undertransmission of the HTR1B haplotypes containing alleles -161G and -2...
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PMID: 19038234
PDF is available here.
PDF is available here.
World Journal of Biological Psychiatry (10)4 Pt 2 2009
The effect of melatonergic and non-melatonergic antidepressants on sleep: weighing the alternatives.
Abstract
In DSM-IV the occurrence of disturbed sleep is one of the principal diagnostic criteria for major depressive disorder (MDD). Further, there is evidence of reciprocity between the two conditions such that, even in the absence of current depressive symptoms, disturbed sleep often predicts their develo...
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PMID: 18609422
PDF is available here.
PDF is available here.
World Journal of Biological Psychiatry (10)4 Pt 2 2009
Abstract
Since deleterious effects of m-CPP, the primary catabolic metabolite of trazodone, were last reviewed 2 years ago, research data continue to accrue showing that clinically significant levels of m-CPP (a) are generated in patients using trazodone for sleep and (b) are present 24 h a day and (c) have...
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PMID: 19384678
PDF is available here.
PDF is available here.
Neuropsychopharmacology (34)1 2009
Abstract
Abstract
Antidepressant pharmacotherapy forms the basis of management of major depressive disorder (MDD). In principle, the management of MDD should first elicit rapid relief of symptoms and then restore normal functioning and prevent relapse. It is recommended that treatment should continue for at least one...
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PMID: 19708725
PDF is available here.
PDF is available here.
Abstract
Currently available antidepressant agents such as tricyclic antidepressants (TCAs) act primarily through monoaminergic systems in the brain, and have proved to be suboptimal for the management of major depressive disorder (MDD). Such agents are also active at non-target receptor sites, contributing...
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PMID: 19708723
PDF is available here.
PDF is available here.
BMC Neuroscience (10)1 2009
Abstract
The data revealed that mRNA from the five genes investigated was detected in all brain regions and showed an overall significant difference in expression levels. Furthermore, the expression of 5-HT2C, 5-HT2A and TPH2 was found to be significantly different between the various brain regions. However,...
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PMID: 19445671
PDF is available here.
PDF is available here.
Abstract
Schizophrenia is a serious mental disorder with a challenging rational pharmacotherapy. Neurochemical transmission in the dopaminergic system, especially via D2 receptors, and related changes in postsynaptic signal transduction are very important in both the formation of schizophrenia and current ph...
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PMID: 19504368
PDF is available here.
PDF is available here.
Journal of Neurochemistry (108)2 2009
Abstract
We explored the roles of endogenous 5-HT and 5-HT(1A) and 5-HT(2C) receptors in the mechanisms by which M100907 suppresses CPP-induced release of cortical GLU and 5-HT using in vivo microdialysis. CPP raised extracellular GLU and 5-HT by about 250% and 170% respectively. The 5-HT synthesis inhibitor...
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PMID: 19046357
PDF is available here.
PDF is available here.
Abstract
We reported the expression of the 5-HT2C receptor (5-HT2C-R) in the aorta and the pulmonary artery in rats exposed to hypoxia, and examined its role in vascular smooth muscle cells. Immunochemistry, quantitative RT-PCR, and western blot were used to examine 5-HT2C-R expression. Small interfering RNA...
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PMID: 19280877
PDF is available here.
PDF is available here.
Journal of Neurochemistry (108)5 2008
Abstract
We quantified editing of 5-HT2C receptor RNA transcripts in Gαq null mice and protein levels of Gαq and Gα11 in transgenic male mice solely expressing either the non-edited (INI) or the fully edited (VGV) isoforms of the 5-HT2C receptor. Pyrosequencing of RNA isolated from amygdaloid cortex in G...
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PMID: 19154337
PDF is available here.
PDF is available here.
Abstract
A role of serotonin receptors (5-HTRs) in spinal rhythmogenesis has been proposed several years ago based mainly upon data showing that bath-applied 5-HT could elicit locomotor-like rhythms in in vitro isolated spinal cord preparations. Such a role was partially confirmed in vivo after revealing tha...
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PMID: 19019202
PDF is available here.
PDF is available here.
Journal of Neuroscience (28)48 2008
Abstract
We derived mutant mouse lines harboring a knock-in INI or VGV allele, resulting in sole expression of one of two extremely different editing isoforms 5-HT(2C)R-INI (editing blocked) or -VGV (fully edited). Although INI mice grew normally, VGV mice had a severely reduced fat mass, despite compensator...
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PMID: 19036977
PDF is available here.
PDF is available here.
Abstract
We generated mice with global 5-HT2CR deficiency (2C null) and mice with 5-HT2CRs re-expression only in pro-opiomelanocortin (POMC) neurons (2C/POMC mice). We show that 2C null mice predictably developed hyperphagia, hyperactivity, and obesity and showed attenuated responses to anorexigenic 5-HT dru...
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PMID: 19038216
PDF is available here.
PDF is available here.
Behavioural Brain Research (193)2 2008
Abstract
We recently found that the interfering peptide Tat-3L4F is able not only to disrupt the protein-protein interaction of PTEN (phosphatase and tensin homologue deleted on chromosome 10) with the serotonin 5-HT2C receptor in the rat ventral tegmental area (VTA) but also to suppress the conditioned plac...
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PMID: 18571742
PDF is available here.
PDF is available here.
Biochemical Pharmacology (76)10 2008
Abstract
We have previously characterized a mechanism of 5HT-stimulated extracellular signal-regulated kinases 1 and 2 (ERK1/2) activation via the non-RNA-edited isoform of the serotonin 5HT(2C) receptor (5HT(2C)R-INI) in a CHO cell line. We have now used CV1 cells, which endogenously express epidermal growt...
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PMID: 18812172
PDF is available here.
PDF is available here.
Behavioural Brain Research (193)1 2008
Abstract
It is well established that the serotonergic system modulates social and aggressive behaviors. This study employed field experiments to examine the effects of serotonin on male social structure and behavior in the Puerto Rican coquí frog, Eleutherodactylus coqui. This frog displays three types of m...
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PMID: 18554729
PDF is available here.
PDF is available here.
Abstract
We show that calmodulin (CaM) binds to a prototypic Ca(2+)-dependent "1-10" CaM-binding motif located in the proximal region of the 5-HT(2C) receptor C-terminus upon receptor activation by 5-HT. Mutation of this motif inhibited both beta-arrestin recruitment by 5-HT(2C) receptor and receptor-operate...
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PMID: 18768750
PDF is available here.
PDF is available here.
Abstract
We describe its effects on food intake in non-deprived C57BL/6 mice adapted to eating a palatable dessert meal each day. PAT showed a dose-related inhibition of food intake with a 50% inhibitory dose of 4.2 mg/kg. The dose-effect curve was similar to that obtained using WAY-161503. Abnormal behavior...
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PMID: 18692085
PDF is available here.
PDF is available here.
Psychopharmacology (200)4 2008
Abstract
These results inform the feasibility of monitoring 5-HT2A/2C receptor-mediated modulation of DA systems in man using PET and, more generally, demonstrate that D2 radiotracer PET imaging may be used to monitor the efficacy of new DA modulators in attenuating stimulated DA release....
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PMID: 18597077
PDF is available here.
PDF is available here.
Molecular Psychiatry (13)11 2008
Abstract
We identified 5-HT 2CR mRNA editing variations that were associated with suicide but not with the comorbid psychiatric diagnoses, and were not influenced by demographic characteristics (age and sex) and alcohol or drug use. These variations consisted of a significant increase in the pool of mRNA var...
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PMID: 17848916
PDF is available here.
PDF is available here.
Neuropharmacology (55)6 2008
Abstract
The serotonin(2C) receptor (5-HT(2C)R) is a member of the serotonin(2) family of 7-transmembrane-spanning (7-TMS) receptors, which possesses unique molecular and pharmacological properties such as constitutive activity and RNA editing. The 5-HT(2C)R is widely expressed within the central nervous syst...
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PMID: 18602407
PDF is available here.
PDF is available here.
Abstract
Ketanserin blocked hERG current (I(hERG)) in a concentration-dependent manner (IC50=0.11 microM). The drug showed an open channel blocking property, the block increasing significantly at depolarizing voltages between +10 to +60 mV. Voltage-dependence for inactivation of hERG channels was negatively...
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PMID: 18574455
PDF is available here.
PDF is available here.