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G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.
基因功能參考文獻(xiàn):
The study emphasised the potential role of 5HT2C receptor gene polymorphisms in Egyptian patients with lifelong premature ejaculation. PMID: 28730747
No differences were found between murderers and thieves either concerning 5HTTLPR and 5-HT2C genotypes or concerning psychological measures. Comparison of polymorphism distribution between groups of prisoners and controls revealed highly significant associations of 5HTTLPR and 5-HTR2C (rs6318) gene polymorphisms with being convicted for criminal behavior. PMID: 29621775
Genetic variants in HTR2C are involved in the susceptibility to metabolic syndrome in patients treated with atypical antipsychotics. PMID: 29441581
The presence of the G allele of rs6318 of the HTR2C gene was found to be associated with characteristics of aggressive behavior and social problems, and aggressive behavior was found to be associated with heterozygosis in females. PMID: 29924134
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. Our findings suggest that the rs6318 (Cys23Ser) polymorphism is not associated with suicidal behavior. PMID: 29049139
The constitutive activity of 5HT2C is decreased by pre-mRNA editing as well as alternative pre-mRNA splicing, which generates a truncated isoform that switches off 5HT2C receptor activity through heterodimerization; showing that RNA processing regulates the constitutive activity of the 5HT2C system. PMID: 28664341
The results suggest that region-specific changes in RNA editing of 5-HT2CR mRNA and deficient receptor function likely contribute to the etiology of major depressive disorder or suicide. PMID: 27576167
Therefore, the 5-HT2C gene polymorphism rs3813929 (more specifically, the TT genotype) predicted greater %EWL 12 months after RYGB surgery among female patients. PMID: 27554131
findings indicate that polymorphisms rs3813929 and rs1800849 from 5-HT2C and UCP3 genes were related to type 2 diabetes mellitus prevalence among the Brazilian obese women candidates for bariatric surgery. PMID: 28977211
A significant association was established between various HTR2C polymorphisms and Hyperprolactinaemia (HPRL). The study revealed an association between HPRL and X-chromosome haplotypes comprised of the rs569959 and rs17326429 polymorphisms. PMID: 27654063
C-carriers showed blunted rather than exaggerated cortisol responses to lab-induced stress in multilevel models (b=0.467, p<0.001), which persisted when covarying subclinical depressive symptoms. This effect was not moderated by sex. Results support a role for the rs6318 C-allele in dysregulated stress responding, and suggest that the C-allele may contribute to risk for depression. PMID: 26787298
We examined cortisol reactivity to a social evaluative stressor in the laboratory. The HTR2C Cys23 allele was associated with greater cortisol reactivity. The consistency of the results across the two sites in this paper as well as the additional site in the companion paper (total N = 426) provides strong support for an association of the Cys23Ser polymorphism with cortisol reactivity in the Trier Social Stress Test. PMID: 27211696
Authors found that 22 patients presented the -759C/T polymorphism in 5-HTR2C gene. PMID: 28174802
This study demonstrated that -759C>T Polymorphism of the HTR2C Gene is Associated with Second Generation Antipsychotic-Induced Weight Gain in Female Patients with Schizophrenia. PMID: 27414739
the occurrence of hyperprolactinemia, although asymptomatic, was higher in the presence of the C allele of the rs6318 SNP of the HTR2C gene. PMID: 26682995
SLC6A14 and 5-HTR2C polymorphisms are associated with food intake and nutritional status in children. PMID: 26160208
RNA element is discovered, which coordinates site-specific RNA editing on HTR2C pre-mRNA by an in vitro editing assay and secondary structural analysis of mutant HTR2C RNA fragments. PMID: 26259820
No significant differences were found between the genotype distribution and allele frequencies of the OSAHS group and the control group regarding the T102C polymorphisms of the 5-HTR 2A gene and the G796C polymorphisms of the 5-HTR 2C gene. PMID: 23494654
Study demonstrates that the GHS-R1a/5-HT2C receptor interaction translates into a biologically significant modulation of ghrelin's orexigenic effect PMID: 25727097
Results of the present study do not support a major role of SNPs of HTR2C rs1414334 in the regulation of weight gain or association of serum levels in patients with schizophrenia on clozapine treatment. PMID: 25284335
ADARB1 rs9983925 and rs4819035 and HTR2C rs6318 were associated with suicide attempt risk. PMID: 25732952
A functional SNP on the HTR2C gene may confer an increased risk for depressive symptoms in White women with a history of significant life stress. PMID: 25514629
Activation of 5-HT2C receptor promotes neprilysin expression in glioma cells. PMID: 25452160
These findings validate our initial observation of association between functional nonsynonymous single nucleotide polymorphism rs6318 on the HTR2C gene and cortisol response to an acute stressor, and extend the results to include females. PMID: 25457638
found the lack of an association between 5-HT2C Cys/Ser variants and the risk of bipolar I disorder in Kurds population. PMID: 25596490
It plays a role in the RNA universe for editing, variant, small RNA and other functional RNAs.[review] PMID: 25427431
Cys23Ser 5-HT2C receptor gene polymorphism is associated with intravaginal ejaculation latency time in men with lifelong premature ejaculation. Men with Cys/Cys genotype have shorter IELTs than men with Ser/Ser genotypes. PMID: 24799636
treatment with chemically distinct 5-HT2C receptor antagonists resulted in a time-dependent change in the quaternary organization to one in which there was a preponderance of receptor monomers. PMID: 25825490
cross-talk mediated via physical association of melatonin MT2 and 5-HT2C receptors into functional heteromers PMID: 25770211
In the case of the HTR2C-759C/T polymorphism, we found a trend in which T alleles were more prevalent in male patients with up to 7% increase in BMI than in those with a greater than 7% increase in BMI PMID: 25304226
The association between HTR2C and Machiavellianism was retained if the anxiety level was taken into account. The results suggest a pleiotropic effect of HTR2Con anxiety and Machiavellianism. PMID: 25966590
This study will describe the association between the HTR2C gene and suicidal behaviour PMID: 25190618
demonstrate the homodimeric structure of 5-HT2C receptors endogenously expressed in their native cellular environment, and identifies the homodimer as a functional signaling unit. PMID: 25609374
Cocaine-dependent subjects carrying a SNP in the HTR2C gene (Ser23 variant) exhibit significantly higher attentional bias to cocaine cues in the cocaine-word Stroop task than those carrying the Cys23 variant. PMID: 24618688
no significant interactions were found between the investigated polymorphisms within the serotonergic and LEP systems in patients without antipsychotic drugs. PMID: 24525657
Data indicate that the five analyzed aminoacidic variants of serotonin 5HT(2C) receptor observing alterations in the interactions between ligands and receptor which give rise to changes of free energy values for every complex considered. PMID: 24562856
adverse drug reactions were significantly associated with variation in the gene encoding the serotonin 2C receptor PMID: 24414086
A functional polymorphism of the 5HTR2C gene is associated with increased risk for cardiovascular disease mortality and morbidity. PMID: 24386118
Greater 5-HT2CR editing found in suicide and MDD. PMID: 22404657
non-coding RNA MBII-52 and MBII-85 increase expression of the serotonin receptor 2C 5' UTR and influence expression of the hosted miRNAs PMID: 23494383
5-HT2AR, 5-HT2BR, and 5-HT2CR expression in HEK293A cells significantly increases susceptibility to JCPyV infection. PMID: 24089568
this study suggests that carriership of the j759 T allele of the HTR2C gene in females may be protective against development of parkinsonism in elderly patients during treatment with haloperidol PMID: 23609402
Genetic variation in HTR2C receptors appears to be involved in the pathogenesis of post-stroke depression in Chinese males. PMID: 23765961
This suggests that PI3K/AKT signaling contributes to both metabolic and cognitive activities. PMID: 23375407
used the most updated and assessed bioinformatic tools to predict which variations can give rise to biological effects among 2450 HTR2C SNPs; suggest 48 SNPs worth considering in future association studies in psychiatry, psychology and pharmacogenomics PMID: 21717509
This review summarizes the association of 5-HT2C missense substitutions and 6 other genes implicated in behavioral and psychological symptoms of dementia in the majority of Alzheimer's disease patients. PMID: 22414959
we report convergent cellular and behavioral data that the interaction between the 5-HT(2C)R and PTEN serves as a regulatory mechanism to control 5-HT(2C)R-mediated biology PMID: 23345234
this study extends the evidence for a protective effect of the HTR2C 759 T allele in developing obesity that is independent of the use of antipsychotic drugs. PMID: 22926610
There was a unique profound increase in 5-HT2C receptor exclusively in natural killer cells in Alzheimer's disease. The disease-specific expression of 5-HT2C, as well as the natural killer cell cyto-toxicity, has been linked with cognitive derangement. PMID: 22766135
Three HTR2C SNPs in strong linkage disequilibrium, rs6318, rs2497538, and rs1414334, were associated with greater weight gain in women but not in men. PMID: 22967772