Function
(From Uniprot) |
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 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 phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.
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| Gene References into Functions |
- Our results indicate that chlorpromazine ameliorates visceral hypersensitivity and that the 5-HT2A receptor is a potential therapeutic target for treating abdominal pain and discomfort in irritable bowel syndrome. PMID: 28750135
- Bilateral diaphragm electromyography (EMG) was performed in vagal-intact and spontaneously breathing rats before and after intravenous administration of the 5-HT2A receptor antagonist Ketanserin (1mg/kg). Intravenous ketanserin significantly attenuated ipsilateral diaphragm EMG activity in C2 spinal cord hemisection animals but had no impact on diaphragm output in uninjured animals. PMID: 28711602
- Together, these data provide evidence of a direct effect of 5-HT on adipose cells, where 5-HT suppresses lipolysis and glucose uptake, which could contribute to altered systemic lipid- and glucose metabolism. PMID: 27109474
- that 5HT2A receptors mediate 3,4-methylenedioxymethamphetamine-induced PGE2 signaling and subsequent increases in glutamate PMID: 26670377
- Study aimed at further characterizing the effects of prenatal immune activation on 5-HT2A and mGlu2/3 receptor function in male and female rat offspring PMID: 26051401
- This study showed that Serotonin-2C and -2a receptor co-expression on cells in the rat medial prefrontal cortex. PMID: 25818050
- Studied the effect of a 5-HT2A receptor antagonist on pain-related behavior, endogenous 5-hydroxytryptamine (5-HT) plasma levels, and expression of 5-HT2A receptors in dorsal root ganglia (DRGs) in a rat lumbar disc herniation model. PMID: 25584948
- Following nicotine withdrawal, 5-HT2A receptor transcript level is reduced in the ventral tegmental area. PMID: 26031442
- rats were trained in an operant conditioning task while receiving fluoxetine), tianeptine (serotonin reuptake enhancer, 10mg/kg), buspirone, risperidone (5-HT2A antagonist, 1mg/kg), ondansetron (5-HT3 antagonist, 2mg/kg) or vehicle PMID: 24949809
- 5-HT can directly activate PAFs through 5-HT2A receptor and promote fibroblasts phenotypic alterations and adventitia fibrosis depending on the signaling of the TGF-beta1/Smad3 pathway. PMID: 25185755
- Findings reveal the "therapeutic" activation of serotonin 5-HT2A in the inhibition of the compulsive drinking behaviour in HD rats. PMID: 25155310
- our findings demonstrate that low levels of serotonin, interacting with 5-HT2A receptor, are able to activate proliferative signals in the thyroid epithelial cells. PMID: 24997405
- findings do not support the hypothesis that changes in 5-HT2A R function are a vital mechanism through which uncontrollable stress contributes to stress-related pathologies such as depression; it remains to be determined whether effects of stress on 5HT2A R binding depend on nature of the stressor or on characteristics of the rat strain PMID: 24823545
- The results indicate that 5-HT1A and 5-HT2A receptors in the dorsomedial nucleus of the hypothalamus play a phasic inhibitory role upon escape expression, as previously reported in the dorsal periaqueductal gray matter PMID: 23787365
- Stress and d-amphetamine withdrawal affect prefrontal 5-HT2AR mRNA expression to a similar degree. PMID: 24287377
- The data presented here suggest that the mechanisms mediating the cannabinoid-induced upregulation of 5-HT2A receptors would be brain-region specific. PMID: 23721787
- Endogenously released 5-HT inhibits A and C fiber-evoked synaptic transmission in the rat spinal cord by the facilitation of GABA/glycine and 5-HT release via 5-HT(2A) and 5-HT(3) receptors. PMID: 23399761
- Together our data suggest that 5-HT(2A) receptors activation is involved in the regulation of distribution of cytoskeleton in the dendritic spines. PMID: 23684573
- 5-HT2A receptor antagonists can reduce the activation of hepatic stellate cells in liver cirrhotic. PMID: 23362947
- This study demonistrated taht that during their adult lives the animals with hippocampal lesions exhibit different alterations, mainly at behavioural level and in the gene expression of 5-HT(2A) receptor. PMID: 23291154
- 5-HT decreasing apoptosis through 5-HT2A receptor is involved, at least in part, in pulmonary artery remolding. PMID: 23301505
- sustained activation of CB2 receptors, which up-regulates 5-HT2A receptor signaling, enhances GRK5 expression; the phosphorylation of CB2 receptors; and the beta-arrestin 2/ERK interactions. PMID: 23592773
- Results suggest that ligands acting on HTR2A likely modulate cocaine-induced locomotion via a common mechanism to influence dopamine-dependent circuitry. PMID: 23201361
- 5-HT2A receptors seem to have a pathophysiological role in the middle cerebral artery smooth muscle. PMID: 22659115
- the increased contractile responses to 5-HT in partial bladder outlet obstruction rat bladder may be partly caused by 5-HT(2A) receptor upregulation in the detrusor smooth muscles. PMID: 23344575
- Activation of 5-HT2A receptors upregulates the function of the neuronal K-Cl cotransporter KCC2. PMID: 23248270
- Secondhand smoke exposure induces transcriptional upregulation of the 5-HT(2A), ET(B) and ET(A) receptors in rat bronchial smooth muscle cells. PMID: 22952915
- Data suggest that chronic activation of cannabinoid receptor 2 in neurons of the prefrontal cortex enhances expression of serotonin 2A receptor (5-HT2A) and dopamine D2 receptor (D2 receptor) and formation of 5-HT2A/D2 receptor complexes. PMID: 22791651
- The enhanced striatal 5HT(2A) receptors modulate the ventilatory response to hypoxia. Immediate glucose resuscitation was found to ameliorate the receptor and transporter alterations. PMID: 21683764
- 5-HT2R mediates maintaining and modulatory effect of the nociceptive response. PMID: 21186576
- This study demonstrated that a complete transection at the T10 spinal level the serotonin 2A receptor mrna was up-regulation. PMID: 22056918
- Region-specific changes in 5-HT(2A) receptor mRNA expression occur in limbic system and associated areas following chronic D-amphetamine treatment. PMID: 21420940
- Upregulation of serotonin 2A receptor underlies the development of serotonin denervation supersensitivity in spinal motoneurons following spinal injury, implicating their involvement in the pathogenesis of subsequent spasticity development. PMID: 21211552
- The 5-HT2A receptor plays a complex role in the amygdaloid complex, since it can regulate amygdaloid activity by acting on different neuronal populations. PMID: 21126512
- The mRNA and protein expressions of 5-HT2A receptor increased in excessive fatigue rats and restraint stress rats. PMID: 21600121
- A pronociceptive role is supported following 5-HT2 receptor activation, most likely through modulation of 5-HT2A receptor activity on spinal nociceptive transmission under normal conditions. PMID: 21276431
- Effects of 5-HT1 and 5-HT2 serotonin receptors on anxiety- and depression-like behavior in female rats PMID: 21598629
- Data describe the changes in 5HT(2A) receptors and its transporter in the cerebral cortex of hypoxic neonatal rats and hypoxic rats resuscitated with glucose, oxygen, and epinephrine. PMID: 20857344
- 5-HT receptors and Ca(2)+ transporting/chaperone ER proteins may participate in the activating process of hepatic stellate cells PMID: 21245988
- While normal rats can compensate for loss of 5-HT(2) receptor activity, after severe spinal cord injury rats require constitutive activity in these 5-HT(2) receptors to produce locomotion. PMID: 20861436
- Changes of exploratory activity in a novel environment induced by social isolation are associated with a decrease in mRNA expression of the Htr2a serotonin receptor genes in the midbrain and in the striatum. PMID: 20662937
- Serotonin 5-HT(2)-receptor blockade, though, does not appear to contribute to the therapeutic effect of the antipsychotic clozapine. PMID: 20811878
- Data suggest that pyridoxine in combination with insulin and A. marmelose has a role in regulation of insulin synthesis and release, through hippocampal 5-HT2A and insulin receptor function. PMID: 20868513
- Hypoxic stress increased the number of total 5HT(2A) receptors along with an up-regulation of 5HT(2A) receptor gene in cerebellum PMID: 20471502
- Serotonin 2 receptor modulation of hyperthermia, corticosterone, and hippocampal serotonin depletions following serial exposure to chronic stress and methamphetamine. PMID: 19879056
- results indicate that the upregulation of 5-HT2A receptors at least partly underlies the 5-HT denervation supersensitivity of spinal motoneurons after a complete spinal transection PMID: 20085755
- Modulation of gamma rhythms is implemented through distinct subpopulations of FSi expressing 5-HT1ARs and 5-HT2ARs. PMID: 20147548
- The effect of lysergic acid diethylamide on prepulse inhibition (PPI) is mediated by the 5-HT(2A) receptor, whereas activation of the 5-HT(2A) receptor does not appear to contribute to the effect of lisuride on PPI. PMID: 19937319
- However, activation of 5HT2 receptors diminishes the subsequent inspiratory-related excitatory neurotransmission to CVNs that is recruited during the recovery from hypoxia likely exerting an inhibitory action on inspiratory-related purinergic signaling. PMID: 19772899
- effect of thyroidectomy on the expression of mRNA in the frontal cortex PMID: 12058363
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