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.
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 glutamatePMID: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 offspringPMID: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 vehiclePMID: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 strainPMID: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 matterPMID: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 ratsPMID: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 cellsPMID: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 cerebellumPMID: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 transectionPMID: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 cortexPMID:12058363
Detected in adult intestine, especially in mucosal epithelium, longitudinal and circular layers of muscularis externa and myenteric plexuses. Highly expressed in Paneth cells, and detected at lower levels in enterocytes (at protein level). Detected in bra