HTR2A

 

HTR2A (5-hydroxytryptamine receptor 2A)

Gene description

The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR).[5] 5-HT is short for 5-hydroxy-tryptamine, which is serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect[6] on certain areas such as the visual cortex and the orbitofrontal cortex.[7]This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones.

5-HT2A may be a necessary receptor for the spread of the human polyoma virus called the JC virus.[8]

Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and classical antipsychotics. Suicidal and otherwise depressed patients have had more 5-HT2A receptors than normal patients. These findings suggest that post-synaptic 5-HT2A overdensity is involved in the pathogenesis of depression.[9]

A haplotype consisting of 4 SNPs in the HTR2A gene has been associated with risk for rheumatoid arthritis [PMID 18006541]; the 4 SNPs being:

  • rs6311
  • rs6313
  • rs1328674
  • rs6314

A SNP in the HTR2A gene, rs7997012 and another gene (GRIK4) may also influence the odds of success upon treatment with the antidepressant citalopram, potentially differently in patients of different ethnic backgrounds.[PMID 17671280]

Recommended name:

5-hydroxytryptamine receptor 2A

Short name:

5-HT-2

Alternative name(s):

5-HT-2A

Serotonin receptor 2A

Gene function

In microbial infections acts as a receptor for human JC polyomavirus/JCPyV..

Disease association

Disease
Bipolar disorder
Schizophrenia
Hyperalgesia
Obsessive-compulsive disorder
Fever
Basal Ganglia Diseases
Obesity
Hyperglycemia
Pancreatitis
Heart failure
Panic disorder
Hyperphagia
Unipolar depression
Diabetic nephropathy
Anorexia nervosa
Metabolic Diseases
Anoxia
Diabetes Mellitus, Experimental
Attention deficit hyperactivity disorder

Advanced information

The following transcription factors affect gene expression (R):

  • AP-1
  • S8
  • STAT3

Tissue specificity:

Detected in brain cortex (at protein level). Detected in blood platelets.

Gene Pathways:

  • Calcium signaling pathway
  • Neuroactive ligand-receptor interaction
  • Gap junction
  • Signal Transduction

Molecular Function:

  • 1-(4-Iodo-2,5-Dimethoxyphenyl)Propan-2-Amine Binding
  • Drug Binding
  • G-Protein Coupled Serotonin Receptor Activity
  • Neurotransmitter Receptor Activity
  • Serotonin Binding
  • Virus Receptor Activity

Biological Processes:

  • Activation Of Phospholipase C Activity
  • Adenylate Cyclase-Inhibiting G-Protein Coupled Receptor Signaling Pathway
  • Aging
  • Artery Smooth Muscle Contraction
  • Behavioral Response To Cocaine
  • Cell Death
  • Cellular Calcium Ion Homeostasis
  • Chemical Synaptic Transmission
  • Detection Of Mechanical Stimulus Involved In Sensory Perception Of Pain
  • Detection Of Temperature Stimulus Involved In Sensory Perception Of Pain
  • Memory
  • Negative Regulation Of Potassium Ion Transport
  • Negative Regulation Of Synaptic Transmission, Glutamatergic
  • Phosphatidylinositol 3-Kinase Signaling
  • Phospholipase C-Activating G-Protein Coupled Receptor Signaling Pathway
  • Phospholipase C-Activating Serotonin Receptor Signaling Pathway
  • Positive Regulation Of Cell Proliferation
  • Positive Regulation Of Erk1 And Erk2 Cascade
  • Positive Regulation Of Fat Cell Differentiation
  • Positive Regulation Of Glycolytic Process
  • Positive Regulation Of Map Kinase Activity
  • Positive Regulation Of Peptidyl-Tyrosine Phosphorylation
  • Positive Regulation Of Phosphatidylinositol Biosynthetic Process
  • Positive Regulation Of Vasoconstriction
  • Protein Localization To Cytoskeleton
  • Regulation Of Behavior
  • Regulation Of Dopamine Secretion
  • Regulation Of Hormone Secretion
  • Release Of Sequestered Calcium Ion Into Cytosol
  • Response To Drug
  • Serotonin Receptor Signaling Pathway
  • Sleep
  • Temperature Homeostasis
  • Urinary Bladder Smooth Muscle Contraction