> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/htr2a-af531933-b067-5dbc-aea0-3a6ff026d9f3
> Record changed: 2026-10-13

# HTR2A

ENSG00000102468

Target class

GPCR

Chromosome

13

Approved drugs

49

Clinical candidates (approved and in development)

63

## Clinical evidence

**Approved drugs**

49

**Clinical candidates (approved and in development)**

63

## Druggability

**Chemical probe available**

Yes

## Names

**Other names**

- 5-HT2A

**Target name**

HTR2A

**Gene name**

5-hydroxytryptamine receptor 2A

**Gene symbol**

HTR2A

**Previous gene symbols**

- HTR2

**Protein name**

5-hydroxytryptamine receptor 2A (5-HT-2) (5-HT-2A) (Serotonin receptor 2A)

## Classification

**Gene biotype**

Protein coding

**Gene family**

5-hydroxytryptamine receptors, G protein-coupled

**Target class**

GPCR

**Target type**

Human gene

## Expression and localisation

**Tissues expressed in**

13

**Highest tissue expression**

15.53

**Tissue specificity (Gini)**

0.746

**Tissue specificity (tau)**

0.939

## Pathways and interactions

**KEGG gene identifiers**

- hsa:3356

**Protein interaction confidence**

0.861103

**Protein interaction partners**

29

### Reactome pathways (2)

- R-HSA-390666
- R-HSA-416476

## Genomic location

**End position**

46897076

**Start position**

46831546

**Chromosome**

13

**Strand**

Reverse

## Identifiers

**Ensembl gene ID**

ENSG00000102468

**HGNC ID**

HGNC:5293

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:5293)

**NCBI Gene ID**

3356

**UniProt ID**

P28223

## Cellular location

- Cell membrane
- Multi-pass membrane protein . Cell projection, dendrite . Cell projection, axon . Cytoplasmic vesicle . Membrane, caveola . Presynapse .

### Publication evidence (2)

- PubMed 28129538  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28129538/)
- PubMed 36171289  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/36171289/)

## Tissue expression

**Tissue specificity (tau)**

0.93946

**Expression inequality (Gini)**

0.745705

### Highest expression

Expression in transcripts per million

**Brain - Frontal Cortex (BA9)**

15.53

**Brain - Cortex**

8.89

**Artery - Tibial**

7.87

**Brain - Anterior cingulate cortex (BA24)**

6.03

**Artery - Coronary**

2.59

### All tissues (54)

Expression in transcripts per million

- Brain - Frontal Cortex (BA9)15.53
- Brain - Cortex8.89
- Artery - Tibial7.87
- Brain - Anterior cingulate cortex (BA24)6.03
- Artery - Coronary2.59
- Brain - Hypothalamus2.54
- Artery - Aorta2.44
- Brain - Amygdala1.67
- Brain - Nucleus accumbens (basal ganglia)1.62
- Testis1.47
- Brain - Hippocampus1.24
- Brain - Caudate (basal ganglia)1.18
- Vagina1.11
- Brain - Substantia nigra0.91
- Fallopian Tube0.79
- Uterus0.74
- Cervix - Ectocervix0.68
- Esophagus - Gastroesophageal Junction0.66
- Colon - Sigmoid0.59
- Brain - Spinal cord (cervical c-1)0.58
- Cervix - Endocervix0.58
- Adipose - Visceral (Omentum)0.5
- Esophagus - Muscularis0.38
- Adipose - Subcutaneous0.35
- Breast - Mammary Tissue0.33

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (9)

- GO:0006874  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006874)
- GO:0007208  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007208)
- GO:0007210  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007210)
- GO:0007268  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007268)
- GO:0009410  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0009410)
- GO:0010513  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0010513)
- GO:0051209  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051209)
- GO:0070374  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0070374)
- GO:0098664  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0098664)

### Cellular components (2)

- GO:0005886  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005886)
- GO:0098666  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0098666)

### Molecular functions (6)

- GO:0001587  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001587)
- GO:0004993  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0004993)
- GO:0005515  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515)
- GO:0042802  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0042802)
- GO:0051378  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051378)
- GO:0071886  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0071886)

## On-target safety

- increased pupil diameter  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased pupil diameter  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- platelet aggregation  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: platelet aggregation  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- hyperreflexia  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: hyperreflexia  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- sweating  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: sweating  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased body temperature  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased body temperature  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased memory  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: decreased memory  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- stereotypy  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: stereotypy  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased pain  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased pain  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased body temperature  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased body temperature  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- psychosis  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: psychosis  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- agitation  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: agitation  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- myoclonus  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: myoclonus  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased sleep  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: increased sleep  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased platelet aggregation  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased platelet aggregation  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased pain  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased pain  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased inflammation  
### Effects

  - Inhibition/Decrease/Downregulation: acute  
### Studies

  - preclinical: decreased inflammation  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased blood pressure  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased blood pressure  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- drug abuse/dependence  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: drug abuse/dependence  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- hypervigilance  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: hypervigilance  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- hallucinations  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: hallucinations  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased heart rate  
### Effects

  - Activation/Increase/Upregulation: acute  
### Studies

  - preclinical: increased heart rate  
### Biological samples (3)

  - nervous system
  - cardiovascular
  - blood  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)

## Off-target safety

- smooth muscle contraction  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: smooth muscle contraction  
### Biological samples (2)

  - cardiovascular system
  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- schizophrenia  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: schizophrenia  
### Biological samples (2)

  - cardiovascular system
  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- potential memory impairments  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: potential memory impairments  
### Biological samples (2)

  - cardiovascular system
  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- serotonin syndrome  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: serotonin syndrome  
### Biological samples (2)

  - cardiovascular system
  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- receptor binding  
### Studies

  - biochemical: NVS\_GPCR\_h5HT2A, is one of one assay component(s) measured or calculated from the NVS\_GPCR\_h5HT2A assay. It is designed to make measurements of radioligand binding, a form of binding reporter, as detected with scintillation counting signals by Filter-based radiodetection technology.  
### Biological samples

  - brain, tissue-based cell-free  
Evidence source  
Source: [www.epa.gov](https://www.epa.gov/chemical-research/exploring-toxcast-data-downloadable-data)
- platelet aggregation  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: platelet aggregation  
### Biological samples (2)

  - cardiovascular system
  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- hallucinations  
### Effects

  - Activation/Increase/Upregulation: general  
### Studies

  - preclinical: hallucinations  
### Biological samples (2)

  - cardiovascular system
  - central nervous system  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)

## Related records

### Trials (2,587)

- "Brexpiprazole (Rexulti™) Safety and Efficacy Among Filipino Patients (RAISE) - A Post Marketing Surveillance Program"
- "Extended" (Alternate Day) Antipsychotic Dosing
- "Olanzapine for Prevention of Chemotherapy Induced Nausea and Vomiting in Children and Adolescents Receiving Highly Emetogenic Chemotherapy (HEC)"
- 1/2-MC4R Genotype and Pediatric Antipsychotic Drug- Induced Weight Gain
- 12 Week Study of the Safety/Efficacy of Asenapine When Added to Lithium/Valproate in the Treatment of Bipolar Disorder (A7501008 / P05844 / MK-8274-017)
- 12- Week Open Label Treatment of Refractory Bipolar Depression
- 12-Month Open-Label Long-term Safety Study of TNX-102 SL Tablets in Fibromyalgia Patients
- 12-Week Open-Label Extension Study of TNX-102 SL in PTSD Patients
- 15 mg Mirtazapine Orally Disintegrating Tablets, Fasting
- 15 mg Mirtazapine Orally Disintegrating Tablets, Non-Fasting
- 15 Month Study for Adults Who Have Been Diagnosed With Schizophrenia and Incarcerated
- 18F-DOPA PET to Elucidate the Antidepressant Mechanism of Lurasidone in Bipolar Disorder
- 24-Week Open Label Extension to a Randomized, 6-Week Double Blind, Placebo Controlled Study, to Evaluate the Safety and Tolerability of Flexible Doses of Extended Release OROS® Paliperidone in the Treatment of Geriatric Subjects With Schizophrenia
- 28-30 Month Study Comparing Paliperidone Palmitate With Oral Risperidone for Treating Adults Diagnosed With Schizophrenia Within the Past 5 Years
- 3-Week Study of Asenapine, Olanzapine and Placebo for Treatment of Bipolar Mania (P07008)
- 3-week Study of Asenapine, Olanzapine and Placebo for Treatment of Bipolar Mania (P07009)
- 3-week Study to Evaluate Efficacy and Safety of Ziprasidone With Either Lithium or Divalproex in Acutely Manic Subjects
- 40 Week Extension Study Of Asenapine and Olanzapine For Bipolar Disorder (A7501007)(COMPLETED)(P05857)
- 40 Week Trial to Study the Safety of Asenapine When Added to Lithium or Valproate in the Treatment of Bipolar Disorder (A7501009)(P05786)
- 5-HT2A Agonist Psilocybin in the Treatment of Tobacco Use Disorder

### Drugs (81)

- Amisulpride Serotonin (5-HT) receptor antagonist
- [Aripiprazole](https://trialight.com/data/asset/aripiprazole-ca9997bd-e762-4bd5-ae57-3df4e68a30dd.md) Serotonin 2a (5-HT2a) receptor antagonist
- Aripiprazole lauroxil Serotonin 2a (5-HT2a) receptor antagonist
- Asenapine Serotonin 2a (5-HT2a) receptor antagonist
- Asenapine maleate Serotonin 2a (5-HT2a) receptor antagonist
- Blonanserin Serotonin 2a (5-HT2a) receptor antagonist
- Brexpiprazole Serotonin 2a (5-HT2a) receptor antagonist
- Carphenazine Serotonin 2a (5-HT2a) receptor antagonist
- Carphenazine maleate Serotonin 2a (5-HT2a) receptor antagonist
- Chlorpromazine Serotonin 2a (5-HT2a) receptor antagonist
- Chlorpromazine hydrochloride Serotonin 2a (5-HT2a) receptor antagonist
- Chlorprothixene Serotonin 2a (5-HT2a) receptor antagonist
- Clothiapine Serotonin 2 (5-HT2) receptor antagonist
- Clozapine Serotonin 2a (5-HT2a) receptor antagonist
- [Cyclobenzaprine](https://trialight.com/data/asset/cyclobenzaprine-b63a35b9-14ef-4262-8b87-59a3229076ce.md) Serotonin 2a (5-HT2a) receptor antagonist
- Cyclobenzaprine hydrochloride Serotonin 2a (5-HT2a) receptor antagonist
- Dexfenfluramine Serotonin (5-HT) receptor agonist
- Dexfenfluramine hydrochloride Serotonin (5-HT) receptor agonist
- Droperidol Serotonin 2a (5-HT2a) receptor antagonist
- Eplivanserin Serotonin 2a (5-HT2a) receptor antagonist

---

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