> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/htr2b-ab574243-d1a9-5885-88fa-56d8da369205
> Record changed: 2026-11-04

# HTR2B

ENSG00000135914

Target class

GPCR

Chromosome

2

Approved drugs

7

Clinical candidates (approved and in development)

10

## Clinical evidence

**Approved drugs**

7

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

10

## Druggability

**Chemical probe available**

Yes

## Names

**Target name**

HTR2B

**Gene name**

5-hydroxytryptamine receptor 2B

**Gene symbol**

HTR2B

**Protein name**

5-hydroxytryptamine receptor 2B (5-HT-2B) (5-HT2B) (Serotonin receptor 2B)

### Other names (2)

- 5-HT(2B)
- 5-HT2B

## 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**

19

**Protein localisation evidence grade**

Supported

**Highest tissue expression**

14.9

**Tissue specificity (Gini)**

0.717

**Tissue specificity (tau)**

0.876

## Pathways and interactions

**KEGG gene identifiers**

- hsa:3357

**Protein interaction confidence**

0.858

**Protein interaction partners**

19

### Reactome pathways (2)

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

## Genomic location

**End position**

231125080

**Start position**

231108230

**Chromosome**

2

**Strand**

Reverse

## Identifiers

**Ensembl gene ID**

ENSG00000135914

**HGNC ID**

HGNC:5294

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:5294)

**NCBI Gene ID**

3357

**UniProt ID**

P41595

## Cellular location

- Cell membrane
- Multi-pass membrane protein . Synapse, synaptosome .
- Nucleoplasm

### Publication evidence (8)

- PubMed 12970106  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/12970106/)
- PubMed 23519210  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23519210/)
- PubMed 23519215  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23519215/)
- PubMed 28129538  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28129538/)
- PubMed 7926008  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/7926008/)
- PubMed 8078486  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/8078486/)
- PubMed 8143856  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/8143856/)
- PubMed 24357322  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/24357322/)

## Tissue expression

**Tissue specificity (tau)**

0.875814

**Expression inequality (Gini)**

0.71657

### Highest expression

Expression in transcripts per million

**Adrenal Gland**

14.9

**Uterus**

14.58

**Cervix - Endocervix**

13.83

**Colon - Sigmoid**

9.33

**Esophagus - Muscularis**

8.93

### All tissues (54)

Expression in transcripts per million

- Adrenal Gland14.9
- Uterus14.58
- Cervix - Endocervix13.83
- Colon - Sigmoid9.33
- Esophagus - Muscularis8.93
- Cervix - Ectocervix6.26
- Esophagus - Gastroesophageal Junction5.1
- Thyroid4.63
- Fallopian Tube3.46
- Artery - Coronary3.24
- Artery - Aorta3.22
- Colon - Transverse2.78
- Heart - Atrial Appendage2.67
- Kidney - Medulla1.96
- Artery - Tibial1.58
- Kidney - Cortex1.44
- Bladder1.28
- Ovary1.12
- Vagina1.06
- Adipose - Subcutaneous0.97
- Cells - Cultured fibroblasts0.96
- Breast - Mammary Tissue0.94
- Adipose - Visceral (Omentum)0.91
- Lung0.66
- Small Intestine - Terminal Ileum0.59

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (17)

- GO:0001819  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001819)
- GO:0001938  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001938)
- GO:0006874  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006874)
- GO:0007186  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007186)
- GO:0007208  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007208)
- GO:0008284  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0008284)
- 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:0014827  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0014827)
- GO:0019722  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0019722)
- GO:0042310  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0042310)
- GO:0043123  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0043123)
- GO:0050795  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0050795)
- GO:0051209  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051209)
- GO:0070371  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0070371)
- 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 (4)

- GO:0005654  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005654)
- GO:0005737  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005737)
- 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 (5)

- GO:0001587  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001587)
- GO:0001965  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0001965)
- 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:0051378  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051378)

## On-target safety

- increased pain  
### Effects

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

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

  - nervous system
  - cardiovascular
  - gastrointestinal  
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
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- cardiac development effect leading to cardiomyopathy (based on knockout mouse data)  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - clinical: cardiac development effect leading to cardiomyopathy (based on knockout mouse data)  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- hypertension  
### Effects

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

  - clinical: hypertension  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- decreased anxiety  
### Effects

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

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

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

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

  - preclinical: pulmonary hypertension  
### Biological samples (3)

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

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

  - clinical: cardiac valvulopathy  
### Biological samples

  - cardiovascular system  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- cardiac valvulopathy  
### Effects

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

  - preclinical: cardiac valvulopathy  
### Biological samples (3)

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

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

  - preclinical: decreased gastrointestinal transit  
### Biological samples (3)

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

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: cardiovascular malformations  
### Biological samples (3)

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

## Off-target safety

- potential cardiac valvulopathy  
### Effects

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

  - preclinical: potential cardiac valvulopathy  
### Biological samples (3)

  - cardiovascular system
  - development
  - pulmonary  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- possible cardiac effects, especially during embryonic development  
### Effects

  - Inhibition/Decrease/Downregulation: developmental toxicity  
### Studies

  - preclinical: possible cardiac effects, especially during embryonic development  
### Biological samples (3)

  - cardiovascular system
  - development
  - pulmonary  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- pulmonary hypertension  
### Effects

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

  - preclinical: pulmonary hypertension  
### Biological samples (3)

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

## Related records

### Trials (1,411)

- "Brexpiprazole (Rexulti™) Safety and Efficacy Among Filipino Patients (RAISE) - A Post Marketing Surveillance Program"
- "Evaluation by Transcranial Magnetic Stimulation of the Benefit of Fluoxetine on Motor Recovery After Stroke"
- \[11C\]Yohimbine PET Study of alpha2-AR
- 12 Week Safety Trial of Flibanserin in Depressed Women Taking an SSRI or SNRI With Decreased Sexual Desire and Distress
- 15 Month Study for Adults Who Have Been Diagnosed With Schizophrenia and Incarcerated
- 16-week Comparative Effectiveness Trial of Lamotrigine vs. Fluoxetine for Bipolar Depression
- 24-week Placebo-controlled Trial of Flibanserin Once Daily in Premenopausal Women With Hypoactive Sexual Desire Disorder
- 5HT3 Antagonism and Auditory Gating in Schizophrenia
- 6-mo. Min Eff Dose of Flibanserin: 25 v 50 mg Bid v 50 mg hs v Pbo in Younger Women in NA
- A 12-week Extension Trial to Evaluate the Safety and Tolerability of Brexpiprazole in the Treatment of Subjects With Agitation Associated With Dementia of the Alzheimer's Type
- A 28-week Safety Study of Flibanserin in Pre- and Postmenopausal Women With Hypoactive Sexual Desire Disorder
- A 4-week, Randomized, Rater-blinded, Parallel Study to Evaluate Quetiapine in Improving Sleep Quality of Schizophrenia
- A Cardiac Safety Study of an Investigational Drug to See How if Affects the Heart in People With Parkinson's Disease Complicated by Motor Fluctuations "OFF" Episodes
- A Cariprazine Study in the Prevention of Relapse in Bipolar I Disorder Patients Whose Current Episode is Manic or Depressive, With or Without Mixed Features
- a Chronobiological Treatment Combining Evening Melatonin and Morning Light Therapy in Idiopathic Hypersomnia: a Prospective, Double Bind, Randomized, Placebo-controlled -Trial
- A Clinical Pharmacology Trial of Brexpiprazole Long Acting Injectable (LAI) Administered as a Single Dose in Patients With Schizophrenia
- A Clinical Study Assessing the Potential of Piboserod for the Treatment of Heart Failure
- A Clinical Study of the Safety and Efficacy of Chemogenetics Therapy in the Treatment of Parkinson's Disease
- A Clinical Study of Trazodone Hydrochloride Prolonged-Release Tablets for Treatment of Depression
- A Comparison Between Oral Melatonin With Nasal Sevoflurane Versus Oral Chloral Hydrate With Nasal Sevoflurane in Sedation of Children Undergoing Brain MRI

### Drugs (61)

- Agomelatine
- Amisulpride Serotonin (5-HT) receptor antagonist
- Apomorphine
- Balovaptan
- Brexpiprazole
- Brolamfetamine
- Bromocriptine
- Cabergoline
- Capeserod
- Cariprazine
- Chlorophenylpiperazine
- Clothiapine Serotonin 2 (5-HT2) receptor antagonist
- Clozapine
- Dexfenfluramine Serotonin (5-HT) receptor agonist
- Dexfenfluramine hydrochloride Serotonin (5-HT) receptor agonist
- Ergotamine
- Flibanserin
- Fluoxetine
- Glemanserin
- Haloperidol

---

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