> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/htr4-2fb1e222-74b4-5a8d-9acd-92f3e497a89f
> Record changed: 2026-10-13

# HTR4

ENSG00000164270

Target class

GPCR

Chromosome

5

Approved drugs

8

Clinical candidates (approved and in development)

20

## Clinical evidence

**Approved drugs**

8

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

20

## Druggability

**Chemical probe available**

Yes

## Names

**Other names**

- 5-HT4

**Target name**

HTR4

**Gene name**

5-hydroxytryptamine receptor 4

**Gene symbol**

HTR4

**Protein name**

5-hydroxytryptamine receptor 4 (5-HT-4) (5-HT4) (Serotonin receptor 4)

## 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**

3

**Highest tissue expression**

2.34

**Tissue specificity (Gini)**

0.73

**Tissue specificity (tau)**

0.913

## Pathways and interactions

**KEGG gene identifiers**

- hsa:3360

**Protein interaction confidence**

0.891

**Protein interaction partners**

4

### Reactome pathways (2)

- R-HSA-390666
- R-HSA-418555

## Genomic location

**End position**

148677235

**Start position**

148446042

**Chromosome**

5

**Strand**

Reverse

## Identifiers

**Ensembl gene ID**

ENSG00000164270

**HGNC ID**

HGNC:5299

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:5299)

**NCBI Gene ID**

3360

**UniProt ID**

Q13639

## Cellular location

- Cell membrane
- Multi-pass membrane protein . Endosome membrane
- Multi-pass membrane protein . Note=Interaction with SNX27 mediates recruitment to early endosomes, while interaction with NHERF1 and EZR might target the protein to specialized subcellular regions, such as microvilli. .

### Publication evidence (2)

- PubMed 10821780  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/10821780/)
- PubMed 35714614  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/35714614/)

## Tissue expression

**Tissue specificity (tau)**

0.913159

**Expression inequality (Gini)**

0.729793

### Highest expression

Expression in transcripts per million

**Small Intestine - Terminal Ileum**

2.34

**Colon - Transverse**

1.36

**Brain - Nucleus accumbens (basal ganglia)**

1.24

**Pituitary**

0.86

**Heart - Atrial Appendage**

0.85

### All tissues (54)

Expression in transcripts per million

- Small Intestine - Terminal Ileum2.34
- Colon - Transverse1.36
- Brain - Nucleus accumbens (basal ganglia)1.24
- Pituitary0.86
- Heart - Atrial Appendage0.85
- Artery - Aorta0.8
- Artery - Coronary0.79
- Brain - Caudate (basal ganglia)0.76
- Colon - Sigmoid0.73
- Artery - Tibial0.5
- Brain - Frontal Cortex (BA9)0.36
- Brain - Cortex0.35
- Brain - Putamen (basal ganglia)0.29
- Adrenal Gland0.2
- Brain - Anterior cingulate cortex (BA24)0.18
- Brain - Hippocampus0.16
- Heart - Left Ventricle0.1
- Fallopian Tube0.08
- Brain - Hypothalamus0.08
- Testis0.07
- Nerve - Tibial0.07
- Brain - Amygdala0.07
- Skin - Not Sun Exposed (Suprapubic)0.06
- Skin - Sun Exposed (Lower leg)0.06
- Uterus0.05

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (5)

- GO:0007186  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007186)
- GO:0007187  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007187)
- GO:0007189  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007189)
- GO:0007192  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007192)
- GO:0120056  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0120056)

### Cellular components (3)

- 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:0016020  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0016020)

### Molecular functions (3)

- 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:0099589  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0099589)

## On-target safety

- increased gastric emptying  
### Effects

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

  - preclinical: increased gastric emptying  
### Biological samples (3)

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

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

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

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

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

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

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

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

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

  - central nervous system
  - cardiovascular
  - gastrointestinal  
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)

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

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

  - preclinical: decreased blood volume  
### Biological samples (3)

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

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

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

  - central 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)

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

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

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

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

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

  - preclinical: increased QTc interval  
### Biological samples (3)

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

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

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

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

## Related records

### Trials (367)

- "THINK Trial: Treatment of Headache With IntraNasal Ketamine: A Randomized Controlled Trial Evaluating the Efficacy of Intranasal Ketamine Versus Standard Therapy in the Management of Primary Headache Syndromes in the Emergency Department"
- A Clinical Study Assessing the Potential of Piboserod for the Treatment of Heart Failure
- A Clinical Trial Analyzing Effects of Prokinetic Drug on the Blood Glucose in Patients With Type 2 Diabetes
- A Comparative Evaluation of Mosapride Versus Metoclopramide for Enteral Feeding Intolerance in Critically Ill Patients
- A Comparison of the Efficacy of Amisulpride and Placebo in the Prevention of PONV in Patients at Moderate-to-high Risk of PONV.
- A Cost Effective Treatment for Headache in Pregnancy When Acetaminophen Alone is Ineffective.
- A Dose-Ranging Study of ATI 7505 in Patients With Postprandial Distress Syndrome
- A Korean Study of Efficacy and Safety of Aprepitant-based Triple Regimen for the Prevention of Chemotherapy-Induced Nausea and Vomiting in the First Cycle of Moderately Emetogenic Chemotherapy (Non-doxorubicin Hydrochloride \[Adriamycin\] and Cyclophosphamide Regimens) (MK-0869-225) (KMEC)
- A Multicenter, Double-Blind, Randomized, Placebo-Controlled, 12-Week, Dose-Range-Finding Trial of YKP10811 Capsules Administered Once Daily to Subjects With Chronic Idiopathic Constipation
- A Phase 1, Multiple Intravenous Dose Study to Examine Safety, Tolerability, and PK of Intravenous TD-8954, a 5-HT4 Receptor Agonist, in Healthy Subjects
- A Phase 2 Study to Evaluate Pharmacodynamics of YKP10811 in Patients With Chronic or Functional Constipation
- A Pilot Clinical Trial of a New Neuromodulation Device for Acute Attacks of Migraine in Children and Adolescents
- A Pilot Study to Evaluate Barhemsys for the Prevention of Postoperative Nausea And Vomiting in the Bariatric Surgery Population
- A Post Marketing Surveillance Study on the Safety and Effectiveness of Prucalopride in the Treatment of Chronic Constipation
- A Randomized, Double-Blind Study to Evaluate the Safety, Tolerability, and Pharmacodynamics of a Single Dose of Intravenous TD-8954 Compared With Metoclopramide in Critically Ill Patients With Enteral Feeding Intolerance
- A Randomized, Double-blind, Placebo-controlled Multicenter Study to Assess the Efficacy, Safety and Tolerability of Tegaserod 2 mg Bid vs Placebo in Patients With Chronic Constipation
- A Randomized, Open-label, Two-way Crossover Trial to Determine the Pharmacokinetics of Metoclopramide When Administered as the Orally Disintegrating Tablet Compared to Reglan® Tablets in Subjects With Diabetic Gastroparesis
- A Study Evaluating the Safety, Tolerability and Pharmacokinetics of ASY202 in Healthy Adults
- A Study of ANAVEX3-71 in Adults With Schizophrenia
- A Study of Cisapride in Patients With Symptomatic Gastro-Oesophageal Reflux Disease

### Drugs (25)

- Amisulpride Serotonin (5-HT) receptor antagonist
- Capeserod Serotonin 4 (5-HT4) receptor partial agonist
- Cisapride Serotonin 4 (5-HT4) receptor agonist
- Cisapride monohydrate Serotonin 4 (5-HT4) receptor agonist
- Clebopride Serotonin 4 (5-HT4) receptor agonist
- Dexfenfluramine Serotonin (5-HT) receptor agonist
- Dexfenfluramine hydrochloride Serotonin (5-HT) receptor agonist
- Felcisetrag Serotonin 4 (5-HT4) receptor agonist
- Levosulpiride Serotonin 4 (5-HT4) receptor agonist
- Metoclopramide Serotonin 4 (5-HT4) receptor agonist
- Metoclopramide hydrochloride Serotonin 4 (5-HT4) receptor agonist
- Mosapride Serotonin 4 (5-HT4) receptor agonist
- [Naronapride](https://trialight.com/data/asset/naronapride-add7b688-2e9b-483e-9964-e2b492d963b7.md) Serotonin 4 (5-HT4) receptor agonist
- Piboserod Serotonin 4 (5-HT4) receptor antagonist
- Prucalopride Serotonin 4 (5-HT4) receptor agonist
- Prucalopride succinate Serotonin 4 (5-HT4) receptor agonist
- PRX-03140 Serotonin 4 (5-HT4) receptor partial agonist
- Relenopride Serotonin 4 (5-HT4) receptor agonist
- Renzapride Serotonin 4 (5-HT4) receptor agonist
- Revexepride Serotonin 4 (5-HT4) receptor agonist

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