> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/hrh2-5ddb02a6-bd6c-59a8-91de-1aa25ffc4091
> Record changed: 2026-10-13

# HRH2

ENSG00000113749

Target class

GPCR

Chromosome

5

Approved drugs

11

Clinical candidates (approved and in development)

12

## Clinical evidence

**Approved drugs**

11

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

12

## Druggability

**Chemical probe available**

Yes

## Names

**Target name**

HRH2

**Gene name**

Histamine receptor H2

**Gene symbol**

HRH2

**Protein name**

Histamine H2 receptor (H2R) (HH2R) (Gastric receptor I)

## Classification

**Gene biotype**

Protein coding

**Gene family**

Histamine receptors

**Target class**

GPCR

**Target type**

Human gene

## Expression and localisation

**Tissues expressed in**

45

**Highest tissue expression**

90.51

**Tissue specificity (Gini)**

0.634

**Tissue specificity (tau)**

0.947

## Pathways and interactions

**KEGG gene identifiers**

- hsa:3274

**Protein interaction confidence**

0.845667

**Protein interaction partners**

6

### Reactome pathways (2)

- R-HSA-390650
- R-HSA-418555

## Genomic location

**End position**

175710756

**Start position**

175657797

**Chromosome**

5

**Strand**

Forward

## Identifiers

**Ensembl gene ID**

ENSG00000113749

**HGNC ID**

HGNC:5183

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:5183)

**NCBI Gene ID**

3274

**UniProt ID**

P25021

## Cellular location

- Cell membrane
- Multi-pass membrane protein.

## Tissue expression

**Tissue specificity (tau)**

0.947317

**Expression inequality (Gini)**

0.634074

### Highest expression

Expression in transcripts per million

**Whole Blood**

90.51

**Spleen**

23.98

**Stomach**

18.85

**Brain - Caudate (basal ganglia)**

14.5

**Brain - Frontal Cortex (BA9)**

13.87

### All tissues (54)

Expression in transcripts per million

- Whole Blood90.51
- Spleen23.98
- Stomach18.85
- Brain - Caudate (basal ganglia)14.5
- Brain - Frontal Cortex (BA9)13.87
- Brain - Cortex13.79
- Brain - Nucleus accumbens (basal ganglia)12.88
- Brain - Putamen (basal ganglia)12.07
- Heart - Left Ventricle11.88
- Lung10.21
- Artery - Coronary9.51
- Heart - Atrial Appendage7.45
- Adipose - Subcutaneous7.36
- Artery - Tibial7.17
- Brain - Anterior cingulate cortex (BA24)6.27
- Prostate5.95
- Adipose - Visceral (Omentum)5.87
- Fallopian Tube4.62
- Artery - Aorta4.53
- Nerve - Tibial4.15
- Breast - Mammary Tissue3.9
- Cervix - Ectocervix3.57
- Bladder3.42
- Uterus3.41
- Cervix - Endocervix3.12

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (3)

- GO:0006955  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0006955)
- 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)

### Cellular components

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

### Molecular functions (2)

- GO:0004969  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0004969)
- GO:0005515  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515)

## On-target safety

- increased heart rate  
### Effects

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

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

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

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

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

  - immune
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- Increased, predation  
### Effects

  - Inhibition/Decrease/Downregulation  
### Studies

  - cell-based  
Evidence source  
Source: [aopwiki.org](https://aopwiki.org/aops/99)
- positive inotropic effect on the human ventricle  
### Effects

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

  - clinical: positive inotropic effect on the human ventricle  
### Biological samples (2)

  - cardiovascular system
  - gastrointestinal  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- reduction of gastric acid secretion  
### Effects

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

  - clinical: reduction of gastric acid secretion  
### Biological samples (2)

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

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

  - preclinical: decreased gastric acid secretion  
### Biological samples (3)

  - immune
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- decreased gastric emptying  
### Effects

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

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

  - immune
  - cardiovascular
  - gastrointestinal  
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)

  - immune
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased drinking  
### Effects

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

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

  - immune
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- Decreased, survival  
### Effects

  - Inhibition/Decrease/Downregulation  
### Studies

  - cell-based  
Evidence source  
Source: [aopwiki.org](https://aopwiki.org/aops/99)
- decreased blood pressure  
### Effects

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

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

  - immune
  - 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)

  - immune
  - cardiovascular
  - gastrointestinal  
PubMed 28216264  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/)
- increased gastric acid secretion  
### Effects

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

  - preclinical: increased gastric acid secretion  
### Biological samples (3)

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

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

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

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

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

  - clinical: emesis  
### Biological samples (2)

  - cardiovascular system
  - gastrointestinal  
Evidence source  
Source: [doi.org](https://doi.org/10.1002/9781118098141.ch2)
- stimulation of gastric acid secretion  
### Effects

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

  - clinical: stimulation of gastric acid secretion  
### Biological samples (2)

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

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

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

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

## Off-target safety

- decreased gastric acid secretion  
### Effects

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

  - preclinical: decreased gastric acid secretion  
### Biological samples (2)

  - cardiovascular system
  - gastrointestinal  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- positive inotropy  
### Effects

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

  - preclinical: positive inotropy  
### Biological samples (2)

  - cardiovascular system
  - gastrointestinal  
PubMed 23197038  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/)
- increased gastric acid secretion  
### Effects

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

  - preclinical: increased gastric acid secretion  
### Biological samples (2)

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

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

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

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

## Related records

### Trials (204)

- : Vascular Function in Health and Disease
- \[KJ-INT-002\] BE Study
- A Clinico-Bacteriological Study and Effect of Stress Ulcer Prophylaxis on Occurrence of Ventilator Associated Pneumonia
- A Comparative Efficacy and Safety Study of Nexium Delayed-Release Capsules (40mg qd and 20mg qd) Versus Ranitidine 150mg Bid for the Healing of NSAID-Associated Gastric Ulcers When Daily NSAID Use is Continued
- A Comparative Efficacy and Safety Study of Nexium Delayed-Release Capsules (40mg qd and 20mg qd) Versus Ranitidine 150mg Bid for the Healing of NSAID-Associated Gastric Ulcers When Daily NSAID Use is Continued in Subjects in the US Only
- A Comparison of Efficacy of Intravenous Esomeprazole and Ranitidine Treatment of Dyspeptic Pain
- A Crossover Study to Assess the Drug-drug Interaction of Acid Reducing Agent(s) on the Pharmacokinetics of a Single Oral Dose of Lumicitabine (JNJ-64041575) in Healthy Adult Participants
- A Multi-center, Randomized, Double-blind Phase III Clinical Trial to Assess and Compare to the Efficacy and Safety of Lafutidine, Famotidine and Omeprazole-referenced in Korean Erosive Esophagitis Patients
- A Multiple Dose Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of BMS-986263 in Healthy Participants
- A Phase 1 Study to Evaluate the Effects of Omeprazole and Famotidine on the Absorption of Telotristat Ethyl in Healthy Subjects
- A Phase 2 Study of Isatuximab in Combination With Pomalidomide and Dexamethasone in MM Patients Who Received One Prior Line of Therapy Containing Lenalidomide and a Proteasome Inhibitor
- A Phase I Study of Oral Ixabepilone in Subjects With Advanced Cancer
- A Phase I/II Study of Intraperitoneal Paclitaxel in Patients With Metastatic Appendiceal Adenocarcinoma
- A Phase II Study of Perioperative Paclitaxel in Patients With Gastric Adenocarcinoma and Carcinomatosis or Positive Cytology
- A Phase II Trial of Neoadjuvant Laparoscopic Hyperthermic Intraperitoneal Chemotherapy (HIPEC) With Chemoradiation
- A Pilot Randomized, Double-Blind, Placebo-Controlled, Parallel Design, Multicenter Trial to Evaluate the Effect of Ranitidine on Immunologic Indicators in Asymptomatic HIV-1 Infected Subjects With a CD4 Cell Count Between 400-700 Cells/mm3
- A Relative Bioavailability Study of 20 mg Famotidine Tablets Under Fasting Condition
- A Relative Bioavailability Study of 20 mg Famotidine Tablets Under Fed Condition
- [A Single and Multiple Ascending Doses, Relative Bioavailability, Food Effect, and Drug-Drug Interaction Study of NX-5948 in Healthy Volunteers](https://trialight.com/data/trial/a-single-and-multiple-ascending-doses-relative-e765be29-f034-4382-84c2-075c49a7d226.md)
- A Study Assessing the Drug Levels, Drug Effects, and Safety of BMS-986322 in Healthy Participants

### Drugs (15)

- Betazole Histamine H2 receptor agonist
- Betazole hydrochloride Histamine H2 receptor agonist
- Cimetidine Histamine H2 receptor antagonist
- Cimetidine hydrochloride Histamine H2 receptor antagonist
- Ebrotidine Histamine H2 receptor antagonist
- [Famotidine](https://trialight.com/data/asset/famotidine-5721dbb9-1373-4622-a660-e27ebf480acc.md) Histamine H2 receptor antagonist
- Lafutidine Histamine H2 receptor antagonist
- Methantheline Histamine H2 receptor antagonist
- Methantheline bromide Histamine H2 receptor antagonist
- Nizatidine Histamine H2 receptor antagonist
- Ranitidine Histamine H2 receptor antagonist
- Ranitidine bismuth citrate Histamine H2 receptor antagonist
- Ranitidine hydrochloride Histamine H2 receptor antagonist
- Tolazoline Histamine H2 receptor agonist
- Tolazoline hydrochloride Histamine H2 receptor agonist

---

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