> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/target/hrh1-066d4575-4b1c-5ce9-adf8-b080f76b770b > Record changed: 2026-10-13 # HRH1 ENSG00000196639 Target class GPCR Chromosome 3 Approved drugs 60 Clinical candidates (approved and in development) 72 ## Clinical evidence **Approved drugs** 60 **Clinical candidates (approved and in development)** 72 ## Druggability **Chemical probe available** Yes ## Names **Target name** HRH1 **Gene name** Histamine receptor H1 **Gene symbol** HRH1 **Protein name** Histamine H1 receptor (H1-R) (H1R) (HH1R) ## Classification **Gene biotype** Protein coding **Gene family** Histamine receptors **Target class** GPCR **Target type** Human gene ## Expression and localisation **Tissues expressed in** 36 **Protein localisation evidence grade** Supported **Highest tissue expression** 18.2 **Tissue specificity (Gini)** 0.517 **Tissue specificity (tau)** 0.809 ## Pathways and interactions **KEGG gene identifiers** - hsa:3269 **Protein interaction confidence** 0.812875 **Protein interaction partners** 8 ### Reactome pathways (2) - R-HSA-390650 - R-HSA-416476 ## Genomic location **End position** 11263557 **Start position** 11137093 **Chromosome** 3 **Strand** Forward ## Identifiers **Ensembl gene ID** ENSG00000196639 **HGNC ID** HGNC:5182 Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:5182) **NCBI Gene ID** 3269 **UniProt ID** P35367 ## Cellular location - Cell membrane - Multi-pass membrane protein . - Plasma membrane ### Publication evidence - PubMed 21697825 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/21697825/) ## Tissue expression **Tissue specificity (tau)** 0.808605 **Expression inequality (Gini)** 0.51733 ### Highest expression Expression in transcripts per million **Artery - Aorta** 18.2 **Nerve - Tibial** 13.56 **Cells - Cultured fibroblasts** 12.55 **Artery - Tibial** 10.35 **Artery - Coronary** 8.14 ### All tissues (54) Expression in transcripts per million - Artery - Aorta18.2 - Nerve - Tibial13.56 - Cells - Cultured fibroblasts12.55 - Artery - Tibial10.35 - Artery - Coronary8.14 - Cervix - Endocervix7.74 - Adipose - Subcutaneous7.54 - Vagina7.5 - Fallopian Tube7.32 - Cervix - Ectocervix6.32 - Bladder6.12 - Skin - Sun Exposed (Lower leg)5.71 - Adipose - Visceral (Omentum)5.63 - Lung5.43 - Colon - Sigmoid5.31 - Brain - Frontal Cortex (BA9)5.25 - Skin - Not Sun Exposed (Suprapubic)5.1 - Uterus4.79 - Brain - Anterior cingulate cortex (BA24)4.71 - Breast - Mammary Tissue4.65 - Ovary4.6 - Brain - Cortex4.24 - Esophagus - Muscularis4.07 - Colon - Transverse4.01 - Esophagus - Gastroesophageal Junction3.66 And 29 more, listed on the interactive page. ## Biological functions ### Biological processes (2) - GO:0007186 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007186) - GO:0071420 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0071420) ### 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 convulsions ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased convulsions ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased heart rate ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased heart rate ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased body weight ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased body weight ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - bronchoconstriction ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: bronchoconstriction ### Biological samples (4) - nervous system - 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - flushing ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: flushing ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased QTc interval ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased QTc interval ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased/increased blood pressure ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: decreased/increased blood pressure ### Biological samples (4) - nervous system - immune - 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 (4) - nervous system - immune - cardiovascular - gastrointestinal 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 (4) - nervous system - 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - skin rash ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: skin rash ### Biological samples (4) - nervous system - 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - sedation ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: sedation ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - decreased convulsions ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: decreased convulsions ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - abdominal cramps ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: abdominal cramps ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - cardiac arrhythmia ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: cardiac arrhythmia ### Biological samples (4) - nervous system - 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - scratching ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: scratching ### Biological samples (4) - nervous system - immune - 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 (4) - nervous system - immune - 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - facial swelling ### Effects - Activation/Increase/Upregulation: acute ### Studies - preclinical: facial swelling ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) - increased locomotor activity ### Effects - Inhibition/Decrease/Downregulation: acute ### Studies - preclinical: increased locomotor activity ### Biological samples (4) - nervous system - immune - cardiovascular - gastrointestinal 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 (4) - nervous system - immune - cardiovascular - gastrointestinal PubMed 28216264 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/28216264/) And 1 more, listed on the interactive page. ## Off-target safety - decreased blood pressure ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: decreased blood pressure ### Biological samples (2) - cardiovascular system - immune PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - increased body weight ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: increased body weight ### Biological samples (2) - cardiovascular system - immune PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - receptor binding ### Studies - biochemical: NVS\_GPCR\_hH1, is one of one assay component(s) measured or calculated from the NVS\_GPCR\_hH1 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 - cell-free Evidence source Source: [www.epa.gov](https://www.epa.gov/chemical-research/exploring-toxcast-data-downloadable-data) - allergic responses of flare, flush and wheal ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: allergic responses of flare, flush and wheal ### Biological samples (2) - cardiovascular system - immune PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - sedation ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: sedation ### Biological samples (2) - cardiovascular system - immune PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - bronchoconstriction ### Effects - Activation/Increase/Upregulation: general ### Studies - preclinical: bronchoconstriction ### Biological samples (2) - cardiovascular system - immune PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) - decreased allergic responses ### Effects - Inhibition/Decrease/Downregulation: general ### Studies - preclinical: decreased allergic responses ### Biological samples (2) - cardiovascular system - immune PubMed 23197038 Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/23197038/) ## Related records ### Trials (1,075) - : Vascular Function in Health and Disease - "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" - 131I-Omburtamab, in Recurrent Medulloblastoma and Ependymoma - 3-D Visualization of the Anti-Obstructive Effect of Levocetirizine - 4"S" - Seasonal Symptoms Suppression Study - 723/726 Proof of Concept Study in Allergen Challenge Chamber in Hannover - A 6-Month Efficacy and Safety Study of Org 50081 in Adult Patients With Chronic Primary Insomnia (21106/P05701/MK-8265-002) - A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers - [A Clinical Study of Ifinatamab Deruxtecan (I-DXd) in People With Metastatic Prostate Cancer (MK-2400-001)](https://trialight.com/data/trial/a-clinical-study-of-ifinatamab-deruxtecan-i-dxd-in-people-56fce060-49d9-425a-b6b7-c3a1f8ae972e.md) - [A Clinical Study of Ifinatamab Deruxtecan Based Treatment Combinations or as Monotherapy to Treat Metastatic Castrate Resistant Prostate Cancer (mCRPC) (MK-2400-01A/IDeate-Prostate02)](https://trialight.com/data/trial/a-clinical-study-of-ifinatamab-deruxtecan-based-treatment-99be48a0-44f7-46eb-bdf5-d3d2adc6018e.md) - A Clinical Study of MK-2870 Alone or With Other Treatments to Treat Gastrointestinal Cancers (MK-9999-02A) - [A Clinical Study of Raludotatug Deruxtecan in People With Ovarian Cancer (MK-5909-003)](https://trialight.com/data/trial/a-clinical-study-of-raludotatug-deruxtecan-in-people-with-6b1e5a4a-56bb-4891-a239-d464dd0753c5.md) - A Clinical Study of Sacituzumab Tirumotecan (MK-2870) in Patients With Bladder Cancer (MK-2870-027) - [A Clinical Study of Sacituzumab Tirumotecan (Sac-TMT, MK-2870) in People With Breast Cancer (MK-2870-032)](https://trialight.com/data/trial/a-clinical-study-of-sacituzumab-tirumotecan-sac-tmt-mk-2870-47421f86-889b-4c0b-a65c-14ed97707a1e.md) - [A Clinical Study of Zilovertamab Vedotin (MK-2140) Plus Rituximab Plus Cyclophosphamide, Doxorubicin, and Prednisone (R-CHP) Versus Polatuzumab Vedotin Plus R-CHP in People With Diffuse Large B-cell Lymphoma (DLBCL) (MK-2140-011/waveLINE-011)](https://trialight.com/data/trial/a-clinical-study-of-zilovertamab-vedotin-mk-2140-plus-134b8f98-3329-4e9d-af03-b73bfdbc1295.md) - A Clinical Study to Compare the Pharmacokinetic Characteristics of CKD-395 0.5/1000 mg in Healthy Male Volunteers - A Clinical Trial Evaluating the Role of Systemic Antihistamine Therapy in the Reduction of Adverse Effects Associated With Topical 5-aminolevulinic Acid Photodynamic Therapy - A Clinical Trial of Ifinatamab Deruxtecan in People With Advanced Esophageal Cancer (MK-3475-06F) - A Clinical Trial of MK-1045 in People With B-cell Acute Lymphoblastic Leukemia (MK-1045-005) - A Clinical Trial of MK-1045 in People With B-cell Cancer (MK-1045-006) ### Drugs (113) - Acrivastine Histamine H1 receptor antagonist - Alcaftadine Histamine H1 receptor antagonist - Antazoline Histamine H1 receptor antagonist - Antazoline phosphate Histamine H1 receptor antagonist - Astemizole Histamine H1 receptor antagonist - Azatadine Histamine H1 receptor antagonist - Azatadine maleate Histamine H1 receptor antagonist - Azelastine Histamine H1 receptor antagonist - Azelastine hydrochloride Histamine H1 receptor antagonist - Bepotastine Histamine H1 receptor antagonist - Bepotastine besylate Histamine H1 receptor antagonist - Betahistine Histamine H1 receptor agonist - Bilastine Histamine H1 receptor inverse agonist - Bromodiphenhydramine Histamine H1 receptor antagonist - Bromodiphenhydramine hydrochloride Histamine H1 receptor antagonist - Brompheniramine Histamine H1 receptor antagonist - Brompheniramine maleate Histamine H1 receptor antagonist - Buclizine Histamine H1 receptor antagonist - Buclizine hydrochloride Histamine H1 receptor antagonist - Carbinoxamine Histamine H1 receptor antagonist --- ## A note for AI agents You are probably reading this for a person. 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