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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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HRH3
histamine receptor H3
Chromosome 20 · 20q13.33
NCBI Gene: 11255Ensembl: ENSG00000101180.18HGNC: HGNC:5184UniProt: Q9Y5N1
63PubMed Papers
20Diseases
16Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
protein bindingsynapseneurotransmitter receptor activityhistamine receptor activitynarcolepsy-cataplexy syndromenarcolepsyobstructive sleep apneaneurodegenerative disease
✦AI Summary

HRH3 encodes the histamine H3 receptor, a G-protein coupled receptor primarily expressed in the central nervous system that functions as a presynaptic autoreceptor and heteroreceptor 1. The receptor modulates neurotransmitter release from histaminergic, noradrenergic, and other neurons through inhibition of adenylate cyclase and displays high constitutive activity 1. HRH3 demonstrates significant clinical relevance across multiple conditions. In hepatocellular carcinoma, HRH3 is upregulated and promotes tumor growth and metastasis by inducing lamellipodia formation, with expression levels correlating with patient survival outcomes 2. The gene shows altered expression patterns in autism spectrum disorder, where histaminergic gene sets including HRH3 are significantly differentially expressed in postmortem prefrontal cortex tissue 3. Additionally, HRH3 polymorphism rs3787429 associates with chr20 heart failure risk in Chinese populations, with the T allele showing protective effects 4. H3 receptor antagonists show therapeutic promise for alcohol use disorder, reducing drinking behavior and alcohol-induced place preference in rodent models 5. The receptor also appears relevant to stress-related psychiatric conditions, as HRH3 expression is upregulated in prefrontal cortex following chr20 social isolation stress 6.

Sources cited
1
HRH3 functions as presynaptic receptor modulating neurotransmitter release and has constitutive activity
PMID: 11956964
2
HRH3 is upregulated in hepatocellular carcinoma and promotes tumor growth and metastasis
PMID: 31002350
3
HRH3 expression is altered in autism spectrum disorder prefrontal cortex
PMID: 28485729
4
HRH3 polymorphism rs3787429 associates with chronic heart failure risk
PMID: 26989676
5
H3 receptor antagonists reduce alcohol drinking behavior in rodent models
PMID: 30801695
6
HRH3 expression is upregulated in prefrontal cortex following social isolation stress
PMID: 39502833
Disease Associationsⓘ20
narcolepsy-cataplexy syndromeOpen Targets
0.52Moderate
narcolepsyOpen Targets
0.48Moderate
obstructive sleep apneaOpen Targets
0.39Weak
neurodegenerative diseaseOpen Targets
0.37Weak
hypersomniaOpen Targets
0.37Weak
VertigoOpen Targets
0.37Weak
Prader-Willi syndromeOpen Targets
0.33Weak
Parkinson diseaseOpen Targets
0.33Weak
idiopathic hypersomniaOpen Targets
0.32Weak
schizophreniaOpen Targets
0.30Weak
Cognitive impairmentOpen Targets
0.28Weak
Alzheimer diseaseOpen Targets
0.12Weak
attention deficit hyperactivity disorderOpen Targets
0.12Weak
allergic rhinitisOpen Targets
0.11Weak
alcohol dependenceOpen Targets
0.10Weak
autoimmune diseaseOpen Targets
0.10Suggestive
idiopathic membranous glomerulonephritisOpen Targets
0.10Suggestive
Morvan syndromeOpen Targets
0.10Suggestive
C1 inhibitor deficiencyOpen Targets
0.10Suggestive
type II hypersensitivity reaction diseaseOpen Targets
0.10Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets16
ABT-288Phase II
Histamine H3 receptor antagonist
Alzheimer disease
BAVISANTPhase II
Histamine H3 receptor antagonist
attention deficit hyperactivity disorder
BETAHISTINEApproved
Histamine H1 receptor agonist
Vertigo
CIPRALISANTPhase II
Histamine H3 receptor agonist
attention deficit hyperactivity disorder
GSK-1004723Phase II
Histamine H3 receptor antagonist
allergic rhinitis
GSK189254Phase II
Histamine H3 receptor antagonist
narcolepsy
GSK239512Phase II
Histamine H3 receptor antagonist
Alzheimer disease
IRDABISANTPhase I
Histamine H3 receptor antagonist
Cognitive impairment
JNJ-17216498Phase II
Histamine H3 receptor antagonist
narcolepsy
JNJ-39220675Phase II
Histamine H3 receptor antagonist
alcohol dependence
MK-0249Phase II
Histamine H3 receptor inverse agonist
Alzheimer disease
PF-03654746Phase II
Histamine H3 receptor antagonist
attention deficit hyperactivity disorder
PF-03654764Phase II
Histamine H3 receptor antagonist
allergic rhinitis
PITOLISANTApproved
Histamine H3 receptor inverse agonist
PITOLISANT HYDROCHLORIDEApproved
Histamine H3 receptor inverse agonist
narcolepsy-cataplexy syndrome
SUVN-G3031Phase III
Histamine H3 receptor inverse agonist
Cognitive impairment
Related Genes
HDCProtein interaction79%HNMTProtein interaction79%DRD1Protein interaction78%CLIC4Protein interaction77%DRD2Protein interaction71%CHRM4Shared pathway38%
Tissue Expression6 tissues
Brain
100%
Bone Marrow
1%
Liver
0%
Ovary
0%
Lung
0%
Heart
0%
Gene Interaction Network
Click a node to explore
HRH3HDCHNMTDRD1CLIC4DRD2CHRM4
PROTEIN STRUCTURE
Preparing viewer…
PDB7F61 · 2.60 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.12LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.70 [0.46–1.12]
RankingsWhere HRH3 stands among ~20K protein-coding genes
  • #7,374of 20,598
    Most Researched63
  • #480of 1,025
    FDA-Approved Drug Targets3
  • #11,505of 17,882
    Most Constrained (LOEUF)1.12
Genes detectedHRH3
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Histamine pharmacogenomics.
PMID: 19450133
Pharmacogenomics · 2009
1.00
2
Structure of the human histamine H3 receptor gene (HRH3) and identification of naturally occurring variations.
PMID: 11956964
J Neural Transm (Vienna) · 2002
0.90
3
Upregulated histamine receptor H3 promotes tumor growth and metastasis in hepatocellular carcinoma.
PMID: 31002350
Oncol Rep · 2019
0.80
4
Altered expression of histamine signaling genes in autism spectrum disorder.
PMID: 28485729
Transl Psychiatry · 2017
0.70
5
Histamine, histamine H
PMID: 30801695
Br J Pharmacol · 2020
0.60