Protein / target
Histamine H1 receptor
Protein at a glance
Biological role
Histamine receptor
Strongest disease association
Seasonal allergic rhinitis
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
G protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter.
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G protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter (PubMed:33828102, PubMed:8280179). Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity)
Subcellular location
Domains and Gene Ontology detail (12)Hide
Gene Ontology
- Cdendrite
- Cplasma membrane
- Csynapse
- Fhistamine receptor activity
- Pcellular response to histamine
- Pchemical synaptic transmission
- PG protein-coupled receptor signaling pathway
- PG protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
- Pinflammatory response
- Pphospholipase C-activating G protein-coupled receptor signaling pathway
- Ppositive regulation of vasoconstriction
- Pregulation of vascular permeability
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Synaptic signalling
- ·synapse
- ·chemical synaptic transmission
G protein-coupled signalling
- ·G protein-coupled receptor for histamine, a biogenic amine that functions as an immune m…
- ·G protein-coupled receptor signaling pathway
- ·G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messen…
- ·phospholipase C-activating G protein-coupled receptor signaling pathway
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
86 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Histamine H1 receptor antagonist
Indicated for Hypersensitivity, Urticaria
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene HRH1
Gene-level evidence surfaced through the gene HRH1that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
View evidence synthesis (4)Hide
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the per-type scores above show the calculation.
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Drug development
95 compounds recorded · 86 approved · 6 in clinical development · 3 earlier-stage
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Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Antibodies — Emerging
Protein degraders — Emerging
View underlying tractability evidence (11)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- Regulatory approval
Approval: Desloratadine Actavis (EMA)
- Regulatory approval
Approval: Desloratadine ratiopharm (EMA)
- Regulatory approval
Approval: Dasselta (EMA)
- Regulatory approval
Approval: Desloratadine Teva (EMA)
- Regulatory approval
Approval: Aerius (EMA)
- Regulatory approval
Approval: Azomyr (EMA)
- Regulatory approval
Approval: Neoclarityn (EMA)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.