ReviewFrontiers in pharmacology2015
The histamine H4 receptor: from orphan to the clinic.
Review in Frontiers in pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
45 citing papers in PubMed, 1 synthesis or guideline pooled it, 133 citations in OpenAlex.
- European S2k Guideline on Chronic PruritusActa dermato-venereologica · 2025Guideline
- From Fragment Hit to Clinical Candidate: Discovery of Dual H1R/H4R Ligands with Superior Efficacy in Allergic Conjunctivitis.Journal of medicinal chemistry · 2026Article
- Immunopathogenesis of itch: an integrative framework for chronic pruritus.JID innovations : skin science from molecules to population health · 2026Review
- Rational Design, Synthesis and Pharmacological Evaluation of Chalcones as Dual-Acting Compounds-Histamine HInternational journal of molecular sciences · 2026Article
- Histamine stimulates human microglia to alter cellular prion protein expression via the HRH2 histamine receptor.Scientific reports · 2024Article
- A Machine Learning Algorithm Suggests Repurposing Opportunities for Targeting Selected GPCRs.International journal of molecular sciences · 2024Article
- The Diverse Network of Brain Histamine in Feeding: Dissect its Functions in a Circuit-Specific Way.Current neuropharmacology · 2024Review
- Expression profile of messenger and micro RNAs related to the histaminergic system in patients with five subtypes of breast cancer.Frontiers in oncology · 2024Article
- Histamine Receptors: Ex Vivo Functional Studies Enabling the Discovery of Hits and Pathways.Membranes · 2023Article
- Structural insights into the agonists binding and receptor selectivity of human histamine HNature communications · 2023Article
- Histamine and Its Receptors in the Mammalian Inner Ear: A Scoping Review.Brain sciences · 2023Article
- Trisubstituted 1,3,5-Triazines as Histamine HMolecules (Basel, Switzerland) · 2023Article
- A Systematic Review of Atopic Dermatitis: The Intriguing Journey Starting from Physiopathology to Treatment, from Laboratory Bench to Bedside.Biomedicines · 2022Review
- Pathophysiology of Post-COVID syndromes: a new perspective.Virology journal · 2022Review
- Effects of histamine and various histamine receptor antagonists on gene expression profiles of macrophages during compressive strain.Journal of orofacial orthopedics = Fortschritte der Kieferorthopadie : Organ/official journal Deutsche Gesellschaft fur Kieferorthopadie · 2022Article
- Review of potential medical treatments for middle ear cholesteatoma.Cell communication and signaling : CCS · 2022Review
- Histamine H4 Receptor Agonism Induces Antitumor Effects in Human T-Cell Lymphoma.International journal of molecular sciences · 2022Article
- Unraveling the venom chemistry with evidence for histamine as key regulator in the envenomation by caterpillarFrontiers in immunology · 2022Article
- The Histamine and Multiple Sclerosis Alliance: Pleiotropic Actions and Functional Validation.Current topics in behavioral neurosciences · 2022Article
- Histamine induced high mobility group box-1 release from vascular endothelial cells through HFrontiers in immunology · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The histamine H4 receptor (H4R) was first noted as a sequence in genomic databases that had features of a class A G-protein coupled receptor. This putative receptor was found to bind histamine consistent with its homology to other histamine receptors and thus became the fourth member of the histamine receptor family. Due to the previous success of drugs that target the H1 and H2 receptors, an effort was made to understand the function of this new receptor and determine if it represented a viable drug target. Taking advantage of the vast literature on the function of histamine, a search for histamine activity that did not appear to be mediated by the other three histamine receptors was undertaken. From this asthma and pruritus emerged as areas of particular interest. Histamine has long been suspected to play a role in the pathogenesis of asthma, but antihistamines that target the H1 and H2 receptors have not been shown to be effective for this condition. The use of selective ligands in animal models of asthma has now potentially filled this gap by showing a role for the H4R in mediating lung function and inflammation. A similar story exists for chronic pruritus associated with conditions such as atopic dermatitis. Antihistamines that target the H1 receptor are effective in reducing acute pruritus, but are ineffective in pruritus experienced by patients with atopic dermatitis. As for asthma, animal models have now suggested a role for the H4R in mediating pruritic responses, with antagonists of the H4R reducing pruritus in a number of different conditions. The anti-pruritic effect of H4R antagonists has recently been shown in human clinical studies, validating the preclinical findings in the animal models. A selective H4R antagonist inhibited histamine-induced pruritus in health volunteers and reduced pruritus in patients with atopic dermatitis. The history to date of the H4R provides an excellent example of the deorphanization of a novel receptor and the translation of this into clinical efficacy in humans.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.