ArticleBritish journal of pharmacology2009
The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS.
Article in British journal of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 75 papers.
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Who cites it
75 citing papers in PubMed, 186 citations in OpenAlex.
- Pharmacokinetics, pharmacodynamics, and safety of izuforant, an H4R inhibitor, in healthy subjects: A phase I single and multiple ascending dose study.Clinical and translational science · 2024Trial
- Sex differences in neuromodulatory subcortical systems and their implications for Alzheimer's disease.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2026Review
- Microglial Deletion of Hrh4 Alleviates Alzheimer's Disease Pathologies by Enhancing Microglial Phagocytosis of Amyloid-β and Tau.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Targeting Histamine H4 Receptor in the Rostral Ventromedial Medulla to Relieve Hypertension.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Histamine stimulates human microglia to alter cellular prion protein expression via the HRH2 histamine receptor.Scientific reports · 2024Article
- Histaminergic System Activity in the Central Nervous System: The Role in Neurodevelopmental and Neurodegenerative Disorders.International journal of molecular sciences · 2024Review
- Histamine HBiomolecules · 2024Review
- Atopic Dermatitis: Managing the Itch.Advances in experimental medicine and biology · 2024Article
- Effects of systemic inflammation on the network oscillation in the anterior cingulate cortex and cognitive behavior.PloS one · 2024Article
- Histamine HNaunyn-Schmiedeberg's archives of pharmacology · 2023Article
- Histamine H4 Receptor Antagonist Ameliorates the Progression of Experimental Autoimmune Encephalomyelitis via Regulation of T-Cell Imbalance.International journal of molecular sciences · 2023Article
- Histamine H4 Receptor Agonist, 4-Methylhistamine, Aggravates Disease Progression and Promotes Pro-Inflammatory Signaling in B Cells in an Experimental Autoimmune Encephalomyelitis Mouse Model.International journal of molecular sciences · 2023Article
- Histamine and Its Receptors in the Mammalian Inner Ear: A Scoping Review.Brain sciences · 2023Article
- Migraine, Allergy, and Histamine: Is There a Link?Journal of clinical medicine · 2023Review
- Trisubstituted 1,3,5-Triazines as Histamine HMolecules (Basel, Switzerland) · 2023Article
- G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders.Signal transduction and targeted therapy · 2023Review
- Precision Medicine in Antidepressants Treatment.Handbook of experimental pharmacology · 2023Review
- Basophils in pruritic skin diseases.Frontiers in immunology · 2023Review
- The Histamine HBiomolecules · 2021Article
- Novel Insight of Histamine and Its Receptor Ligands in Glaucoma and Retina Neuroprotection.Biomolecules · 2021Review
15 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe histamine H4 receptor is the most recently identified of the G protein-coupled histamine receptor family and binds several neuroactive drugs, including amitriptyline and clozapine. So far, H4 receptors have been found only on haematopoietic cells, highlighting its importance in inflammatory conditions. Here we investigated the possibility that H4 receptors may be expressed in both the human and mouse CNS.
methodsImmunological and pharmacological studies were performed using a novel anti-H4 receptor antibody in both human and mouse brains, and electrophysiological techniques in the mouse brain respectively. Pharmacological tools, selective for the H4 receptor and patch clamp electrophysiology, were utilized to confirm functional properties of the H4 receptor in layer IV of the mouse somatosensory cortex.
resultsHistamine H4 receptors were prominently expressed in distinct deep laminae, particularly layer VI, in the human cortex, and mouse thalamus, hippocampal CA4 stratum lucidum and layer IV of the cerebral cortex. In layer IV of the mouse somatosensory cortex, the H4 receptor agonist 4-methyl histamine (20 micromol x L(-1)) directly hyperpolarized neurons, an effect that was blocked by the selective H4 receptor antagonist JNJ 10191584, and promoted outwardly rectifying currents in these cells. Monosynaptic thalamocortical CNQX-sensitive excitatory postsynaptic potentials were not altered by 4-methyl histamine (20 micromol x L(-1)) suggesting that H4 receptors did not act as hetero-receptors on thalamocortical glutamatergic terminals. CONCLUSIONS AND IMPLICATIONS: This is the first demonstration that histamine H4 receptors are functionally expressed on neurons, which has major implications for the therapeutic potential of these receptors in neurology and psychiatry.
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Registered trials
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.