ArticleNaunyn-Schmiedeberg's archives of pharmacology2011
Expression and functional properties of canine, rat, and murine histamine H₄ receptors in Sf9 insect cells.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 43 citations in OpenAlex.
- Binding affinities for histamine receptors 1 to 4: Systematic comparison of ligands from the Psychoactive Drug Screening Program KMolecular pharmacology · 2026Review
- Chemical Probes for Histamine Receptor Subtypes.Current topics in behavioral neurosciences · 2022Article
- Chemical Probes for Histamine Receptor Subtypes.Current topics in behavioral neurosciences · 2022Article
- Basal Histamine HChemistry (Weinheim an der Bergstrasse, Germany) · 2019Article
- Differential effects of functionally different histamine HNaunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.Handbook of experimental pharmacology · 2017Review
- International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.Pharmacological reviews · 2015Review
- Molecular determinants for the high constitutive activity of the human histamine H4 receptor: functional studies on orthologues and mutants.British journal of pharmacology · 2015Article
- Article
- Histamine H4-receptors inhibit mast cell renin release in ischemia/reperfusion via protein kinase C ε-dependent aldehyde dehydrogenase type-2 activation.The Journal of pharmacology and experimental therapeutics · 2014Article
- Synthesis, biological evaluation, and computational studies of Tri- and tetracyclic nitrogen-bridgehead compounds as potent dual-acting AChE inhibitors and hH3 receptor antagonists.ACS chemical neuroscience · 2014Article
- Pharmacological profile of astemizole-derived compounds at the histamine H1 and H4 receptor--H1/H4 receptor selectivity.Naunyn-Schmiedeberg's archives of pharmacology · 2014Article
- Distinct signalling pathways of murine histamine H1- and H4-receptors expressed at comparable levels in HEK293 cells.PloS one · 2014Article
- The dual H3/4R antagonist thioperamide does not fully mimic the effects of the 'standard' H4R antagonist JNJ 7777120 in experimental murine asthma.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
- Article
- Antagonists of GPR35 display high species ortholog selectivity and varying modes of action.The Journal of pharmacology and experimental therapeutics · 2012Article
- Interactions of recombinant human histamine H₁R, H₂R, H₃R, and H₄R receptors with 34 antidepressants and antipsychotics.Naunyn-Schmiedeberg's archives of pharmacology · 2012Article
- Inhibitors of membranous adenylyl cyclases.Trends in pharmacological sciences · 2012Review
- Commercially available antibodies against human and murine histamine H₄-receptor lack specificity.Naunyn-Schmiedeberg's archives of pharmacology · 2012Article
- Article
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The histamine H₄ receptor (H₄R) is expressed on cells of the immune system including eosinophils, dendritic cells, and T cells and plays an important role in the pathogenesis of bronchial asthma, atopic dermatitis, and pruritus. Analysis of the H₄R in these diseases depends on the use of animal models. However, there are substantial pharmacological differences between various H₄R species orthologs. The purpose of this study was to analyze the pharmacological properties of canine, rat, and murine H₄R in comparison to human H₄R expressed in Sf9 insect cells. Only hH₄R and cH₄R exhibited a sufficiently high [³H]histamine affinity for radioligand binding studies. Generally, cH₄R exhibited lower ligand-affinities than hH₄R. Similarly, in high-affinity GTPase studies, ligands were more potent at hH₄R than at other H₄R species orthologs. Unlike the other H₄R species orthologs, hH₄R exhibited high agonist-independent (constitutive) activity. Most strikingly, the prototypical H₄R antagonist (1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine) (JNJ7777120) exhibited partial agonistic activity at cH₄R, rH₄R, and mH₄R, whereas at hH₄R, JNJ7777120 was a partial inverse agonist. H₄R agonists from the class of N ( G )-acylated imidazolylpropylguanidines and cyanoguanidines exhibited substantial differences in terms of affinity, potency, and efficacy among H₄R species orthologs, too. The species-dependent pharmacological profiles are not due to the highly variable amino acid sequence position 341. Finally, H₄R species orthologs differ from each other in terms of regulation by NaCl. Collectively, there are profound pharmacological differences between H₄R species orthologs. Most importantly, caution must be exerted when interpreting pharmacological effects of "the prototypical H₄R antagonist" JNJ7777120 as H₄R antagonism.
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