ArticleBritish journal of pharmacology2009
In vitro and in vivo characterization of A-940894: a potent histamine H4 receptor antagonist with anti-inflammatory properties.
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 16 papers.
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Who cites it
16 citing papers in PubMed, 41 citations in OpenAlex.
- New antihistamines - perspectives in the treatment of some allergic and inflammatory disorders.Archives of medical science : AMS · 2019Article
- Differential effects of functionally different histamine HNaunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Histamine drives severity of innate inflammation via histamine 4 receptor in murine experimental colitis.Mucosal immunology · 2018Article
- JNJ7777120 Ameliorates Inflammatory and Oxidative Manifestations in a Murine Model of Contact Hypersensitivity via Modulation of TLR and Nrf2 Signaling.Inflammation · 2018Article
- International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.Pharmacological reviews · 2015Review
- Suppression of Laser-Induced Choroidal Neovascularization by the Oral Medicine Targeting Histamine Receptor H4 in Mice.Translational vision science & technology · 2015Article
- The histamine H4 receptor: from orphan to the clinic.Frontiers in pharmacology · 2015Review
- Modulation of tissue inflammatory response by histamine receptors in scorpion envenomation pathogenesis: involvement of H4 receptor.Inflammation · 2014Article
- Article
- Antinociceptive and anti-inflammatory activities of crude methanolic extract of red alga Bryothamnion triquetrum.Marine drugs · 2012Article
- Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.Bioorganic & medicinal chemistry letters · 2011Article
- Antihistamines in ocular allergy: are they all created equal?Current allergy and asthma reports · 2011Review
- Expression and functional properties of canine, rat, and murine histamine H₄ receptors in Sf9 insect cells.Naunyn-Schmiedeberg's archives of pharmacology · 2011Article
- Lipopolysaccharide induces H1 receptor expression and enhances histamine responsiveness in human coronary artery endothelial cells.Immunology · 2011Article
- Histamine receptors and cancer pharmacology.British journal of pharmacology · 2010Review
- Advances in histamine pharmacology reveal new drug targets.British journal of pharmacology · 2009Article
Corrections and comments
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Authors and funding
20 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe histamine H4 receptor is widely expressed in cells of immune origin and has been shown to play a role in a variety of inflammatory processes mediated by histamine. In this report, we describe the in vitro and in vivo anti-inflammatory properties of a potent histamine H4 receptor antagonist, A-940894 (4-piperazin-1-yl-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-ylamine). EXPERIMENTAL APPROACH: We have analysed the pharmacological profile of A-940894 at mouse native, rat recombinant and human recombinant and native, histamine H4 receptors by radioligand binding, calcium mobilization, mast cell shape change, eosinophil chemotaxis assays and in the mouse model of zymosan-induced peritonitis. KEY
resultsA-940894 potently binds to both human and rat histamine H4 receptors and exhibits considerably lower affinity for the human histamine H1, H2 or H3 receptors. It potently blocked histamine-evoked calcium mobilization in the fluorometric imaging plate reader assays and inhibited histamine-induced shape change of mouse bone marrow-derived mast cells and chemotaxis of human eosinophils in vitro. In a mouse mast cell-dependent model of zymosan-induced peritonitis, A-940894 significantly blocked neutrophil influx and reduced intraperitoneal prostaglandin D2 levels. Finally, A-940894 has good pharmacokinetic properties, including half-life and oral bioavailability in rats and mice. CONCLUSIONS AND IMPLICATIONS: These data suggest that A-940894 is a potent and selective histamine H4 receptor antagonist with pharmacokinetic properties suitable for long-term in vivo testing and could serve as a useful tool for the further characterization of histamine H4 receptor pharmacology.
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