ArticleBritish journal of pharmacology2009
Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430.
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 17 papers.
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Who cites it
17 citing papers in PubMed, 49 citations in OpenAlex.
- The Histamine Four Receptor Regulates LFA-1 But Not Mac-1 -Dependent Neutrophil Adhesion and Inflammatory Functions.Inflammation · 2026Article
- Histamine 2 Receptor Agonism and Histamine 4 Receptor Antagonism Ameliorate Inflammation in a Model of Psoriasis.Acta dermato-venereologica · 2020Article
- The role of the histamine HBritish journal of pharmacology · 2020Review
- Histamine in the kidneys: what is its role in renal pathophysiology?British journal of pharmacology · 2020Review
- Effects of PARP-1 Deficiency and Histamine HFrontiers in pharmacology · 2019Article
- Pathophysiological Role of Histamine H4 Receptor in Cancer: Therapeutic Implications.Frontiers in pharmacology · 2019Article
- Systemic injection of an H4 receptor agonist induces a decrease in CREB and pCREB levels in the cerebellar vermis and prefrontal cortex in mice.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologica · 2019Article
- Activation of histamine HJournal of molecular medicine (Berlin, Germany) · 2018Article
- Histamine therapeutic efficacy in metastatic melanoma: Role of histamine H4 receptor agonists and opportunity for combination with radiation.Oncotarget · 2017Article
- Serum amyloid A expression in the breast cancer tissue is associated with poor prognosis.Oncotarget · 2016Article
- Histamine H₄ receptors in the gastrointestinal tract.British journal of pharmacology · 2015Review
- Histamine induces chemotaxis and phagocytosis in murine bone marrow-derived macrophages and RAW 264.7 macrophage-like cells via histamine H4-receptor.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2014Article
- Therapeutic potential of histamine H₄ receptor agonists in triple-negative human breast cancer experimental model.British journal of pharmacology · 2013Article
- Overexpression of histamine H₄ receptors in the kidney of diabetic rat.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2013Article
- Histamine receptors and cancer pharmacology.British journal of pharmacology · 2010Review
- Molecular and biochemical pharmacology of the histamine H4 receptor.British journal of pharmacology · 2009Review
- Advances in histamine pharmacology reveal new drug targets.British journal of pharmacology · 2009Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeWe compare the pharmacological profiles of a new histamine H4 receptor agonist 2-(2-guanidinoethyl)isothiourea (VUF 8430) with that of a previously described H4 receptor agonist, 4-methylhistamine. EXPERIMENTAL APPROACH: Radioligand binding and functional assays were performed using histamine H4 receptors expressed in mammalian cell lines. Compounds were also evaluated ex vivo in monocyte-derived dendritic cells endogenously expressing H4 receptors and in vivo in anaesthetized rats for gastric acid secretion activity. KEY
resultsBoth VUF 8430 and 4-methylhistamine were full agonists at human H4 receptors with lower affinity at rat and mouse H4 receptors. Both compounds induced chemotaxis of monocyte-derived dendritic cells. VUF 8430 also showed reasonable affinity and was a full agonist at the H3 receptor. Agmatine is a metabolite of arginine, structurally related to VUF 8430, and was a H4 receptor agonist with micromolar affinity. At histamine H3 receptors, agmatine was a full agonist, whereas 4-methylhistamine was an agonist only at high concentrations. Both VUF 8430 and agmatine were inactive at H1 and H2 receptors, whereas 4-methylhistamine is as active as histamine at H2 receptors. In vivo, VUF 8430 only caused a weak secretion of gastric acid mediated by H2 receptors, whereas 4-methylhistamine, dimaprit, histamine and amthamine, at equimolar doses, induced 2.5- to 6-fold higher output than VUF 8430. CONCLUSIONS AND IMPLICATIONS: Our results suggest complementary use of 4-methylhistamine and VUF 8430 as H4 receptor agonists. Along with H4 receptor antagonists, both agonists can serve as useful pharmacological tools in studies of histamine H4 receptors.
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