Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist

@article{Lim2005EvaluationOH,
  title={Evaluation of Histamine H1-, H2-, and H3-Receptor Ligands at the Human Histamine H4 Receptor: Identification of 4-Methylhistamine as the First Potent and Selective H4 Receptor Agonist},
  author={H. Lim and R. V. van Rijn and P. Ling and R. Bakker and R. Thurmond and R. Leurs},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2005},
  volume={314},
  pages={1310 - 1321}
}
The histamine H4 receptor (H4R) is involved in the chemotaxis of leukocytes and mast cells to sites of inflammation and is suggested to be a potential drug target for asthma and allergy. So far, selective H4R agonists have not been identified. In the present study, we therefore evaluated the human H4R (hH4R) for its interaction with various known histaminergic ligands. Almost all of the tested H1R and H2R antagonists, including several important therapeutics, displaced less than 30% of specific… Expand
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References

SHOWING 1-10 OF 50 REFERENCES
A Potent and Selective Histamine H4 Receptor Antagonist with Anti-Inflammatory Properties
  • 331
  • PDF
Chemical differentiation of histamine H1- and H2-receptor agonists.
  • 233
Histamine H4 and H2 Receptors Control Histamine-Induced Interleukin-16 Release from Human CD8+ T Cells
  • 139
  • Highly Influential
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
  • 26
8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.
  • 28
  • PDF
IDENTIFICATION OF A HISTAMINE H4 RECEPTOR ON HUMAN EOSINOPHILS—ROLE IN EOSINOPHIL CHEMOTAXIS
  • 198
Involvement of histamine H4 and H1 receptors in scratching induced by histamine receptor agonists in BalbC mice
  • 208
Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.
  • 121
  • PDF
Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
  • 64
  • Highly Influential
Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow.
  • 425
  • Highly Influential
...
1
2
3
4
5
...