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={Herman D. Lim and Richard M. van Rijn and Ping Ling and Remko A. Bakker and Robin L. Thurmond and Rob Leurs},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2005},
  volume={314},
  pages={1310 - 1321}
}
  • H. LimR. V. van Rijn R. Leurs
  • Published 1 September 2005
  • Biology, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
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… 

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Clobenpropit analogs as dual activity ligands for the histamine H 3 and H 4 receptors : Synthesis , pharmacological evaluation , and cross-target QSAR studies Adapted from :

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