Paradoxical Stimulatory Effects of the “Standard” Histamine H4-Receptor Antagonist JNJ7777120: the H4 Receptor Joins the Club of 7 Transmembrane Domain Receptors Exhibiting Functional Selectivity

@article{Seifert2011ParadoxicalSE,
  title={Paradoxical Stimulatory Effects of the “Standard” Histamine H4-Receptor Antagonist JNJ7777120: the H4 Receptor Joins the Club of 7 Transmembrane Domain Receptors Exhibiting Functional Selectivity},
  author={Roland Seifert and Erich H. Schneider and Stefan Dove and Irena Brunskole and Detlef Neumann and Andrea Strasser and Armin Buschauer},
  journal={Molecular Pharmacology},
  year={2011},
  volume={79},
  pages={631 - 638}
}
The histamine H4 receptor (H4R) is expressed in several cell types of the immune system and is assumed to play an important pro-inflammatory role in various diseases, including bronchial asthma, atopic dermatitis, and pruritus. Accordingly, H4R antagonists have been suggested to provide valuable drugs for the treatment of these diseases. Over the past decade, the indole derivative 1-[(5-chloro-1H-indol-2-yl)carbonyl]-4-methylpiperazine (JNJ7777120) has become the “standard” H4R antagonist and… 

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