Structural requirements for inverse agonism and neutral antagonism of indole-, benzimidazole-, and thienopyrrole-derived histamine H4 receptor ligands.

@article{Schneider2010StructuralRF,
  title={Structural requirements for inverse agonism and neutral antagonism of indole-, benzimidazole-, and thienopyrrole-derived histamine H4 receptor ligands.},
  author={Erich H. Schneider and Andrea Stra\sser and Robin L. Thurmond and Roland Seifert},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2010},
  volume={334 2},
  pages={513-21}
}
The human histamine H(4) receptor (hH(4)R), coexpressed with Galpha(i2) and Gbeta(1)gamma(2) in Sf9 insect cells, is highly constitutively active, and thioperamide [THIO; N-cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide] is one of the most efficacious hH(4)R inverse agonists. High constitutive hH(4)R activity may have pathophysiological implications in which case inverse agonists may behave differently than neutral antagonists. To learn more about the structural requirements for hH(4)R… CONTINUE READING

Citations

Publications citing this paper.
Showing 1-10 of 16 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 44 references

Structure-activity relationships of inverse agonists for G-protein-coupled receptors

  • W Soudijn, I van Wijngaarden, AP Ijzerman
  • Med Res Rev 25:398-426
  • 2005
Highly Influential
7 Excerpts

Similar Papers

Loading similar papers…