Imetit dihydrobromide is a high affinity and effective agonist of histamine H3 and H4receptors (Ki: 0.3 and 2.7 nM). Imetit mimics the histamine effect in triggering a shape change in eosinophils (EC50: 25 nM).
VUF-10214 is an H4receptor-ligand. VUF-10214 has significant anti-inflammatory properties in the carrageenan-induced paw edema model in vivo studies in the rat reveal.
JNJ-10191584, a potent and selective antagonist at the histamine H4receptor, has antiinflammatory and analgesic effects in animal studies of acute inflammation.
UR-PI376 is a histamine H4receptor agonist (hH4R agonist) (pEC50 = 7.47, alpha = 0.93), with low activity for hH1R and hH2R and significant selectivity for hH3R (pKB = 6.00, alpha =- 0.28), as in stable-use a membrane preparation of hH(x)R-expressing Sf9
H4R antagonist 1 is a highly selective histamine H4receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.