High affinity and selective histamine H4 antagonist (Ki = 12.5 nM). Exhibits >80-fold selectivity for H4 over other histamine receptors and no significant activity at a range of other targets. Inhibits histamine-induced eosinophil shape change in whole blood in vitro and ovalbumin-induced inflammation in ovalbumin-sensitized mice in vivo. Orally bioavailable.
Thurmond et al (2014) Clinical and preclinical characterization of the histamine H4 receptor antagonist JNJ-39758979. J.Pharmacol.Exp.Ther. 349 176 PMID:24549371