JNJ-7777120

JNJ-7777120 is a potent and selective histamine H₄ receptor antagonist (K_i=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory^[1][2]. In Vitro:JNJ-7777120 (0, 10, 100, 1000 nM; ~6 h) shows functional antagonism of the human and mouse histamine H4 receptors in SK-N-MC cells^[1].
JNJ-7777120 (10 µM; 10 min) blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells^[1].
JNJ7777120 (30-100 µM; 30 min) inhibits dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC^[2]. In Vivo:JNJ-7777120 shows equipotent against the human, mouse, and rat receptors and exhibits at least 1000-fold selectivity over H₁, H₂, or H₃ receptors^[1].
JNJ-7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ~3 h in both species^[1].
JNJ-7777120 (20 mg/kg; s.c.; single daily for 2 days) blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice^[1].
JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model^[1].