Emedastine (difumarate)

Emedastine difumarate is an orally active, selective and high affinity histamine H₁ receptor antagonist with a K_i value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis^[1][2][3]. In Vitro: Emedastine difumarate inhibits histamine H₂ receptor (K_i=49067 nM) and histamine H₃ receptor (K_i=12430 nM)^[1].
High concentrations of Emedastine difumarate (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts^[2].
Emedastine difumarate (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration^[2]. In Vivo: Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg^[3].
Pretreatment with Emedastine difumarate (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B^[3].
Emedastine difumarate (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs^[2].
Emedastine difumarate inhibits histamine-induced contractions of isolated ileum (IC₅₀=6.1 nM)^[2].