Emedastine difumarate  (Synonyms: 富马酸依美斯汀；富马酸依美司丁)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

534.56

C₂₅H₃₄N₄O₉

87233-62-3

富马酸依美斯汀；富马酸依美司丁

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64.  [Content Brief]

  [2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.  [Content Brief]

  [3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52.  [Content Brief]