Cayman Emedastine (Fumarate); Purity- Greater Than Or Equal To 98

Emedastine is a histamine H₁ receptor antagonist (K_i = 1.3 nM).¹ It is selective for histamine H₁ over H₂ and H₃ receptors (K_is = 49 and 12.43 µM, respectively), as well as α₁-, α₂-, and β₁-adrenergic and dopamine D₁ and D₂ receptors, and the serotonin (5-HT) receptor subtypes 5-HT₁ and 5-HT₂ at 10 µM.^1,2 Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC₅₀s = 1.6 and 2.9 nM, respectively).³ It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (IC₅₀s = 2.23, 3.42, and 1.50 nM, respectively).⁴ Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs.² Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.

WARNING This product is not for human or veterinary use.