Formulation: A solid
Formal Name: 9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-1-13C-1,1,13b-d3-3-amine, monohydrobromide
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C15[13C]H12D3N3 • HBr
Formula Weight: 334,2
Shelf life (days): 1460
Notes: Epinastine-13C-d3 is intended for use as an internal standard for the quantification of epinastine (Item No. 18136) by GC- or LC-MS. Epinastine is a histamine H1 receptor antagonist (apparent Kis = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.{48872} Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).{11338} It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).{48873} Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.{48872} Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.
English
Deutsch
