Epinastine-13C-d3 (hydrobromide)

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.1,2 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.2 Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).3 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.).4 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.2 Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.WARNING This product is not for human or veterinary use.

[1] ANTON M. TER LAAK. Is there a difference in the affinity of histamine H1 receptor antagonists for CNS and peripheral receptors An in vitro study[J]. European journal of pharmacology, 1993, 232 2: Pages 199-205. DOI: 10.1016/0014-2999(93)90774-c
[2] GRAZYNA GALATOWICZ. Ocular anti-allergic compounds selectively inhibit human mast cell cytokines in vitro and conjunctival cell infiltration in vivo[J]. Clinical and Experimental Allergy, 2007, 37 11: 1648-1656. DOI: 10.1111/j.1365-2222.2007.02782.x
[3] MATSUSHITA NOBUTOSHI . Pharmacological Studies on the Novel Antiallergic Drug HQL-79: II. Elucidation of Mechanisms for Antiallergic and Antiasthmatic Effects[J]. Japanese journal of pharmacology, 1998, 78 1: Pages 11-22. DOI: 10.1254/jjp.78.11
[4] TADAFUMI TAMURA . Effects of orally administered olopatadine hydrochloride on the ocular allergic reaction in rats[J]. Allergology International, 2003, 52 2: Pages 77-83. DOI: 10.1046/j.1440-1592.2003.00281.x