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Olopatadine-d3 is intended for use as an internal standard for the quantification of olopatadine (Item No. 11999) by GC- or LC-MS. Olopatadine is a histamine H1 receptor antagonist (Ki =41 nM).1 It is 1,059- and 4,177-fold selective for histamine H1 over H2 and H3 receptors, respectively. Olopatadine inhibits histamine-induced phosphoinositide turnover in isolated human conjunctival epithelial cells, isolated human corneal fibroblasts, and human trabecular meshwork (TM3) cells (IC50s = 9.5, 19, and 39.9 nM, respectively). In vivo, olopatadine inhibits passive cutaneous anaphylaxis in rats (ED50 = 49 µg/kg) and IgG1-mediated bronchoconstriction in ovalbumin-sensitized guinea pigs (ED50 = 30 µg/kg).2 Formulations containing olopatadine have been used in the treatment of allergic rhinitis and conjunctivitis, as well as in the treatment of itch in patients with well-controlled urticaria.
WARNING This product is not for human or veterinary use.
1. Olopatadine (AL-
2. Synthesis and antiallergic activity of 11-