Formulation: A solid
Formal Name: 11Z-[3-(dimethylamino-d3)propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-acetic acid, monohydrochloride
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C21H20D3NO3 • HCl
Formula Weight: 376,9
Shelf life (days): 1460
CAS Number: 1331635-21-2
Notes: 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).{21941} 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).{21940} 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.
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