A histamine H1 receptor antagonist
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Labeled Version(s)
31918Olopatadine-d3 (hydrochloride)
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Olopatadine (hydrochloride)

Item No. 11999

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
11Z-[3-(dimethylamino)propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-acetic acid, monohydrochloride
CAS Number
140462-76-6
Synonyms
  • ALO 4943A
  • KW 4679
Molecular Formula
C21H23NO3 • HCl
Formula Weight
373.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 3 mg/mlEthanol: 0.25 mg/mlPBS (pH 7.2): 0.50 mg/ml
λmax
206, 301 nm
SMILES
CN(C)CC/C=C1C2=C(C=CC=C2)COC3=CC=C(CC(O)=O)C=C3/1.Cl
InChi Code
InChI=1S/C21H23NO3.ClH/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24;/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24);1H/b18-8-;
InChi Key
HVRLZEKDTUEKQH-NOILCQHBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $41

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    25 mg

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    50 mg

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    100 mg

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    Product Description

    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.

    References & Product Citations
    Product Description References

    1. Sharif, N.A., Xu, S.X., and Yanni, J.M. Olopatadine (AL-4943A): Ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis. J. Ocul. Pharmacol. Ther. 12(4), 401-407 (1996).

    2. Ohshima, E., Otaki, S., Sato, H., et al. Synthesis and antiallergic activity of 11-(aminoalkylidene)-6,11-dihydrodibenz[b,e]oxepin derivatives. J. Med. Chem. 35(11), 2074-2084 (1992).