HVRLZEKDTUEKQH-NEGCSKJWSA-N Chemical Properties

storage temp. 

Store at -20°C

solubility 

Methanol: Slightly soluble,

form 

A solid

Water Solubility 

Water: Slightly soluble

HVRLZEKDTUEKQH-NEGCSKJWSA-N Usage And Synthesis

Uses

Labelled Olopatadine. Dual acting histamine H1-receptor antagonist and mast cell stabilizer. Antiallergic; antihistaminic.

Biological Activity

Olopatadine-d3 is intended for use as an internal standard for the quantification of olopatadine 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.

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 conjunctivitisJ. 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 derivativesJ. Med. Chem.35(11)2074-2084(1992)

HVRLZEKDTUEKQH-NEGCSKJWSA-N(1331635-21-2)Related Product Information

• 2-[(4-METHYLPHENOXY)METHYL]BENZOIC ACID
• (E)-Olopatadine Hydrochloride
• 3-((Dimethylamino)propyl)triphenylphosphonium bromide
• Olopatadine Impurity 11 HBr
• Olopatadine Impurity 5
• Olopatadine-d3 N-Oxide
• N-DesMethyl Olopatadine
• 1-Propanamine, 3-(diphenylphosphinyl)-N,N-dimethyl-
• Olopatadine Impurity 9
• Olopatadine Amide
• Isohexyltriphenylphosphonium Bromide
• α-Hydroxy Olopatadine
• Olopatadine Impurity 29
• Olopatadine Impurity 4
• (E)-Olopatadine-O-methyl
• N-DesMethyl Olopatadine Methyl Ester Trifluoroacetic Acid Salt
• 1253107-27-5
• (Z)-[4-[2-(4-Dimethylaminobut-1-enyl)benzyloxy]-3-iodophenyl]acetic Acid Methyl Ester