HVRLZEKDTUEKQH-NEGCSKJWSA-N
- CAS NO.:1331635-21-2
- Empirical Formula: C21H21ClD3NO3
- Molecular Weight: 376.891645334
- Update Date: 2023-06-08 09:03:02
What is HVRLZEKDTUEKQH-NEGCSKJWSA-N?
The Uses of HVRLZEKDTUEKQH-NEGCSKJWSA-N
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)
Properties of HVRLZEKDTUEKQH-NEGCSKJWSA-N
storage temp. | Store at -20°C |
solubility | Methanol: Slightly soluble, |
form | A solid |
Water Solubility | Water: Slightly soluble |
Safety information for HVRLZEKDTUEKQH-NEGCSKJWSA-N
Computed Descriptors for HVRLZEKDTUEKQH-NEGCSKJWSA-N
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