Olopatadine (hydrochloride)

Olopatadine is a histamine H1 receptor antagonist (Ki =41 nM). 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). 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.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: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 3 mg/ml, Ethanol: 0.25 mg/ml, PBS (pH 7.2): 0.50 mg/ml. lambdamax: 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.