Azelastine (hydrochloride)

Azelastine is a histamine H1 receptor antagonist (Ki = 1.26 nM in bovine cerebral cortex membranes). It is selective for histamine H1 over histamine H3 receptors (Ki = 158.49 nM), as well as alpha1A- and alpha1B-adrenergic receptors (Ki = 50.12 nM for both). Azelastine (0.14 µg/animal) reduces nose rubbing, sneezing, and nasal mucosa expression of IL-4 in a dust mite-induced mouse model of allergic rhinitis. It also reduces infection by a lentivirus pseudotyped with the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike glycoprotein, also known as the surface glycoprotein, in HEK293 cells expressing angiotensin-converting enzyme 2 (ACE2) when used at a concentration of 7 µg/ml. Formulations containing azelastine have been used in the treatment of seasonal allergic rhinitis and vasomotor rhinitis.Formal Name: 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone, monohydrochloride. CAS Number: 79307-93-0. Molecular Formula: C22H24ClN3O . HCl. Formula Weight: 418.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 210, 289 nm. SMILES: O=C1N(C2CCN(C)CCC2)N=C(CC3=CC=C(Cl)C=C3)C4=CC=CC=C41.Cl. InChi Code: InChI=1S/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16,/h2-3,6-11,18H,4-5,12-15H2,1H3,1H. InChi Key: YEJAJYAHJQIWNU-UHFFFAOYSA-N.