2930288-75-6

Azelastine-13C-d3 is intended for use as an internal standard for the quantification of azelastine (Item No. 20873) by GC- or LC-MS. Azelastine is a histamine H1 receptor antagonist (Ki = 1.26 nM in bovine cerebral cortex membranes).1 It is selective for histamine H1 over histamine H3 receptors (Ki = 158.49 nM), as well as α1A- and α1B-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.2 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.3 Formulations containing azelastine have been used in the treatment of seasonal allergic rhinitis and vasomotor rhinitis.WARNING This product is not for human or veterinary use.

[1] PANAYIOTIS A. PROCOPIOU*. The Discovery of Phthalazinone-Based Human H1 and H3 Single-Ligand Antagonists Suitable for Intranasal Administration for the Treatment of Allergic Rhinitis[J]. Journal of Medicinal Chemistry, 2011, 54 7: 2183-2195. DOI: 10.1021/jm1013874
[2] SHAOYI SUN . Discovery of XEN445: A potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice[J]. Bioorganic & Medicinal Chemistry, 2013, 21 24: Pages 7724-7734. DOI: 10.1016/j.bmc.2013.10.023
[3] LEAH R. REZNIKOV . Identification of antiviral antihistamines for COVID-19 repurposing[J]. Biochemical and biophysical research communications, 2021, 538: Pages 173-179. DOI: 10.1016/j.bbrc.2020.11.095