Azelastine (hydrochloride)

79307-93-0

C22H25Cl2N3O

H2O : 6.67 mg/mL (15.94 mM; Need ultrasonic); DMSO : 50 mg/mL (119.51 mM; Need ultrasonic)

Immunology/Inflammation; GPCR/G Protein; Neuronal Signaling

Azelastine hydrochloride is a potent, second-generation, selective, histamine antagonist. Target: Histamine Receptor Azelastine hydrochloride is a selective H(1)-receptor antagonist that inhibits histamine release and interferes with activation of several other mediators of allergic inflammation. Azelastine hydrochloride can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine [1]. Topical azelastine progressively improved itching and conjunctival redness in PAC patients compared to placebo and was at least as effective as levocabastine. Rapid relief is consistent with H(1)-receptor antagonist action, while continued improvement up to 6 weeks may be consistent with mechanisms involving other mediators of allergic inflammation [2]. Azelastine nasal spray was reported to control all rhinitis symptoms, including nasal congestion, regardless of rhinitis diagnosis during the 2-week study period. Patients with seasonal allergic rhinitis and patients with seasonal allergic rhinitis plus nonallergic triggers were identified as patient types most likely to respond to azelastine nasal spray [3].