Azelastine Hydrochloride is an effective, rapid-acting, and well-tolerated second-generation antihistamine that improves nasal symptoms associated with SAR (seasonal allergic rhinitis) and VMR (vasomotor rhinitis). Azelastine hydrochloride (azelastine) nasal spray is a histamine receptor-1 (H1) antagonist often used in treating allergic rhinitis to relieve its symptoms. Addition of azelastine at doses of 1μM or above elicited a significant dilation response to 1μM methoxamine-induced mucosal contraction. Azelastine could inhibit electrical field stimulation-induced spike mucosal contraction. Moreover, increase in concentration of azelastine had minimal effect on basal tension of nasal mucosa[3]. The treatment with the use of the combination of azelastine hydrochloride and mometasone furoate resulted in a more pronounced alleviation of rhinological symptoms and improvement of the quality of life at the early stages of therapy in comparison with mometasone furoate monotherapy[4].
Azelastine HCl/盐酸氮卓斯汀 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEp-2 cells
0.024–50 µM
24 hours
Test the antiviral activity of Azelastine-HCl against RSV, EC50 of 1.038 µM
Viruses. 2023 Nov 23;15(12):2300.
MRC-5 cells
2–12 µM
72 hours
Test the antiviral activity of Azelastine-HCl against HCoV-229E, EC50 of 3.4 µM
Viruses. 2023 Nov 23;15(12):2300.
Vero-TMPRSS2/ACE2 cells
0.05–12.5 µM
48 hours
Test the antiviral activity of Azelastine-HCl against SARS-CoV-2 omicron variant, EC50 of 2.8 µM
Viruses. 2023 Nov 23;15(12):2300.
Reconstituted human nasal tissue
0.02% (523.5 µM)
20 minutes, repeated every 24 hours for 3 days
Evaluate the antiviral effect of Azelastine nasal spray against SARS-CoV-2 infection, significantly reducing viral particle numbers
Front Pharmacol. 2022 Jun 30;13:861295.
Vero-TMPRSS2/ACE2 cells
0.4–12.5 µM
48 hours
Evaluate the antiviral effect of Azelastine against SARS-CoV-2 variants, with EC50 values ranging from 2.8–6.5 µM
Front Pharmacol. 2022 Jun 30;13:861295.
Vero E6 cells
0.4–12.5 µM
48 hours
Evaluate the antiviral effect of Azelastine against SARS-CoV-2 infection, with EC50 values of approximately 2.2 and 6.5 µM
Front Pharmacol. 2022 Jun 30;13:861295.
Azelastine HCl/盐酸氮卓斯汀 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
HT29 cell xenograft model
Oral
10 mg/kg or 20 mg/kg
Every two days
To evaluate the inhibitory effect of Azelastine on HT29 cell xenograft tumor growth, results showed that Azelastine significantly inhibited tumor growth.
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