**Background**
Allergic rhinitis and asthma are prevalent inflammatory conditions characterized by the release of histamine, which triggers various physiological responses through the activation of histamine receptors. Among these, the histamine 1 (H1) receptor plays a pivotal role in mediating the allergic response, making it a primary target for therapeutic intervention. Beyond respiratory allergies, recent research has explored the potential of antihistamines in managing metabolic disorders and viral entry, including SARS-CoV-2. Understanding the diverse pharmacological profile of H1 antagonists is essential for developing comprehensive treatment strategies for airway remodeling and systemic metabolic dysfunction. In this context, we will introduce a potent and selective H1 receptor antagonist – Azelastine.
**Definition**
Azelastine is a potent and selective histamine 1 (H1) antagonist. According to the Azelastine technical information, it is utilized in the research of allergic rhinitis, asthma, diabetic hyperlipidemia, and SARS-CoV-2.
**In Vitro and In Vivo Studies**
The Azelastine biological activity has been demonstrated across various experimental models. In vitro studies using human nasal epithelial cells (HNEpC) showed that Azelastine (100 μM and 400 μM) significantly inhibited HNEpC proliferation over a 21-day incubation period, suggesting a potential role in combating airway remodeling. Furthermore, Western Blot analysis revealed that treatment with 100 μM Azelastine for 7 days significantly up-regulated the levels of H1R, M1R, and M3R in HNEpC.
Azelastine in vivo efficacy has been extensively evaluated in metabolic models. In diabetic hyperlipidemic male albino Wistar rats, oral administration of Azelastine (4 mg/kg; daily for 8 weeks) significantly reduced blood glucose, HbA1c, and serum alkaline phosphatase (ALP) and osteocalcin. This treatment also improved the lipid profile by decreasing LDL-c and increasing HDL-c, while downregulating apolipoprotein B and increasing apolipoprotein A expression. Additionally, the administration of Azelastine attenuated calcium deposition and aortic calcification in these models. In conclusion, Azelastine is a versatile H1 receptor antagonist with significant potential in treating allergic inflammation and modulating metabolic complications in diabetic hyperlipidemic states.
Keywords
Azelastine, 79307-93-0, Histamine Receptor, SARS-CoV, SARS coronavirus, antihistamine, allergic rhinitis, asthma, SARS-CoV-2, Inhibitor, inhibitor, inhibit
References
[1] Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochloridel. Expert Rev Clin Immunol. 2005 Jul;1(2):191-201.
[2] Mohamed M Elseweidy, et al. Azelastine a potent antihistamine agent, as hypolipidemic and modulator for aortic calcification in diabetic hyperlipidemic rats model. Arch Physiol Biochem. 2020 Jul 2;1-8.
[3] Carlos D. Zappia, et al. Azelastine potentiates antiasthmatic dexamethasone effect on a murine asthma model. Pharmacol Res Perspect. 2019 Dec; 7(6): e00531.
[4] Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1–7.
[5] Shao-Cheng Liu, et al. Effect of budesonide and azelastine on histamine signaling regulation in human nasal epithelial cells. Eur Arch Otorhinolaryngol. 2017 Feb;274(2):845-853.