Desmethylazelastine 

Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2^{[1][2][3][4][5]}.

Pharmacokinetic parameters of desmethylazelastine after a single oral administration of 1.0 mg/kg azelastine hydrochloride in guinea pigs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

367.87

C₂₁H₂₂ClN₃O

47491-38-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Chand N, et al. Pharmacodynamic and pharmacokinetic studies with azelastine in the guinea pig: evidence for preferential distribution into the lung. Allergy. 1993 Jan;48(1):19-24.  [Content Brief]

  [2]. Lieberman P, et al. Management of allergic rhinitis with a combination antihistamine/anti-inflammatory agent. J Allergy Clin Immunol. 1999 Mar;103(3 Pt 2):S400-4.  [Content Brief]

  [3]. Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochloridel. Expert Rev Clin Immunol. 2005 Jul;1(2):191-201.  [Content Brief]

  [4]. 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.  [Content Brief]

  [5]. Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1-7.  [Content Brief]