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].

Product Specifications

CAS Number

[47491-38-3]

UNSPSC

12352005

Hazard Statement

H302

Target

Drug Metabolite

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Infection; Metabolic Disease; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/desmethylazelastine.html

Solubility

10 mM in DMSO

Smiles

O=C1C2=C(C(CC3=CC=C(C=C3)Cl)=NN1C4CCNCCC4)C=CC=C2

Molecular Formula

C21H22ClN3O

Molecular Weight

367.87

Precautions

P264-P270-P330-P501

References & Citations

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