N-Desmethyl Azelastine

Names

[ Name ]:
N-Desmethyl Azelastine

[Synonym ]:
2-(azepan-4-yl)-4-[(4-chlorophenyl)methyl]phthalazin-1-one

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Research Areas >> Infection

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

[In Vivo]

1.19Pharmacokinetic parameters of desmethylazelastine after a single oral administration of 1.0 mg/kg azelastine hydrochloride in guinea pigs[1]. Blood Lung Cmax (ng/mL)[a] 17.6 2863 Tmax (h) 3.0-6.0 4.0-6.0 Tlag (h) 0.25 0.39 AUC0-24 (ng•h/mL)[a] 180 28502 t1/2 (h) 4.24 3.90 CL (L/h) 0.213 Lung-blood ratio[b] 146 146[a] For lung, the unit in grams (g) instead of milliliter (mL).[b] Mean value calculated from all time points.

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.29g/cm3

[ Boiling Point ]:
544.1ºC at 760mmHg

[ Molecular Formula ]:
C₂₁H₂₂ClN₃O

[ Molecular Weight ]:
367.87200

[ Flash Point ]:
282.8ºC

[ Exact Mass ]:
367.14500

[ PSA ]:
46.92000

[ LogP ]:
4.28410

[ Index of Refraction ]:
1.66

Synthetic Route

Click to get detail synthetic route

Related Compounds

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