47491-38-3

47491-38-3 structure

Name: N-Desmethyl Azelastine
Chemical Name: N-Desmethyl Azelastine
CAS Number: 47491-38-3
Molecular Formula: C₂₁H₂₂ClN₃O
Molecular Weight: 367.87200
Catalog: Research Areas Cardiovascular Disease
Create Date: 2017-01-08 03:27:14
Modify Date: 2024-01-08 12:14:41
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].

Name	N-Desmethyl Azelastine
Synonyms	2-(azepan-4-yl)-4-[(4-chlorophenyl)methyl]phthalazin-1-one

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.

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

955359-87-2

47491-38-3

Literature: GLAXO GROUP LIMITED Patent: WO2007/122156 A1, 2007 ; Location in patent: Page/Page column 67 ; WO 2007/122156 A1

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